Molecules

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Open AccessArticle

Down Regulation of CIAPIN1 Reverses Multidrug Resistance in Human Breast Cancer Cells by Inhibiting MDR1

by Dan Lu, Zhibo Xiao, Wenxiu Wang, Yuqing Xu, Shujian Gao, Lili Deng, Wen He, Yu Yang, Xiaofei Guo and Xuemei Wang

Molecules 2012, 17(6), 7595-7611; https://doi.org/10.3390/molecules17067595 - 20 Jun 2012

Cited by 21 | Viewed by 6224

Abstract

Cytokine-induced apoptosis inhibitor 1 (CIAPIN1), initially named anamorsin, a newly indentified antiapoptotic molecule is a downstream effector of the receptor tyrosine kinase-Ras signaling pathway. Current study has revealed that CIAPIN1 may have wide and important functions, especially due to its close correlations with [...] Read more.

Cytokine-induced apoptosis inhibitor 1 (CIAPIN1), initially named anamorsin, a newly indentified antiapoptotic molecule is a downstream effector of the receptor tyrosine kinase-Ras signaling pathway. Current study has revealed that CIAPIN1 may have wide and important functions, especially due to its close correlations with malignant tumors. However whether or not it is involved in the multi-drug resistance (MDR) process of breast cancer has not been elucidated. To explore the effect of CIAPIN1 on MDR, we examined the expression of P-gp and CIAPIN1 by immunohistochemistry and found there was positive correlation between them. Then we successfully interfered with RNA translation by the infection of siRNA of CIAPIN1 into MCF7/ADM breast cancer cell lines through a lentivirus, and the expression of the target gene was significantly inhibited. After RNAi the drug resistance was reduced significantly and the expression of MDR1mRNA and P-gp in MCF7/ADM cell lines showed a significant decrease. Also the expression of P53 protein increased in a statistically significant way (p ≤ 0.01) after RNAi exposure. In addition, flow cytometry analysis reveals that cell cycle and anti-apoptotic enhancing capability of cells changed after RNAi treatment. These results suggested CIAPIN1 may participate in breast cancer MDR by regulating MDR1 and P53 expression, changing cell cycle and enhancing the anti-apoptotic capability of cells. Full article

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282 KiB

Open AccessArticle

Effect of Acid and Base Catalyzed Hydrolysis on the Yield of Phenolics and Antioxidant Activity of Extracts from Germinated Brown Rice (GBR)

by Ismaila Muhammad Sani, Shahid Iqbal, Kim Wei Chan and Maznah Ismail

Molecules 2012, 17(6), 7584-7594; https://doi.org/10.3390/molecules17067584 - 19 Jun 2012

Cited by 48 | Viewed by 7353

Abstract

The influence of both acidic and basic hydrolysis on the yield, total phenolic content and antioxidative capacity of methanolic extract of germinated brown rice (GBR) was studied. Total phenolic content (TPC), total flavonoid content (TFC), 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical [...] Read more.

The influence of both acidic and basic hydrolysis on the yield, total phenolic content and antioxidative capacity of methanolic extract of germinated brown rice (GBR) was studied. Total phenolic content (TPC), total flavonoid content (TFC), 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical cation scavenging, and ferric reducing antioxidant power (FRAP) tests were used for the measurement of antioxidant ability. There was a significant difference (p < 0.05) in the TPC and DPPH radical scavenging assay results when comparing neutral with acidic and basic catalysed hydrolysis. The yield of the crude extract was slightly higher in acidic hydrolysis than in basic hydrolysis (p > 0.05). The TPC and TFC were highest in acidic hydrolysis. A significant correlation was observed between ABTS radical cation scavenging and FRAP. The antioxidant activity measured using DPPH radical scavenging assay showed high activity in acidic hydrolysis, while the ABTS radical cationscavenging activity and FRAP showed the highest values in basic hydrolysis. The samples were further evaluated using HPLC to determine the individual phenolic concentrations in different hydrolytic media contributing to the antioxidant effects. This study revealed that acidic and basic hydrolysis can improve the yield, phenolic content, and antioxidant activity of germinated brown rice. Full article

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365 KiB

Open AccessArticle

Synthesis of Main-Chain Chiral Quaternary Ammonium Polymers for Asymmetric Catalysis Using Quaternization Polymerization

by Naoki Haraguchi, Parbhej Ahamed, Md. Masud Parvez and Shinichi Itsuno

Molecules 2012, 17(6), 7569-7583; https://doi.org/10.3390/molecules17067569 - 19 Jun 2012

Cited by 17 | Viewed by 7737

Abstract

Main-chain chiral quaternary ammonium polymers were successfully synthesized by the quaternization polymerization of cinchonidine dimer with dihalides. The polymerization occurred smoothly under optimized conditions to give novel type of main-chain chiral quaternary ammonium polymers. The catalytic activity of the polymeric chiral organocatalysts was [...] Read more.

Main-chain chiral quaternary ammonium polymers were successfully synthesized by the quaternization polymerization of cinchonidine dimer with dihalides. The polymerization occurred smoothly under optimized conditions to give novel type of main-chain chiral quaternary ammonium polymers. The catalytic activity of the polymeric chiral organocatalysts was investigated on the asymmetric benzylation of N-(diphenylmethylidene)glycine tert-butyl ester. Full article

(This article belongs to the Special Issue Asymmetric Catalysis)

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335 KiB

Open AccessArticle

Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of Oridonin as Potential Anti-Tumor Agents

by Dahong Li, Lei Wang, Hao Cai, Yihua Zhang and Jinyi Xu

Molecules 2012, 17(6), 7556-7568; https://doi.org/10.3390/molecules17067556 - 18 Jun 2012

Cited by 36 | Viewed by 7243

Abstract

To search for novel nitric oxide (NO) releasing anti-tumor agents, a series of novel furoxan/oridonin hybrids were designed and synthesized. Firstly, the nitrate/nitrite levels in the cell lysates were tested by a Griess assay and the results showed that these furoxan-based NO-releasing derivatives [...] Read more.

