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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (15 August 2023) | Viewed by 36076

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Special Issue Editors

Dr. Anna Choromańska

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Department of Molecular and Cellular Biology, Wroclaw Medical University, Wrocław, Poland
Interests: extracellular vesicles; electroporation; anti-cancer medicinal plants; cell migration
Special Issues, Collections and Topics in MDPI journals

Dr. Nina Rembiałkowska

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Guest Editor

Department of Molecular and Cellular Biology, Wroclaw Medical University, Wrocław, Poland
Interests: membrane permeabilization; electroporation; pulsed electric field; irreversible electroporation; electrochemotherapy; drug delivery; drug resistance; anti-cancer drug delivery; cancer biology; in vitro cell culture; tumor cell culture; cell viability; cytotoxicity; in vivo electroporation; natural chemotherapeutics; apoptosis; cell death; immunofluorescence; biomedical engineering
Special Issues, Collections and Topics in MDPI journals

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Dear Colleagues,

Over the last few years, many innovative therapeutic strategies that combine nanotechnology, bioengineering, and molecular biology have been developed, but their effectiveness is minimal due to cancer cells' secondary and primary resistance. The search for new drugs is still a priority for cancer therapies. There is a growing interest in medicinal plants and compounds isolated from them with various biological activities. As biopharmaceuticals are produced by living cells, their structure is much more complex and diverse than synthetic drugs, which are products of chemical syntheses. This complicated structure largely depends on the spatial conformation assumed by the compound. These can be secondary, tertiary, and quaternary structures. Therefore, the final form of natural drugs is challenging to replicate at the atomic level. There are also apparent differences in the mechanism of action of natural and synthetic drugs. Chemical drugs usually affect only a few processes in the body, while biological drugs, being in their final form a mixture of different conformational isomers, exhibit a more complex, multidirectional mechanism of action.

Plants are considered factories of biologically active compounds not only for the production of primary metabolites but also for secondary ones. They are usually compounded with a complex structure and synthesized with a meager yield, depending on the physiology and development stage of the plant. Among such substances, we can distinguish phenolic compounds (e.g., flavonoids), terpenoids, and nitrogen compounds (e.g., alkaloids, glycosides), with significant therapeutic potential in the course of related reactions degenerative processes, treatment of metabolic, inflammatory, or neurological diseases.

The purpose of this Special Issue of Molecules is to collect interesting information for the scientific community that deals with the bioactivity of plant extracts and natural compounds. The focus will be on research articles and reviews, including reports of anticancer, antioxidative, anti-inflammatory, and anti-infectious, characteristics, as well as studies assessing the influence of natural compounds on age-related disorders and metabolic syndrome.

Dr. Anna Choromańska
Dr. Nina Rembiałkowska
Guest Editors

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Keywords

natural compounds
plant extract
anticancer activity
antimicrobial activity
antifungal activity
antiviral activity
anti-inflammatory activity
synergistic effect
chronic disorders
age-related disorders
metabolic syndrome

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Natural Compounds in Modern Therapies, 2nd Edition in Molecules (3 articles)

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16 pages, 4695 KiB

Open AccessArticle

Trans-(±)-TTPG-B Attenuates Cell Cycle Progression and Inhibits Cell Proliferation on Cholangiocarcinoma Cells

by Thidarath Rattanaburee, Chompunud Chompunud Na Ayudhya, Tienthong Thongpanchang, Varomyalin Tipmanee and Potchanapond Graidist

Molecules 2023, 28(21), 7342; https://doi.org/10.3390/molecules28217342 - 30 Oct 2023