To search for novel nitric oxide (NO) releasing anti-tumor agents, a series of novel furoxan/oridonin hybrids were designed and synthesized. Firstly, the nitrate/nitrite levels in the cell lysates were tested by a Griess assay and the results showed that these furoxan-based NO-releasing derivatives could produce high levels of NO in vitro. Then the anti-proliferative activity of these hybrids against four human cancer cell lines was also determined, among which, 9h exhibited the most potential anti-tumor activity with IC₅₀ values of 1.82 µM against K562, 1.81 µM against MGC-803 and 0.86 µM against Bel-7402, respectively. Preliminary structure-activity relationship was concluded based on the experimental data obtained. These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel anti-tumor agents. Full article

(This article belongs to the Collection Bioactive Compounds)

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287 KiB

Open AccessArticle

Design, Synthesis and Antiviral Potential of 14-Aryl/Heteroaryl-14H-dibenzo[a,j]xanthenes Using an Efficient Polymer-Supported Catalyst

by Kalla Reddi Mohan Naidu, Balam Satheesh Krishna, Mungara Anil Kumar, Palanisamy Arulselvan, Shaik Ibrahim Khalivulla and Ola Lasekan

Molecules 2012, 17(6), 7543-7555; https://doi.org/10.3390/molecules17067543 - 18 Jun 2012

Cited by 80 | Viewed by 7041

Abstract

Polyethyleneglycol bound sulfonic acid (PEG-OSO₃H), a chlorosulphonic acid-modified polyethylene glycol was successfully used as an efficient and eco-friendly polymeric catalyst in the synthesis of 14-aryl/heteroaryl-14H-dibenzo[a,j]xanthenes obtained from the reaction of 2-naphthol and carbonyl compounds under solvent-free conditions [...] Read more.

Polyethyleneglycol bound sulfonic acid (PEG-OSO₃H), a chlorosulphonic acid-modified polyethylene glycol was successfully used as an efficient and eco-friendly polymeric catalyst in the synthesis of 14-aryl/heteroaryl-14H-dibenzo[a,j]xanthenes obtained from the reaction of 2-naphthol and carbonyl compounds under solvent-free conditions with short reaction times and excellent yields. The biological properties of these synthesized title compounds revealed that compounds 3b, 3c, 3f and 3i showed highly significant anti-viral activity against tobacco mosaic virus. Full article

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Open AccessArticle

The Joint Action of Destruxins and Botanical Insecticides (Rotenone, Azadirachtin and Paeonolum) Against the Cotton Aphid, Aphis gossypii Glover

by Fei Yi, Chunhua Zou, Qiongbo Hu and Meiying Hu

Molecules 2012, 17(6), 7533-7542; https://doi.org/10.3390/molecules17067533 - 18 Jun 2012

Cited by 31 | Viewed by 5768

Abstract

The joint action of destruxins and three botanical insecticides, rotenone (Rot), azadirachtin (Aza) and paeonolum (Pae) against the cotton aphid, Aphis gossypii, was bioassayed. In laboratory experiment, several synergistic groups of destruxins with botanical insecticides were found by means of Sun’s Co-toxicity [...] Read more.

The joint action of destruxins and three botanical insecticides, rotenone (Rot), azadirachtin (Aza) and paeonolum (Pae) against the cotton aphid, Aphis gossypii, was bioassayed. In laboratory experiment, several synergistic groups of destruxins with botanical insecticides were found by means of Sun’s Co-toxicity Coefficients (CTC) and Finney’s Synergistic Coefficient (SC). The best synergistic effect was discovered in the ratio group Des/Rot 1/9 with the CTC or SC and LC₅₀ values of 479.93 or 4.8 and 0.06 μg/mL, respectively. The second and third synergistic effects were recorded in the ratio groups Des/Rot 7/3 and 9/1. Although the ratio groups Des/Aza 6/4, Des/Pae 4/6, 3/7 and 2/8 indicated synergism by Sun’s CTC, they were determined as additive actions by Finney’s SC. Additive actions were also found in most of the ratio groups, but antagonism were recorded only in three ratio groups: Des/Pae 9/1, 7/3 and 6/4. In greenhouse tests, the highest mortality was 98.9% with the treatment Des/Rot 1/9 at 0.60 μg/mL, meanwhile, the treatments Des/Pae 4/6 and Des/Aza 6/4 had approximately 88% mortality. Full article

(This article belongs to the Section Natural Products Chemistry)

234 KiB

Open AccessCommunication

Enantioselective Michael Addition of 3-Aryl-Substituted Oxindoles to Methyl Vinyl Ketone Catalyzed by a Binaphthyl-Modified Bifunctional Organocatalyst

by Hyun Joo Lee, Saet Byeol Woo and Dae Young Kim

Molecules 2012, 17(6), 7523-7532; https://doi.org/10.3390/molecules17067523 - 18 Jun 2012

Cited by 30 | Viewed by 6526

Abstract

The enantioselective conjugate addition reaction of 3-aryl-substituted oxindoles with methyl vinyl ketone promoted by binaphthyl-modified bifunctional organocatalysts was investigated. The corresponding Michael adducts, containing a quaternary center at the C3-position of the oxindoles, were generally obtained in high yields with excellent enantioselectivities (up [...] Read more.

The enantioselective conjugate addition reaction of 3-aryl-substituted oxindoles with methyl vinyl ketone promoted by binaphthyl-modified bifunctional organocatalysts was investigated. The corresponding Michael adducts, containing a quaternary center at the C3-position of the oxindoles, were generally obtained in high yields with excellent enantioselectivities (up to 91% ee). Full article

(This article belongs to the Special Issue Asymmetric Catalysis)

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Open AccessArticle

Guanidine Affects Differentially the Twitch Response of Diaphragm, Extensor Digitorum Longus and Soleus Nerve-Muscle Preparations of Mice

by Rosana Ferrari, Léa Rodrigues-Simioni and Maria Alice Da Cruz Höfling

Molecules 2012, 17(6), 7503-7522; https://doi.org/10.3390/molecules17067503 - 15 Jun 2012

Cited by 1 | Viewed by 5291

Abstract

Guanidine has been used with some success to treat myasthenia gravis and myasthenic syndrome because it increases acetylcholine release at nerve terminals through K⁺, Na⁺ and Ca²⁺ channels-involving mechanisms. Currently, guanidine derivatives have been proposed for treatment of several [...] Read more.

Guanidine has been used with some success to treat myasthenia gravis and myasthenic syndrome because it increases acetylcholine release at nerve terminals through K⁺, Na⁺ and Ca²⁺ channels-involving mechanisms. Currently, guanidine derivatives have been proposed for treatment of several diseases. Studies aimed at providing new insights to the drug are relevant. Experimentally, guanidine (10 mM) induces on mouse phrenic nerve-diaphragm (PND) preparations neurotransmission facilitation followed by blockade and a greatest secondary facilitation after its removal from bath. Herein, we hypothesized that this peculiar triphasic response may differ in muscles with distinct twitch/metabolic characteristics. Morphological alterations and contractile response of PND, extensor digitorum longus (EDL) and soleus (SOL) preparations incubated with guanidine (10 mM) for 15, 30, 60 min were analyzed. Guanidine concentrations of 5 mM (for PND and EDL) and 1 mM (for EDL) were also tested. Guanidine triphasic effect was only observed on PND regardless the concentration. The morphological alterations in muscle tissue varied along time but did not impede the PND post-wash facilitation. Higher doses (20–25 mM) did not increase EDL or SOL neurotransmission. The data suggest a complex mechanism likely dependent on the metabolic/contractile muscle phenotype; muscle fiber types and density/type of ion channels, sarcoplasmic reticulum and mitochondria organization may have profound impact on the levels and isoform expression pattern of Ca²⁺ regulatory membrane proteins so reflecting regulation of calcium handling and contractile response in different types of muscle. Full article

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Open AccessReview

Ionic Liquids — Promising but Challenging Solvents for Homogeneous Derivatization of Cellulose

by Martin Gericke, Pedro Fardim and Thomas Heinze

Molecules 2012, 17(6), 7458-7502; https://doi.org/10.3390/molecules17067458 - 15 Jun 2012

Cited by 299 | Viewed by 15901

Abstract

In the past decade, ionic liquids (ILs) have received enormous interest as solvents for cellulose. They have been studied intensively for fractionation and biorefining of lignocellulosic biomass, for dissolution of the polysaccharide, for preparation of cellulosic fibers, and in particular as reaction media [...] Read more.

In the past decade, ionic liquids (ILs) have received enormous interest as solvents for cellulose. They have been studied intensively for fractionation and biorefining of lignocellulosic biomass, for dissolution of the polysaccharide, for preparation of cellulosic fibers, and in particular as reaction media for the homogeneous preparation of highly engineered polysaccharide derivatives. ILs show great potential for application on a commercial scale regarding recyclability, high dissolution power, and their broad structural diversity. However, a critical analysis reveals that these promising features are combined with serious drawbacks that need to be addressed in order to utilize ILs for the efficient synthesis of cellulose derivatives. This review presents a comprehensive overview about chemical modification of cellulose in ILs. Difficulties encountered thereby are discussed critically and current as well as future developments in this field of polysaccharide research are outlined. Full article

(This article belongs to the Collection Ionic Liquids)

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966 KiB

Open AccessShort Note

An Oxidized Squalene Derivative from Protium subserratum Engl. (Engl.) Growing in Peru

by John Lokvam and Paul V. A. Fine

Molecules 2012, 17(6), 7451-7457; https://doi.org/10.3390/molecules17067451 - 15 Jun 2012

Cited by 7 | Viewed by 4621

Abstract

Protium subserratum (Burseraceae) is a neotropical tree species that is comprised of several habitat-specific ecotypes having distinct defense chemical profiles. A previously unknown triterpene, 25,30-dicarboxy-26,27,28,29-tetraacetoxy-10,11,14,15-tetrahydrosqualene, was isolated from P. subserratum young leaf tissue of one ecotype growing in Peru. The structure of 1 [...] Read more.

Protium subserratum (Burseraceae) is a neotropical tree species that is comprised of several habitat-specific ecotypes having distinct defense chemical profiles. A previously unknown triterpene, 25,30-dicarboxy-26,27,28,29-tetraacetoxy-10,11,14,15-tetrahydrosqualene, was isolated from P. subserratum young leaf tissue of one ecotype growing in Peru. The structure of 1 was determined by spectroscopic study, including 1 and 2D nuclear magnetic resonance experiments. Full article

(This article belongs to the Section Natural Products Chemistry)

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Open AccessArticle

NIR Spectroscopic Properties of Aqueous Acids Solutions

by Ahmad Fairuz Omar, Hanafi Atan and Mohd Zubir MatJafri

Molecules 2012, 17(6), 7440-7450; https://doi.org/10.3390/molecules17067440 - 15 Jun 2012

Cited by 33 | Viewed by 6386

Abstract

Acid content is one of the important quality attributes in determining the maturity index of agricultural product, particularly fruits. Despite the fact that much research on the measurement of acidity in fruits through non-destructive spectroscopy analysis at NIR wavelengths between 700 to 1,000 [...] Read more.

Acid content is one of the important quality attributes in determining the maturity index of agricultural product, particularly fruits. Despite the fact that much research on the measurement of acidity in fruits through non-destructive spectroscopy analysis at NIR wavelengths between 700 to 1,000 nm has been conducted, the same response towards individual acids is not well known. This paper presents NIR spectroscopy analysis on aqueous citric, tartaric, malic and oxalic solutions through quantitative analysis by selecting a set of wavelengths that can best be used to measure the pH of the solutions. The aquaphotomics study of the acid solutions has generated R² above 0.9 for the measurement of all acids. The most important wavelengths for pH are located at 918–925 nm and 990–996 nm, while at 975 nm for water. Full article

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Open AccessArticle

Application of 4D-QSAR Studies to a Series of Raloxifene Analogs and Design of Potential Selective Estrogen Receptor Modulators

by Ana Carolina Rennó Sodero, Nelilma Correia Romeiro, Elaine Fontes Ferreira Da Cunha, Uiaran De Oliveira Magalhães, Ricardo Bicca De Alencastro, Carlos Rangel Rodrigues, Lúcio Mendes Cabral, Helena Carla Castro and Magaly Girão Albuquerque

Molecules 2012, 17(6), 7415-7439; https://doi.org/10.3390/molecules17067415 - 15 Jun 2012

Cited by 12 | Viewed by 6028

Abstract

Four-dimensional quantitative structure-activity relationship (4D-QSAR) analysis was applied on a series of 54 2-arylbenzothiophene derivatives, synthesized by Grese and coworkers, based on raloxifene (an estrogen receptor-alpha antagonist), and evaluated as ERa ligands and as inhibitors of estrogen-stimulated proliferation of MCF-7 breast cancer cells. [...] Read more.