Cited by 1 | Viewed by 1423

Abstract

This research aimed to determine the target protein and molecular mechanism of trans-(±)-kusunokinin (KU) derivatives ((±)-arctigenin (ARC) and trans-(±)-TTPG-B). Molecular docking was used to predict potential synthesized (±)-KU targets among 22 proteins. The (+)-TTPG-B bound HSP90α better than EC44, native (±)-KU and trans-(±)-ARC. In contrast, (−)-ARC bound PI3K more strongly than any other test compound. CSF1R and AKR1B1 were not supposed to be the target of (±)-TTPG-B and (±)-ARC, unlike native (±)-KU. The (+)-TTPG-B bound Tyr139 and Trp162 of HSP90α. Moreover, (−)-ARC bound PI3K via hydrogen bonds and π-π stacking at distinct amino acids, which was different from the other tested compounds. Using half of the IC₅₀ concentration, (±)-TTPG-B, (±)-KU and (±)-ARC enhanced cell cycle arrest at the G0/G1 phase after 12 h and 24 h on KKU-M213 (CCA) cells. The (±)-TTPG-B showed a stronger inhibitory effect than (±)-ARC and (±)-KU on HSP90α, PI3K, HSP90β, c-Myc, AKT, MEK1, CyclinB1, CyclinD1, and CDK1 for 24 and 48 h after treatment with the same concentration (0.015 µM). Thus, trans-(±)-TTPG-B, a newly synthesized compound, has pharmacological potential for development as a target therapy for CCA treatment. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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14 pages, 2048 KiB

Open AccessArticle

Cytotoxic and Antitumor Effects of the Hydroalcoholic Extract of Tagetes erecta in Lung Cancer Cells

by Alma Sarahi Cuellar González, Marisol Galván Valencia, Rodolfo Daniel Cervantes-Villagrana, Alondra Bocanegra Zapata and Alberto Rafael Cervantes-Villagrana

Molecules 2023, 28(20), 7055; https://doi.org/10.3390/molecules28207055 - 12 Oct 2023

Cited by 5 | Viewed by 3114

Abstract

Among all cancers, lung cancer is the one with the highest mortality rate, and it also has limited therapeutics. Antitumor agents based on medicinal plants have gained importance as a source of bioactive substances. Tagetes erecta is a plant of great cultural value, and recent reports have suggested its cytotoxic effects in tumor cells. Our objective was to evaluate the antitumor activity of Tagetes erecta extract in a lung carcinoma model. Hydroalcoholic extracts were obtained from fresh flowers and leaves of T. erecta; both extracts did not exert toxicity on Artemia salina. We observed cytotoxic effects induced by the floral extract in Lewis lung carcinoma (LLC) and breast tumor cell line (MCF7), but not by the leaf extract. In vivo, a xenograft lung carcinoma model was performed with LLC cells implanted on C57BL/6 mice, which showed that the floral extract reduced tumor growth and improved the effect of etoposide. Microscopic analysis of tumors showed a reduction in mitoses and an increase in necrotic areas with the extract and the etoposide. The main phytochemical compounds found are 2,3-dihydro-benzofuran, octadecanoic acid, benzenacetic acid, oleic acid, linoleic acid, and acetic acid. We conclude that the hydroalcoholic extract of T. erecta flowers has cytotoxic effects in lung carcinoma cells and enhances the effect of etoposide. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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16 pages, 3953 KiB

Open AccessArticle

Oral Glucose Tolerance Test (OGTT) Evidence for the Postprandial Anti-Hyperglycemic Property of Salacca zalacca (Gaertn.) Voss Seed Extract

by Vilasinee Hirunpanich Sato, Savita Chewchinda, Arman Syah Goli, Hitoshi Sato, Jannarin Nontakham and Boonyadist Vongsak

Molecules 2023, 28(19), 6775; https://doi.org/10.3390/molecules28196775 - 23 Sep 2023

Cited by 1 | Viewed by 2105

Abstract

Salak seed extract (Salacca zalacca) is known for its high antioxidant content and low caffeine levels, making it a promising candidate for the development of value-added health products. However, there is a lack of scientific evidence for its anti-hyperglycemic effects. To address this, we investigated the in vitro and in vivo anti-hyperglycemic and antioxidant effects of salak seed extract. The HPLC chromatogram of salak seed extract shows a prominent peak that corresponds to chlorogenic acid. In vitro studies revealed that salak seeds inhibited α-glucosidase activity and glucose uptake in Caco-2 cells in a concentration-dependent manner, while also exhibiting antioxidant properties. The extract exhibits a non-competitive inhibition on α-glucosidase activity, with an IC₅₀ and K_i of 16.28 ± 7.22 and 24.81 μg/mL, respectively. In vivo studies utilizing streptozotocin-nicotinamide-induced diabetic mice showed that the extract significantly reduced fasting blood glucose (FBG) levels in the oral glucose tolerance test. Continuous administration of the salak seed extract resulted in lower FBG levels by 13.8% as compared with untreated diabetic mice, although this change was not statistically significant. The estimated LD₅₀ value of salak seed extract exceeds 2000 mg/kg, and no toxicity symptoms have been detected. Our research supports that salak seed extract has the potential to serve as a functional food or supplement that may be beneficial in reducing postprandial hyperglycemia among people with type 2 diabetes. This effect was explained by the salak’s inhibitory mechanisms of glucose absorption due to inhibition of both α-glucosidase activity and intestinal glucose uptake, coupled with its antioxidant effects. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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18 pages, 3094 KiB

Open AccessArticle

Development and Characterization of a Hydrogel Containing Curcumin-Loaded Nanoemulsion for Enhanced In Vitro Antibacteria and In Vivo Wound Healing

by Thi Thanh Ngoc Le, Thi Kieu Nhi Nguyen, Van Minh Nguyen, Thi Cam Minh Dao, Hoai Bao Chau Nguyen, Cong Thuan Dang, Thi Bao Chi Le, Thi Khanh Linh Nguyen, Phuong Thao Tien Nguyen, Le Hoang Nam Dang, Van Minh Doan and Hoang Nhan Ho

Molecules 2023, 28(17), 6433; https://doi.org/10.3390/molecules28176433 - 4 Sep 2023

Cited by 10 | Viewed by 2853

Abstract

Curcumin (CUR) is a natural compound extracted from turmeric (Curcuma longa L.) used to cure acne, wound healing, etc. Its disadvantages, such as poor solubility and permeability, limit its efficacy. Nanoemulsion (NE)-based drug delivery systems have gained popularity due to their advantages. This study aimed to optimize a CUR-NE-based gel and evaluate its physicochemical and biological properties. A NE was prepared using the catastrophic phase inversion method and optimized using the Design Expert 12.0 software. The CUR-NE gel was characterized in terms of visual appearance, pH, drug release, antibacterial and wound healing effects. The optimal formulation contained CUR, Capryol 90 (oil), Labrasol:Cremophor RH40 (1:1) (surfactants), propylene glycol (co-surfactant), and water. The NE had a droplet size of 22.87 nm and a polydispersity index of 0.348. The obtained CUR-NE gel had a soft, smooth texture and a pH of 5.34 ± 0.05. The in vitro release of CUR from the NE-based gel was higher than that from a commercial gel with nanosized CUR (21.68 ± 1.25 µg/cm², 13.62 ± 1.63 µg/cm² after 10 h, respectively). The CUR-NE gel accelerated in vitro antibacterial and in vivo wound healing activities as compared to other CUR-loaded gels. The CUR-NE gel has potential for transdermal applications. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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21 pages, 4066 KiB

Open AccessArticle

Walnut Kernel Oil and Defatted Extracts Enhance Mesenchymal Stem Cell Stemness and Delay Senescence

by Marwa A. Elsied, Zeina W. Sharawi, Hadba Al-Amrah, Rabab A. Hegazy, Amro E. Mohamed, Rasha M. Saleh, Sanad S. El-kholy, Foad A. Farrag, Masoud H. Fayed and Mohammed A. El-Magd

Molecules 2023, 28(17), 6281; https://doi.org/10.3390/molecules28176281 - 28 Aug 2023