Four-dimensional quantitative structure-activity relationship (4D-QSAR) analysis was applied on a series of 54 2-arylbenzothiophene derivatives, synthesized by Grese and coworkers, based on raloxifene (an estrogen receptor-alpha antagonist), and evaluated as ERa ligands and as inhibitors of estrogen-stimulated proliferation of MCF-7 breast cancer cells. The conformations of each analogue, sampled from a molecular dynamics simulation, were placed in a grid cell lattice according to three trial alignments, considering two grid cell sizes (1.0 and 2.0 Å). The QSAR equations, generated by a combined scheme of genetic algorithms (GA) and partial least squares (PLS) regression, were evaluated by “leave-one-out” cross-validation, using a training set of 41 compounds. External validation was performed using a test set of 13 compounds. The obtained 4D-QSAR models are in agreement with the proposed mechanism of action for raloxifene. This study allowed a quantitative prediction of compounds’ potency and supported the design of new raloxifene analogs. Full article

(This article belongs to the Special Issue QSAR and Its Applications)

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Open AccessArticle

A Monoclonal Antibody-Based ELISA for Multiresidue Determination of Avermectins in Milk

by Chunmei Wang, Zhanhui Wang, Wenxiao Jiang, Tiejun Mi and Jianzhong Shen

Molecules 2012, 17(6), 7401-7414; https://doi.org/10.3390/molecules17067401 - 15 Jun 2012

Cited by 14 | Viewed by 5645

Abstract

Due to the widespread use and potential toxicity of avermectins (AVMs), multi-residue monitoring of AVMs in edible tissues, especially in milk, has become increasingly important. With the aim of developing a broad-selective immunoassay for AVMs, a broad-specific monoclonal antibody (Mab) was raised. Based [...] Read more.

Due to the widespread use and potential toxicity of avermectins (AVMs), multi-residue monitoring of AVMs in edible tissues, especially in milk, has become increasingly important. With the aim of developing a broad-selective immunoassay for AVMs, a broad-specific monoclonal antibody (Mab) was raised. Based on this Mab, a homologous indirect enzyme-linked immunosorbent assay (ELISA) for the rapid detection of AVMs in milk was developed. Under the optimized conditions, the IC₅₀ values in assay buffer were estimated to be 3.05 ng/mL for abamectin, 13.10 ng/mL for ivermectin, 38.96 ng/mL for eprinomectin, 61.00 ng/mL for doramectin, 14.38 ng/mL for emamectin benzoate. Detection capability (CCβ) of the ELISA was less than 5 ng/mL and 2 ng/mL in milk samples prepared by simple dilution and solvent extraction, respectively. The optimized ELISA was used to quantify AVMs in milk samples spiked at different amounts. The mean recovery and coefficient of variation (CV) were 95.90% and 15.42%, respectively. The Mab-based ELISA achieved a great improvement in AVMs detection. Results proved this broad-selective ELISA would be useful for the multi-residue determination of AVMs in milk without purification process. Full article

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Open AccessArticle

Application of 2,3-Naphthalenediamine in Labeling Natural Carbohydrates for Capillary Electrophoresis

by Chien-Yuan Kuo, Shwu-Huey Wang, Chunchi Lin, Sylvain Kuo-Shiang Liao, Wei-Ting Hung, Jim-Min Fang and Wen-Bin Yang

Molecules 2012, 17(6), 7387-7400; https://doi.org/10.3390/molecules17067387 - 15 Jun 2012

Cited by 11 | Viewed by 5696

Abstract

Neutral and acidic monosaccharide components in Ganoderma lucidum polysaccharide are readily labeled with 2,3-naphthalenediamine, and the resulting saccharide-naphthimidazole (NAIM) derivatives are quantified by capillary electrophoresis (CE) in borate buffer. Using sulfated-α-cyclodextrin as the chiral selector, enantiomers of monosaccharide-NAIMs are resolved on CE in [...] Read more.

Neutral and acidic monosaccharide components in Ganoderma lucidum polysaccharide are readily labeled with 2,3-naphthalenediamine, and the resulting saccharide-naphthimidazole (NAIM) derivatives are quantified by capillary electrophoresis (CE) in borate buffer. Using sulfated-α-cyclodextrin as the chiral selector, enantiomers of monosaccharide-NAIMs are resolved on CE in phosphate buffer, allowing a simultaneous determination of the absolute configuration and sugar composition in the mucilage polysaccharide of a medicinal herb Dendrobium huoshanense. Together with the specific enzymatic reactions of various glycoside hydrolases on the NAIM derivatives of glycans, the structures of natural glycans can be deduced from the digestion products identified by CE analysis. Though heparin dissachrides could be successfully derived with the NAIM-labeling method, the heparin derivatives with the same degree of sulfation could not be separated by CE. Full article

(This article belongs to the Section Natural Products Chemistry)

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Open AccessCommunication

Substituted Benzamides Containing Azaspiro Rings as Upregulators of Apolipoprotein A-I Transcription

by Yu Du, Yuan Yang, Wei Jiang, Li Wang, Xiao-Jian Jia, Shu-Yi Si, Xiao-Fang Chen and Bin Hong

Molecules 2012, 17(6), 7379-7386; https://doi.org/10.3390/molecules17067379 - 14 Jun 2012

Cited by 7 | Viewed by 4863

Abstract

Apolipoprotein A-I (Apo A-I) is the principal protein component of high density lipoprotein (HDL), which is generally considered as a potential therapeutic target against atherosclerosis. The understanding of the Apo A-I regulation mechanism has fuelled the development of novel HDL targeted therapeutic approaches. [...] Read more.

Apolipoprotein A-I (Apo A-I) is the principal protein component of high density lipoprotein (HDL), which is generally considered as a potential therapeutic target against atherosclerosis. The understanding of the Apo A-I regulation mechanism has fuelled the development of novel HDL targeted therapeutic approaches. To identify novel agents that can upregulate Apo A-I expression, we performed a cell-based reporter assay to screen 25,600 small molecules. Based on the dataset obtained from screening, a series of novel analogs of substituted benzamides containing azaspiro rings were assessed for their ability to induce the transcription of the Apo A-I gene, and the structure-activity relationship (SAR) around these analogs was also proposed. The results indicated that the trifluoromethyl substituted benzamide containing an azaspiro ring is a promising backbone for designing Apo A-I transcriptional upregulator and could be viable leads for development of new drugs to prevent and treat atherosclerosis in the future. Full article

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Open AccessArticle

A New Method for Production of Chiral 2-Aryl-2-fluoropropanoic Acids Using an Effective Kinetic Resolution of Racemic 2-Aryl-2-fluoropropanoic Acids

by Atsushi Tengeiji and Isamu Shiina

Molecules 2012, 17(6), 7356-7378; https://doi.org/10.3390/molecules17067356 - 14 Jun 2012

Cited by 14 | Viewed by 6936

Abstract

We report a new method for the preparation of chiral 2-aryl-2-fluoropropanoic acids, including 2-fluoroibuprofen, a fluorinated analogue of non-steroidal anti-inflammatory drugs (NSAIDs), by the kinetic resolution of racemic 2-aryl-2-fluoropropanoic acids using enantioselective esterification. By applying pivalic anhydride (Piv₂O) as a coupling [...] Read more.