Cited by 4 | Viewed by 1563

Abstract

Decreased stemness and increased cellular senescence impair the ability of mesenchymal stem cells (MSCs) to renew themselves, change into different cell types, and contribute to regenerative medicine. There is an urgent need to discover new compounds that can boost MSCs’ stemness and delay senescence. Therefore, this study aimed to investigate the impact of walnut kernel oil (WKO) and defatted (WKD) extracts on bone marrow (BM)-MSC stemness and senescence. Premature senescence and inflammation were induced in BM-MSCs using H₂O₂ and LPS, respectively. Phytochemical constituents of WKO and WKD extracts were detected by HPLC. The stemness (proliferation and migration), senescence-related markers (p53, p21, SIRT1, and AMPK), oxidative stress/antioxidant markers, inflammatory cytokines, and cell cycle of BM-MSCs were measured by MTT assay, qPCR, ELISA, and flow cytometry. WKO and WKD extracts improved rat BM-MSC stemness, as evidenced by (1) increased cell viability, (2) decreased apoptosis (low levels of Bax and caspase3 and high levels of Bcl2), (3) upregulated MMP9 and downregulated TIMP1 expression, and (4) cell cycle arrest in the G0/G1 phase and declined cell number in the S and G2/M phases. Additionally, WKO and WKD extracts reduced rat BM-MSC senescence, as indicated by (1) decreased p53 and p21 expression, (2) upregulated expression and levels of SIRT1 and AMPK, (3) reduced levels of ROS and improved antioxidant activity (higher activity of CAT, SOD, and GPx and upregulated expression of NrF2 and HO-1), and (4) declined levels of TNFα, IL1β, and NF-κB. When compared to the WKO extract, the WKD extract had a greater impact on the induction of stemness and reduction of senescence of BM-MSCs due to its stronger antioxidant activity, which could be attributed to its higher levels of flavonoids and phenolic compounds, as detected by HPLC analysis. WKO and WKD extracts enhance rat BM-MSC stemness and protect them from senescence, suggesting their potential use as enhancers to increase MSCs’ therapeutic efficacy. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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14 pages, 4520 KiB

Open AccessArticle

Functional Axis of PDE5/cGMP Mediates Timosaponin-AIII-Elicited Growth Suppression of Glioblastoma U87MG Cells

by Ya-Fang Liao, Hui-Jun Pan, Nuerziba Abudurezeke, Chun-Lu Yuan, Yan-Li Yuan, Shu-Da Zhao, Dan-Dan Zhang and Shuang Huang

Molecules 2023, 28(9), 3795; https://doi.org/10.3390/molecules28093795 - 28 Apr 2023

Cited by 3 | Viewed by 2079

Abstract

Glioblastoma (GBM) is the most aggressive brain tumor, with high mortality. Timosaponin AIII (TIA), a steroidal saponin isolated from the medicinal plant Anemarrhena asphodeloides Bge., has been shown to possess anticancer properties in various cancer types. However, the effect of TIA on GBM is unknown. In this study, we reveal that TIA not only inhibited U87MG in vitro cell growth but also in vivo tumor development. Moreover, we found that the cause of TIA-induced cell growth suppression was apoptosis. When seeking to uncover antitumor mechanisms of TIA, we found that TIA diminished the expression of cGMP-specific phosphodiesterase 5(PDE5) while elevating the levels of guanylate cyclases (sGCβ), cellular cGMP, and phosphorylation of VASP^ser239. Following the knockdown of PDE5, PDE5 inhibitor tadalafil and cGMP analog 8-Bro-cGMP both inhibited cell growth and inactivated β-catenin; we reason that TIA elicited an antitumor effect by suppressing PDE5, leading to the activation of the cGMP signaling pathway, which, in turn, impeded β-catenin expression. As β-catenin is key for cell growth and survival in GBM, this study suggests that TIA elicits its anti-tumorigenic effect by interfering with β-catenin function through the activation of a PDE5/cGMP functional axis. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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11 pages, 2439 KiB

Open AccessArticle

Stilbenoids and Flavonoids from Cajanus cajan (L.) Millsp. and Their α-Glucosidase Inhibitory Activities

by Yaxian Zhao, Xinman Zhao, Mengjia Guo, Krishnapriya M. Varier, Babu Gajendran, Shaohuan Liu, Ling Tao, Xiangchun Shen and Nenling Zhang

Molecules 2023, 28(9), 3779; https://doi.org/10.3390/molecules28093779 - 27 Apr 2023

Cited by 4 | Viewed by 1825

Abstract

Two new stilbenoids, cajanstilbenoid C (1) and cajanstilbenoid D (2), together with eight other known stilbenoids (3-10) and seventeen known flavonoids (11-27), were isolated from the petroleum ether and ethyl acetate portions of the 95% ethanol extract of leaves of Cajanus cajan (L.) Millsp. The planar structures of the new compounds were elucidated by NMR and high-resolution mass spectrometry, and their absolute configurations were determined by comparison of their experimental and calculated electronic circular dichroism (ECD) values. All the compounds were assayed for their inhibitory activities against yeast α-glucosidase. The results demonstrated that compounds 3, 8-9, 11, 13, 19-21, and 24-26 had strong inhibitory activities against α-glucosidase, with compound 11 (IC₅₀ = 0.87 ± 0.05 μM) exhibiting the strongest activity. The structure–activity relationships were preliminarily summarized. Moreover, enzyme kinetics showed that compound 8 was a noncompetitive inhibitor, compounds 11, 24-26 were anticompetitive, and compounds 9 and 13 were mixed-competitive. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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18 pages, 4918 KiB

Open AccessArticle

Molecular Docking and Simulation-Binding Analysis of Plant Phytochemicals with the Hepatocellular Carcinoma Targets Epidermal Growth Factor Receptor and Caspase-9

by Ghulam Mustafa, Shumaila Younas, Hafiza Salaha Mahrosh, Mohammed Fahad Albeshr and Eijaz Ahmed Bhat

Molecules 2023, 28(8), 3583; https://doi.org/10.3390/molecules28083583 - 20 Apr 2023

Cited by 10 | Viewed by 4337

Abstract

Among primary liver cancers, hepatocellular carcinoma (HCC) is one of the most common forms and it has been categorized as the joint-fourth largest reason of cancer-related deaths globally. Different factors such as alcohol abuse, hepatitis B and C, viral infections, and fatty liver diseases are mainly related to the pathogenesis of HCC. In the current study, 1000 total various plant phytochemicals were docked to proteins involved in HCC. The compounds were docked to the active site amino acids of epidermal growth factor receptor and caspase-9 as receptor proteins in order to explore their inhibiting potential. The top five compounds against each receptor protein were explored as potential drug candidates on the basis of their binding affinity and root-mean square deviation values. The top two compounds against each protein were found to be liquoric acid (S-score −9.8 kcal/mol) and madecassic acid (S-score −9.3 kcal/mol) against EGFR, and limonin (S-score −10.5 kcal/mol) and obamegine (S-score −9.3 kcal/mol) against the caspase-9 protein. The selected phytochemicals were further assessed through drug scanning using Lipinski’s rule of five to explore their molecular properties and druggability. According to the ADMET analysis, the selected phytochemicals were found to be non-toxic and non-carcinogenic. Finally, the molecular dynamics simulation study revealed that liquoric acid and limonin were stabilized within the binding pockets of EGFR and capase-9, respectively, and stayed firmly bound throughout the simulation. In light of the current findings, the phytochemicals reported in this study, especially liquoric acid and limonin, could be used as potential drugs for the treatment of HCC in the future. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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17 pages, 5560 KiB

Open AccessArticle

Identification of Plant Peptides as Novel Inhibitors of Orthohepevirus A (HEV) Capsid Protein by Virtual Screening

by Ghulam Mustafa, Hafiza Salaha Mahrosh, Syed Awais Attique, Rawaba Arif, Mohammad Abul Farah, Khalid Mashay Al-Anazi and Sajad Ali

Molecules 2023, 28(6), 2675; https://doi.org/10.3390/molecules28062675 - 16 Mar 2023