We report a new method for the preparation of chiral 2-aryl-2-fluoropropanoic acids, including 2-fluoroibuprofen, a fluorinated analogue of non-steroidal anti-inflammatory drugs (NSAIDs), by the kinetic resolution of racemic 2-aryl-2-fluoropropanoic acids using enantioselective esterification. By applying pivalic anhydride (Piv₂O) as a coupling agent, bis(α-naphthyl)methanol [(α-Np)₂CHOH] as an achiral alcohol, and (+)-benzotetramisole (BTM) as a chiral acyl-transfer catalyst, a series of racemic 2-aryl-2-fluoropropanoic acids were kinetically separated to afford the optically active carboxylic acids and the corresponding esters with good to high enantiomeric excesses. This technology can provide a convenient approach to furnish the chiral α-fluorinated drugs containing quaternary carbons at the α-positions in the 2-aryl-2-fluoropropanoic acid structure. Full article

(This article belongs to the Special Issue Asymmetric Catalysis)

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Open AccessArticle

Ring-Expansion Reaction of Oximes with Aluminum Reductants

by Hidetsura Cho, Yusuke Iwama, Nakako Mitsuhashi, Kenji Sugimoto, Kentaro Okano and Hidetoshi Tokuyama

Molecules 2012, 17(6), 7348-7355; https://doi.org/10.3390/molecules17067348 - 14 Jun 2012

Cited by 22 | Viewed by 7044

Abstract

The ring-expansion reactions of heterocyclic ketoximes and carbocyclic ketoximes with several reductants such as AlHCl₂, AlH₃ (alane), LiAlH₄, LiAlH(O^tBu)₃, and (MeOCH₂CH₂O)₂AlH₂Na (Red-Al) were examined. Among reductants, [...] Read more.

The ring-expansion reactions of heterocyclic ketoximes and carbocyclic ketoximes with several reductants such as AlHCl₂, AlH₃ (alane), LiAlH₄, LiAlH(O^tBu)₃, and (MeOCH₂CH₂O)₂AlH₂Na (Red-Al) were examined. Among reductants, AlHCl₂ (LiAlH₄:AlCl₃ = 1:3) in cyclopentyl methyl ether (CPME) has been found to be a suitable reagent for the reaction, and the rearranged cyclic secondary amines were obtained in good to excellent yields. Full article

(This article belongs to the Special Issue Heterocycles)

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Open AccessArticle

Isolation and Partial Characterization of an Antifungal Protein Produced by Bacillus licheniformis BS-3

by Tang-Bing Cui, Hai-Yun Chai and Li-Xiang Jiang

Molecules 2012, 17(6), 7336-7347; https://doi.org/10.3390/molecules17067336 - 14 Jun 2012

Cited by 31 | Viewed by 6565

Abstract

An antifungal protein produced by Bacillus licheniformis strain BS-3 was purified to homogeneity by ammonium sulfate precipitation, DEAE-52 column chromatography and Sephadex G-75 column chromatography. The purified protein was designated as F2 protein, inhibited the growth of Aspergillus niger, Magnaporthe oryzae and [...] Read more.

An antifungal protein produced by Bacillus licheniformis strain BS-3 was purified to homogeneity by ammonium sulfate precipitation, DEAE-52 column chromatography and Sephadex G-75 column chromatography. The purified protein was designated as F2 protein, inhibited the growth of Aspergillus niger, Magnaporthe oryzae and Rhizoctonia solani. F2 protein was a monomer with approximately molecular weight of 31 kDa in sodium dodecyl sulfate-polyacrylamide gel electrophoresis and gave a single peak on High Performance Liquid Chromatography (HPLC). Using Rhizoctonia solani as the indicator strain, the EC₅₀ of F2 protein was 35.82 µg/mL, displaying a higher antifungal activity in a range of pH 6.0 to pH 10.0, and at a temperature below 70 °C for 30 min. F2 protein was moderately resistant to hydrolysis by trypsin, proteinase K, after which its relative activities were 41.7% and 59.5%, respectively. F2 protein was assayed using various substrates to determine the enzymatic activities, the results showed the hydrolyzing activity on casein, however, no enzymatic activities on colloidal chitin, CM-cellulose, xylan, M. lysodeikticus, and p-nitrophenyl-N-acetylglucosaminide. Full article

(This article belongs to the Section Natural Products Chemistry)

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Open AccessArticle

Optimizing the Extraction of Anti-tumor Polysaccharides from the Fruit of Capparis spionosa L. by Response Surface Methodology

by Yu-Bin Ji, Fang Dong, Dong-Bin Ma, Jing Miao, Li-Na Jin, Zhen-Feng Liu and Ling-Wen Zhang

Molecules 2012, 17(6), 7323-7335; https://doi.org/10.3390/molecules17067323 - 14 Jun 2012

Cited by 34 | Viewed by 5852

Abstract

Capparis spionosa L. is a traditional medicinal plant in China and central Asia. In this study, an experiment was designed to investigate the optimization of the extraction of anti-tumor polysaccharides from the fruit of Capparis spionosa L. (CSPS) by response surface methodology (RSM). [...] Read more.