Cited by 4 | Viewed by 2041

Abstract

Hepatitis E virus (HEV) is the notable causative agent of acute and chronic hepatic, renal, pancreatic, neurological, and hematopoietic blood cell infections with high risk in immunocompromised patients. Hepatic failure is mostly documented among adults, pregnant women, and patients with preexisting liver disease. HEV is a positive sense RNA virus of 7.2 kb genome size with typically three open reading frames (ORFs) which play essential roles in viral replication, genome assembly, and transcription. The mutational substitution in the viral RNA genome makes more it difficult to understand the actual relationship in the host–virus association. ORFs of HEV encode different structural and non-structural proteins and one of them is the capsid protein which is coded by ORF2. The capsid protein mediates the encapsulation of the viral genome as well as being involved in virion assembly. In the current study, the ligand-based docking approach was employed to inhibit the active amino acids of the viral capsid protein. Depending upon S-score, ADMET profiling, and drug scanning, the top ten tetrapeptides were selected as potential drug candidates with no toxicity counter to HEV receptor protein. The S-score or docking score is a mathematical function which predicts the binding affinities of docked complexes. The binding affinity of the predicted drug–target complexes helps in the selectivity of the desired compound as a potential drug. The best two selected peptides (i.e., TDGH with S-score of −8.5 and EGDE with S-score of −8.0) interacted with the active site amino acids of the capsid protein (i.e., Arg399, Gln420, and Asp444). The molecular dynamics simulations of RMSD trajectories of TDGH–capsid protein and EDGE–capsid protein have revealed that both docked complexes were structurally stable. The study revealed that these tetrapeptides would serve as strong potential inhibitors and a starting point for the development of new drug molecules against the HEV capsid protein. In future, in vivo studies are needed to explore selected peptides as potential drug candidates. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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17 pages, 5541 KiB

Open AccessArticle

Investigating In Situ Expression of c-MYC and Candidate Ubiquitin-Specific Proteases in DLBCL and Assessment for Peptidyl Disruptor Molecule against c-MYC-USP37 Complex

by Durr e Sameen Kamran, Mushtaq Hussain and Talat Mirza

Molecules 2023, 28(6), 2441; https://doi.org/10.3390/molecules28062441 - 7 Mar 2023

Cited by 2 | Viewed by 2013

Abstract

Diffuse Large B-Cell Lymphoma (DLBCL) is the most common form of non-Hodgkin’s lymphoma (NHL). Elevated expression of c-MYC in DLBCL is associated with poor prognosis of the disease. In different cancers, c-MYC has been found regulated by different ubiquitin-specific proteases (USPs), but to date, the role of USPs in c-MYC regulation has not been investigated in DLBCL. In this study, in situ co expression of c-MYC and three candidates USPs, USP28, USP36 and USP37, have been investigated in both the ABC and GCB subtypes of DLBCL. This shows that USP37 expression is positively correlated with the c-MYC expression in the ABC subtype of DLBCL. Structurally, both c-MYC and USP37 has shown large proportion of intrinsically disordered regions, minimizing their chances for full structure crystallization. Peptide array and docking simulations has shown that N-terminal region of c-MYC interacts directly with residues within and in proximity of catalytically active C19 domain of the USP37. Given the structural properties of the interaction sites in the c-MYC-USP37 complex, a peptidyl inhibitor has been designed. Molecular docking has shown that the peptide fits well in the targeted site of c-MYC, masking most of its residues involved in the binding with USP37. The findings could further be exploited to develop therapeutic interventions against the ABC subtype of DLBCL. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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14 pages, 2359 KiB

Open AccessArticle

Effect of Isoquercitrin on Free Fatty Acid-Induced Lipid Accumulation in HepG2 Cells

by Sou Hyun Kim, Chawon Yun, Doyoung Kwon, Yun-Hee Lee, Jae-Hwan Kwak and Young-Suk Jung

Molecules 2023, 28(3), 1476; https://doi.org/10.3390/molecules28031476 - 3 Feb 2023