Capparis spionosa L. is a traditional medicinal plant in China and central Asia. In this study, an experiment was designed to investigate the optimization of the extraction of anti-tumor polysaccharides from the fruit of Capparis spionosa L. (CSPS) by response surface methodology (RSM). Four independent variables (extraction temperature, extraction time, ratio of water to sample and extraction cycles) were explored. Meanwhile, the in vivo anti-tumor activity of CSPS was investigated. The results showed that the experimental data could be fitted to a second-order polynomial equation using multiple regression analysis. The optimum extraction conditions were as follows: extraction temperature 92 °C, extraction time 140 min, ratio of water to sample 26 mL/g, and three extraction cycle. Under these conditions, the yield of polysaccharides reached 13.01%, which was comparable to the predicted yield (12.94%, p > 0.05). This indicated that the model was adequate for the extraction process. Additionally, CSPS could prolong the survival time of H₂₂ bearing mice in vivo. The anti-tumor activities of CSPS were dose-dependent. Full article

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245 KiB

Open AccessArticle

Impact of Soil Field Water Capacity on Secondary Metabolites, Phenylalanine Ammonia-lyase (PAL), Maliondialdehyde (MDA) and Photosynthetic Responses of Malaysian Kacip Fatimah (Labisia pumila Benth)

by Hawa Z. E. Jaafar, Mohd Hafiz Ibrahim and Nur Farhana Mohamad Fakri

Molecules 2012, 17(6), 7305-7322; https://doi.org/10.3390/molecules17067305 - 13 Jun 2012

Cited by 118 | Viewed by 8009

Abstract

A randomized complete block design 2 × 4 experiment was designed and conducted for 15 weeks to characterize the relationships between production of total phenolics, flavonoid, anthocyanin, leaf gas exchange, total chlorophyll, phenylalanine ammonia-lyase (PAL) and malondialdehyde (MDA) activity in two varieties of [...] Read more.

A randomized complete block design 2 × 4 experiment was designed and conducted for 15 weeks to characterize the relationships between production of total phenolics, flavonoid, anthocyanin, leaf gas exchange, total chlorophyll, phenylalanine ammonia-lyase (PAL) and malondialdehyde (MDA) activity in two varieties of Labisia pumila Benth, namely the var. alata and pumila, under four levels of evapotranspiration replacement (ER) (100%; well watered), (75%, moderate water stress), (50%; high water stress) and (25%; severe water stress). The production of total phenolics, flavonoids, anthocyanin, soluble sugar and relative leaf water content was affected by the interaction between varieties and SWC. As the ER levels decreased from 100% to 25%, the production of PAL and MDA activity increased steadily. At the highest (100%) ER L. pumila exhibited signiﬁcantly higher net photosynthesis, apparent quantum yield, maximum efficiency of photosystem II (f_v/f_m) and lower dark respiration rates compared to the other treatment. The production of total phenolics, flavonoids and anthocyanin was also found to be higher under high water stress (50% ER replacement) compared to severe water stress (25% ER). From this study, it was observed that as net photosynthesis, apparent quantum yield and chlorophyll content were downregulated under high water stress the production of total phenolics, flavonoids and anthocyanin were upregulated implying that the imposition of high water stress can enhance the medicinal properties of L. pumila Benth. Full article

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Open AccessArticle

Antioxidant Activity of Various Parts of Cinnamomum cassia Extracted with Different Extraction Methods

by Cheng-Hong Yang, Rong-Xian Li and Li-Yeh Chuang

Molecules 2012, 17(6), 7294-7304; https://doi.org/10.3390/molecules17067294 - 13 Jun 2012

Cited by 107 | Viewed by 10998

Abstract

The aim of this study was to investigate the antioxidant activities of various parts (barks, buds, and leaves) of Cinnamomum cassia extracted with ethanol and supercritical fluid extraction (SFE). For the antioxidant activity comparison, IC₅₀ values ofthe SFE and ethanol extracts [...] Read more.

The aim of this study was to investigate the antioxidant activities of various parts (barks, buds, and leaves) of Cinnamomum cassia extracted with ethanol and supercritical fluid extraction (SFE). For the antioxidant activity comparison, IC₅₀ values ofthe SFE and ethanol extracts in the DPPH scavenging assay were 0.562–10.090 mg/mL and 0.072–0.208 mg/mL, and the Trolox equivalent antioxidant capacity (TEAC) values were 6.789–58.335 mmole Trolox/g and 133.039–335.779 mmole Trolox/g, respectively. In addition, the total flavonoid contents were 0.031–1.916 g/ 100 g dry weight of materials (DW) and 2.030–3.348 g/ 100 g DW, and the total phenolic contents were 0.151–2.018 g/ 100 g DW and 6.313–9.534 g/ 100 g DW in the SFE and ethanol extracts, respectively. Based on the results, the ethanol extracts of Cinnamon barks have potential value as an antioxidant substitute and this study also provide a better technique to extract the natural antioxidant substances from C. cassia. Full article

(This article belongs to the Section Natural Products Chemistry)

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200 KiB

Open AccessArticle

Antibacterial, Antifungal and Cytotoxic Activities of Two Flavonoids from Retama raetam Flowers

by Hayet Edziri, Maha Mastouri, Mohamed Ali Mahjoub, Zine Mighri, Aouni Mahjoub and Luc Verschaeve

Molecules 2012, 17(6), 7284-7293; https://doi.org/10.3390/molecules17067284 - 13 Jun 2012

Cited by 102 | Viewed by 8263

Abstract

We have investigated the antibacterial, antifungal and cytotoxic activities of two flavonoids isolated from Retama raetam flowers using the disc diffusion and micro-dilution broth methods. The cytotoxic activity was tested against Hep-2 cells using the MTT assay. The compounds licoflavone C (1 [...] Read more.

We have investigated the antibacterial, antifungal and cytotoxic activities of two flavonoids isolated from Retama raetam flowers using the disc diffusion and micro-dilution broth methods. The cytotoxic activity was tested against Hep-2 cells using the MTT assay. The compounds licoflavone C (1) and derrone (2) were active against Pseudomonas aeruginosa and Escherichia coli (7.81–15.62 µg/mL) and showed important antifungal activity. Strong antifungal activity against Candida species (7.81 µg/mL) was for example found with compound 2. The tested compounds also showed strong cytotoxicity against Hep-2 cells. These two compounds may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens. Full article

(This article belongs to the Section Natural Products Chemistry)

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482 KiB

Open AccessReview

Hypervalent Nonbonded Interactions of a Divalent Sulfur Atom. Implications in Protein Architecture and the Functions

by Michio Iwaoka and Noriyoshi Isozumi

Molecules 2012, 17(6), 7266-7283; https://doi.org/10.3390/molecules17067266 - 13 Jun 2012

Cited by 119 | Viewed by 8481

Abstract

In organic molecules a divalent sulfur atom sometimes adopts weak coordination to a proximate heteroatom (X). Such hypervalent nonbonded S···X interactions can control the molecular structure and chemical reactivity of organic molecules, as well as their assembly and packing in the solid state. [...] Read more.

In organic molecules a divalent sulfur atom sometimes adopts weak coordination to a proximate heteroatom (X). Such hypervalent nonbonded S···X interactions can control the molecular structure and chemical reactivity of organic molecules, as well as their assembly and packing in the solid state. In the last decade, similar hypervalent interactions have been demonstrated by statistical database analysis to be present in protein structures. In this review, weak interactions between a divalent sulfur atom and an oxygen or nitrogen atom in proteins are highlighted with several examples. S···O interactions in proteins showed obviously different structural features from those in organic molecules (i.e., π_O → σ_S* versus n_O → σ_S* directionality). The difference was ascribed to the HOMO of the amide group, which expands in the vertical direction (π_O) rather than in the plane (n_O). S···X interactions in four model proteins, phospholipase A₂ (PLA₂), ribonuclease A (RNase A), insulin, and lysozyme, have also been analyzed. The results suggested that S···X interactions would be important factors that control not only the three-dimensional structure of proteins but also their functions to some extent. Thus, S···X interactions will be useful tools for protein engineering and the ligand design. Full article

(This article belongs to the Special Issue Hypervalent Compounds)

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216 KiB

Open AccessArticle

Chemical Composition and Insecticidal Activity Against Sitophilus zeamais of the Essential Oils Derived from Artemisia giraldii and Artemisia subdigitata

by Sha-Sha Chu, Zhi-Long Liu, Shu-Shan Du and Zhi-Wei Deng

Molecules 2012, 17(6), 7255-7265; https://doi.org/10.3390/molecules17067255 - 13 Jun 2012

Cited by 37 | Viewed by 5617

Abstract

The aim of this research was to determine the chemical composition and insecticidal activity of the essential oils derived from flowering aerial parts of Artemisia giraldii Pamp. and A. subdigitata Mattf. (Family: Asteraceae) against the maize weevil (Sitophilus zeamais Motsch.). Essential oils [...] Read more.

The aim of this research was to determine the chemical composition and insecticidal activity of the essential oils derived from flowering aerial parts of Artemisia giraldii Pamp. and A. subdigitata Mattf. (Family: Asteraceae) against the maize weevil (Sitophilus zeamais Motsch.). Essential oils of aerial parts of A. giraldii and A. subdigitata were obtained from hydrodistillation and investigated by GC and GC-MS. A total of 48 and 33 components of the essential oils of A. giraldii and A. subdigitata were identified, respectively. The principal compounds in A. giraldii essential oil were β-pinene (13.18%), iso-elemicin (10.08%), germacrene D (5.68%), 4-terpineol (5.43%) and (Z)-β-ocimene (5.06%). 1,8-Cineole (12.26%) and α-curcumene (10.77%) were the two main components of the essential oil of A. subdigitata, followed by β-pinene (7.38%), borneol (6.23%) and eugenol (5.87%). The essential oils of A. giraldii and A. subdigitata possessed fumigant toxicity against the maize weevils with LC₅₀ values of 6.29 and 17.01 mg/L air, respectively. The two essential oils of A. giraldii and A. subdigitata also exhibited contact toxicity against S. zeamais adults with LD₅₀ values of 40.51 and 76.34 µg/adult, respectively. The results indicated that the two essential oils show potential in terms of fumigant and contact toxicity against grain storage insects. Full article

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Open AccessArticle

Aqueous Extracts of the Edible Gracilaria tenuistipitata are Protective Against H₂O₂-Induced DNA Damage, Growth Inhibition, and Cell Cycle Arrest

by Jing-Iong Yang, Chi-Chen Yeh, Jin-Ching Lee, Szu-Cheng Yi, Hurng-Wern Huang, Chao-Neng Tseng and Hsueh-Wei Chang

Molecules 2012, 17(6), 7241-7254; https://doi.org/10.3390/molecules17067241 - 13 Jun 2012

Cited by 61 | Viewed by 8023

Abstract

Potential antioxidant properties of an aqueous extract of the edible red seaweed Gracilaria tenuistipitata (AEGT) against oxidative DNA damage were evaluated. The AEGT revealed several antioxidant molecules, including phenolics, flavonoids and ascorbic acid. In a cell-free assay, the extract exhibited 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical [...] Read more.

Potential antioxidant properties of an aqueous extract of the edible red seaweed Gracilaria tenuistipitata (AEGT) against oxidative DNA damage were evaluated. The AEGT revealed several antioxidant molecules, including phenolics, flavonoids and ascorbic acid. In a cell-free assay, the extract exhibited 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity that significantly reduced H₂O₂-induced plasmid DNA breaks in a dose-response manner (P < 0.001). The AEGT also suppressed H₂O₂-induced oxidative DNA damage in H1299 cells by reducing the percentage of damaged DNA in a dose-response manner (P < 0.001) as measured by a modified alkaline comet-nuclear extract (comet-NE) assay. The MTT assay results showed that AEGT confers significant protection against H₂O₂-induced cytotoxicity and that AEGT itself is not cytotoxic (P < 0.001). Moreover, H₂O₂-induced cell cycle G2/M arrest was significantly released when cells were co-treated with different concentrations of AEGT (P < 0.001). Taken together, these findings suggest that edible red algae Gracilaria water extract can prevent H₂O₂-induced oxidative DNA damage and its related cellular responses. Full article

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Open AccessArticle

Astragalus membranaceus Extract Activates Immune Response in Macrophages via Heparanase

by Qiaojing Qin, Jianying Niu, Zhaoxia Wang, Wangjie Xu, Zhongdong Qiao and Yong Gu

Molecules 2012, 17(6), 7232-7240; https://doi.org/10.3390/molecules17067232 - 13 Jun 2012

Cited by 24 | Viewed by 7103

Abstract

Astragalus membranaceus (AM), a traditional Chinese medicinal herb, has immunoregulatory properties in many diseases. We investigated the effects and mechanism of Astragalus membranaceus extract (AME) in the macrophage migration and immune response mediator release. The viability of Ana-1 macrophages treated with AME was [...] Read more.