Cited by 13 | Viewed by 3806

Abstract

Liver metabolic disorders and oxidative stress are crucial factors in the development of nonalcoholic fatty liver disease (NAFLD); however, treatment strategies to combat NAFLD remain poorly established, presenting an important challenge that needs to be addressed. Herein, we aimed to examine the effect of isoquercitrin on lipid accumulation induced by exogenous free fatty acids (FFA) using HepG2 cells and elucidate the underlying molecular mechanism. The cells were exposed to 0.5 mM FFA to induce intracellular lipid accumulation, followed by co-treatment with isoquercitrin to confirm the potential inhibitory effect on FFA-induced lipid production. HepG2 cells exposed to FFA alone exhibited intracellular lipid accumulation, compromised endoplasmic reticulum (ER) stress, and enhanced expression of proteins and genes involved in lipid synthesis; however, co-treatment with isoquercitrin decreased the expression of these molecules in a dose-dependent manner. Furthermore, isoquercitrin could activate AMP-activated protein kinase (AMPK), a key regulatory protein of hepatic fatty acid oxidation, suppressing new lipid production by phosphorylating acetyl-CoA carboxylase (ACC) and inhibiting sterol regulatory element-binding transcription factor 1 (SREBP-1)/fatty acid synthase (FAS) signals. Overall, these findings suggest that isoquercitrin can be employed as a therapeutic agent to improve NAFLD via the regulation of lipid metabolism by targeting the AMPK/ACC and SREBP1/FAS pathways. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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15 pages, 4219 KiB

Open AccessArticle

Phytoconstituents Assisted Biofabrication of Copper Oxide Nanoparticles and Their Antiplasmodial, and Antilarval Efficacy: A Novel Approach for the Control of Parasites

by Chidambaram Jayaseelan, Ahmed Abdulhaq, Chinnasamy Ragavendran and Syam Mohan

Molecules 2022, 27(23), 8269; https://doi.org/10.3390/molecules27238269 - 27 Nov 2022

Cited by 5 | Viewed by 1806

Abstract

The present work aimed to biofabricate copper oxide nanoparticles (CuO NPs) using Tinospora cordifolia leaf extract. The biofabricated CuO NPs were treated against the malarial parasite of chloroquine-resistant Plasmodium falciparum (INDO) and the antilarval efficacy was evaluated against the malaria vector Anopheles stephensi and dengue vector Aedes aegypti. The prominence at 285 nm in the UV–visible spectrum helped to identify the produced CuO NPs. Based on the XRD patterns, the concentric rings correspond to reflections at 38.26° (111), 44.11° (200), 64.58° (220), and 77.34° (311). These separations are indicative of CuO’s face-centered cubic (fcc) structure. The synthesized CuO NPs have FTIR spectra with band intensities of 3427, 2925, 1629, 1387, 1096, and 600 cm⁻¹. The absorbance band at 3427 cm⁻¹ is known to be associated with the stretching O-H due to the alcoholic group. FTIR proved that the presence of the -OH group is responsible for reducing and capping agents in the synthesis of nanoparticles (NPs). The synthesized CuO NPs were found to be polymorphic (oval, elongated, and roughly spherical) in form with a size range of 11–47 nm and an average size of 16 nm when the morphology was examined using FESEM and HRTEM. The highest antiplasmodial efficacy against the chloroquine-resistant strain of P. falciparum (INDO) was found in the synthesized CuO NPs, with LC₅₀ values of 19.82 µg/mL, whilst HEK293 cells are the least toxic, with a CC₅₀ value of 265.85 µg/mL, leading to a selectivity index of 13.41. However, the antiplasmodial activity of T. cordifolia leaf extract (TCLE) and copper sulfate (CS) solution showed moderate activity, with LC₅₀ values of 52.24 and 63.88 µg/mL, respectively. The green synthesized NPs demonstrated extremely high antilarval efficacy against the larvae of An. stephensi and Ae. aegypti, with LC₅₀ values of 4.06 and 3.69 mg/L, respectively. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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12 pages, 1198 KiB