Astragalus membranaceus (AM), a traditional Chinese medicinal herb, has immunoregulatory properties in many diseases. We investigated the effects and mechanism of Astragalus membranaceus extract (AME) in the macrophage migration and immune response mediator release. The viability of Ana-1 macrophages treated with AME was evaluated by the MTT method. The secretion and mRNA levels of IL-1β and TNF-a were measured by ELISA and RT-PCR, respectively. Macrophage migration was assayed by transwell assay. The activity of heparanase (HPA) was determined by a heparin-degrading enzyme assay. Our results didn’t show any toxicity of AME in macrophages. AME increased the activity of HPA, cell migration, mRNA levels and secretion of IL-1β and TNF-a in macrophages. Pretreatment with anti-HPA antibody reduced cell migration, secretion of IL-1β and TNF-a did not change the mRNA levels of IL-1β and TNF-a significantly in AME-treated macrophages. This suggests that AME may increase the release of immune response mediator and cell migration via HPA to activate immune response in macrophages. Full article

(This article belongs to the Section Natural Products Chemistry)

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Open AccessArticle

Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

by Mohamed M. Ismail, Mona M. Kamel, Lamia W. Mohamed, Samar I. Faggal and Mai A. Galal

Molecules 2012, 17(6), 7217-7231; https://doi.org/10.3390/molecules17067217 - 12 Jun 2012

Cited by 33 | Viewed by 5472

Abstract

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b [...] Read more.

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil. Full article

(This article belongs to the Section Medicinal Chemistry)

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Open AccessArticle

Liquiritigenin Inhibits Tumor Growth and Vascularization in a Mouse Model of Hela Cells

by Yuxin Liu, Sirou Xie, Yu Wang, Kang Luo, Yang Wang and Yunqing Cai

Molecules 2012, 17(6), 7206-7216; https://doi.org/10.3390/molecules17067206 - 12 Jun 2012

Cited by 48 | Viewed by 7407

Abstract

Angiogenesis is one of the crucial steps in the transition of a tumor from a small, harmless cluster of mutated cells to a large, malignant growth, capable of spreading to other organs throughout the body. Vascular endothelial growth factor (VEGF) that stimulates vasculogenesis [...] Read more.

Angiogenesis is one of the crucial steps in the transition of a tumor from a small, harmless cluster of mutated cells to a large, malignant growth, capable of spreading to other organs throughout the body. Vascular endothelial growth factor (VEGF) that stimulates vasculogenesis and angiogenesis is thought to be as an anti-angiogenic target for cancer therapy. Liquiritigenin (LQ), a flavanone existing in Radix glycyrrhiza, shows extensive biological activities, such as anti-inflammatory and anti-cancer properties. In our studies, liquiritigenin effectively inhibited the growth of tumors xenografted in nude mice from human cervical cancer cell line HeLa cells, and microvascular density (MVD) of the tumor exposed to liquiritigenin was reduced in a dose dependent manner, especially in the high dose group. Moreover, the expression and secretion of VEGF were down-regulated by the drug in vivo and in vitro. Therefore, liquiritigenin can be further studied on cancer and other diseases associated with VEGF up-regulation. Full article

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Open AccessArticle

Ginsenoside Rb1 Attenuates Intestinal Ischemia Reperfusion Induced Renal Injury by Activating Nrf2/ARE Pathway

by Qian Sun, Qing-Tao Meng, Ying Jiang and Zhong-Yuan Xia

Molecules 2012, 17(6), 7195-7205; https://doi.org/10.3390/molecules17067195 - 12 Jun 2012

Cited by 51 | Viewed by 7486

Abstract

Intestinal ischemia reperfusion (IIR) is a serious clinical condition associated with simultaneous multiple organ dysfunction. The aim of this study was to investigate the effects of ginsenoside Rb1 on IIR induced renal injury in mice. An intestinal ischemia reperfusion mouse model was established [...] Read more.

Intestinal ischemia reperfusion (IIR) is a serious clinical condition associated with simultaneous multiple organ dysfunction. The aim of this study was to investigate the effects of ginsenoside Rb1 on IIR induced renal injury in mice. An intestinal ischemia reperfusion mouse model was established by superior mesenteric artery (SMA) occlusion for 45 min, followed by reperfusion for 2 h. IIR induced renal injury characterized by increase of BUN, Cr and NGAL in serum, MDA levels and decrease of SOD levels in the renal tissues. Ginsenoside Rb1 (30, 60 mg/kg) given intraperitoneally before reperfusion attennuated renal injury, which was associated with decrease of BUN, Cr and NGAL in serum, MDA levels and increase of SOD levels in the renal tissues. Furthermore, the immunohistochemistry and Western blot data showed that ginsenoside Rb1 dramatically reversed IIR induced renal injury, associated with upregulated nuclear factor erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) in renal tissues. Our data suggests that ginsenoside Rb1 attenuates acute renal injury induced by intestinal ischemia reperfusion by activating the Nrf2/ARE pathway. Full article

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294 KiB

Open AccessArticle

Comparison of the Chemical Composition and Pharmacological Effects of the Aqueous and Ethanolic Extracts from a Tibetan “Snow Lotus” (Saussurea laniceps) Herb

by Tao Yi, Hongwing Lo, Zhongzhen Zhao, Zhiling Yu, Zhijun Yang and Hubiao Chen

Molecules 2012, 17(6), 7183-7194; https://doi.org/10.3390/molecules17067183 - 12 Jun 2012

Cited by 35 | Viewed by 5814

Abstract

To understand the impacts of different processing methods on the composition and effects of the herb Saussurea laniceps (SL), the present study report the first comparison of the chemical constituents of aqueous and ethanolic SL extracts using chromatographic analysis, and to compare their [...] Read more.

To understand the impacts of different processing methods on the composition and effects of the herb Saussurea laniceps (SL), the present study report the first comparison of the chemical constituents of aqueous and ethanolic SL extracts using chromatographic analysis, and to compare their pharmacological effects in a mouse anti-inflammatory, anti-nociceptive model and an in vitro anti-oxidant test. Chemical comparison demonstrated that the types of chemicals in the two extracts were identical, but the contents of the main constituents in the aqueous extract were lower than those of the ethanolic extract. A transesterification of dicaffeoylquinic acids took place in the aqueous extract during boiling. As for pharmacological effects, oral administration of aqueous and ethanolic SL extracts significantly inhibited croton oil-induced mice ear edema, and significantly inhibited acetic acid-induced mice writhings, respectively. In the DPPH anti-oxidant activity test, the IC₅₀ values were calculated as 409.6 mg/L and 523.4 mg/L for the ethanolic and aqueous extracts, respectively. The inhibitory effects of the ethanolic extract were more potent than those of the aqueous extract in all pharmacological tests, although there was no significant difference. This study suggests that the two preparations should be distinguished when used. Full article

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Molecules, Volume 17, Issue 6 (June 2012) – 97 articles , Pages 6179-7611

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