Open AccessArticle

Anticancer Efficacy of 6-Gingerol with Paclitaxel against Wild Type of Human Breast Adenocarcinoma

by Kamila Wala, Wojciech Szlasa, Natalia Sauer, Paulina Kasperkiewicz-Wasilewska, Anna Szewczyk, Jolanta Saczko, Nina Rembiałkowska, Julita Kulbacka and Dagmara Baczyńska

Molecules 2022, 27(9), 2693; https://doi.org/10.3390/molecules27092693 - 22 Apr 2022

Cited by 9 | Viewed by 2888

Abstract

Breast cancer is one of the most common malignant neoplasms, and despite the dynamic development of anticancer therapies, 5-year survival in the metastatic stage is still less than 30%. 6-Gingerol (1-[4′-hydroxy-3′-methoxyphenyl]-5-hydroxy-3-decanone) is a substance contained in ginger, which exhibits anti-cancer properties. Paclitaxel is a cytostatic substance used to treat breast cancer, but its therapeutically effective dose has many adverse effects. The aim of the presented study was to assess the anticancer effect of 6-gingerol and the possibility of increasing the effectiveness of Paclitaxel in the death induction of wild type human breast cancer cells. MCF-7/WT cells were treated with drugs—6-gingerol and paclitaxel at selected concentrations. The mitochondrial activity assay, caspase 7 activity assay, ATP assay, microscopy studies, and RT-PCR assays were performed to evaluate the antitumor activity and mechanism of action of both compounds, alone and in combination. After 72 h of incubation, the mitochondrial activity showed that the combination of 5 nM Paclitaxel with 10 µM 6-Gingerol led to the same decrease in viability as the use of 20 nM Paclitaxel alone; 10 µM 6-Gingerol led to an enhancement of caspase 7 activity, with the highest activity observed after 24 h of incubation. A real-time PCR study showed that 6-Gingerol induces the simultaneous transcription of Bax with TP53 genes in large excess to BCL-2. In contrast, 5 nM Paclitaxel induces TP53 transcription in excess of BCL-2 and Bax. Our results suggest that 6-Gingerol may act as a cell death-inducing agent in cancer cells and, in combination with paclitaxel, and increase the effectiveness of conventional chemotherapy. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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Suppression of Inflamm-Aging by Moringa oleifera and Zingiber officinale Roscoe in the Prevention of Degenerative Diseases: A Review of Current Evidence

by Nur Fatin Nabilah Mohd Sahardi and Suzana Makpol

Molecules 2023, 28(15), 5867; https://doi.org/10.3390/molecules28155867 - 3 Aug 2023

Cited by 1 | Viewed by 2544

Abstract

Inflammation or inflamm-aging is a chronic low-grade inflammation that contributes to numerous types of degenerative diseases among the elderly and might be impeded by introducing an anti-inflammatory agent like Moringa oleifera Lam (moringa) and Zingiber officinale Roscoe (ginger). Therefore, this paper aims to review the role of moringa and ginger in suppressing inflamm-aging to prevent degenerative diseases. Various peer-reviewed publications were searched and downloaded using the reputed search engine “Pubmed” and “Google Scholar”. These materials were reviewed and tabulated. A comparison between these previous findings was made based on the mechanism of action of moringa and ginger against degenerative diseases, focusing on their anti-inflammatory properties. Many studies have reported the efficacy of moringa and ginger in type 2 diabetes mellitus, neurodegenerative disease, cardiovascular disease, cancer, and kidney disease by reducing inflammatory cytokines activities, mainly of TNF-α and IL-6. They also enhanced the activity of antioxidant enzymes, including catalase, glutathione, and superoxide dismutase. The anti-inflammatory activities can be seen by inhibiting NF-κβ activity. Thus, the anti-inflammatory potential of moringa and ginger in various types of degenerative diseases due to inflamm-aging has been shown in many recent types of research. Full article

(This article belongs to the Special Issue Natural Compounds in Modern Therapies)

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