Life | Special Issue : Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health

Research

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21 pages, 2647 KiB

Open AccessArticle

Hogweed Seed Oil: Physico–Chemical Characterization, LC-MS Profile, and Neuroprotective Activity of Heracleum dissectum Nanosuspension

by Daniil N. Olennikov and Nadezhda K. Chirikova

Life 2023, 13(5), 1112; https://doi.org/10.3390/life13051112 - 29 Apr 2023

Cited by 3 | Viewed by 2141

Abstract

The seeds of dissected hogweed (Heracleum dissectum Ledeb., Apiaceae) are the source of hogweed oil (HSO), which is still underexplored and requires careful chemical and biological studies. The performed physico–chemical analysis of HSO elucidated basic physical characteristics and revealed the presence of [...] Read more.

The seeds of dissected hogweed (Heracleum dissectum Ledeb., Apiaceae) are the source of hogweed oil (HSO), which is still underexplored and requires careful chemical and biological studies. The performed physico–chemical analysis of HSO elucidated basic physical characteristics and revealed the presence of fatty acids, essential oil components, pigments, and coumarins. High-performance liquid chromatography with photodiode array detection and electrospray ionization triple quadrupole mass spectrometric detection (HPLC–PDA–ESI–tQ–MS/MS) identified 38 coumarins that were characterized and quantified. Various furanocoumarins were the major components of HSO polyphenolics, including imperatorin, phellopterin, and isoimperatorin, and the total coumarin content in HSO varied from 181.14 to 238.42 mg/mL. The analysis of storage stability of the selected compounds in HSO indicated their good preservation after 3-year storage at cold and freezing temperatures. The application of the CO₂-assisted effervescence method allowed the production of an HSO nanosuspension, which was used in a brain ischemia model of rats. The HSO nanosuspension enhanced cerebral hemodynamics and decreased the frequency of necrotic processes in the brain tissue. Thus, H. dissectum seeds are a good source of coumarins, and HSO nanosuspension promotes neuroprotection of the brain after lesions, which supports earlier ethnopharmacological data. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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24 pages, 1583 KiB

Open AccessArticle

Thymus musilii Velen. Methanolic Extract: In Vitro and In Silico Screening of Its Antimicrobial, Antioxidant, Anti-Quorum Sensing, Antibiofilm, and Anticancer Activities

by Emira Noumi, Iqrar Ahmad, Nouha Bouali, Harun Patel, Siwar Ghannay, Ayshah Aysh ALrashidi, Mohammad A. Abdulhakeem, Mitesh Patel, Ozgur Ceylan, Riadh Badraoui, Afnan Elayyan Mousa Elayyan, Mohd Adnan, Adel Kadri and Mejdi Snoussi

Life 2023, 13(1), 62; https://doi.org/10.3390/life13010062 - 25 Dec 2022

Cited by 19 | Viewed by 2813

Abstract

Thymus musilii Velen. is a rare plant species cultivated in the Ha’il region (Saudi Arabia) under greenhouse conditions. In this work, we described, for the first time, the phytochemical composition, antimicrobial, antioxidant, anti-quorum sensing, and anticancer activities of T. musilii methanolic extract using [...] Read more.

Thymus musilii Velen. is a rare plant species cultivated in the Ha’il region (Saudi Arabia) under greenhouse conditions. In this work, we described, for the first time, the phytochemical composition, antimicrobial, antioxidant, anti-quorum sensing, and anticancer activities of T. musilii methanolic extract using both experimental and computational approaches. The obtained results showed the identification of eight small-like peptides and eighteen phyto-compounds by using high-resolution liquid chromatography–mass spectrometry (HR-LCMS) dominated mainly by compounds belonging to isoprenoid, fatty acyl, flavonoid, and alkaloid classes. The tested extracts exhibited high antifungal and antibacterial activity with the mean diameter of growth inhibition zones ranging from 12.33 ± 0.57 mm (Pseudomonas aeruginosa ATCC 27853) to 29.33 ± 1.15 mm (Candida albicans ATCC 10231). Low minimal inhibitory concentrations were recorded for the tested micro-organisms ranging from 0.781 mg/mL to 12.5 mg/mL. While higher doses were necessary to completely kill all tested bacterial and fungal strains. Thyme extract was able to scavenge DPPH^•, ABTS^•+, β-carotene, and FRAP free radicals, and the IC₅₀ values were 0.077 ± 0.0015 mg/mL, 0.040 ± 0.011 mg/mL, 0.287 ± 0.012 mg/mL, and 0.106 ± 0.007 mg/mL, respectively. The highest percentage of swarming and swimming inhibition was recorded at 100 µg/mL with 39.73 ± 1.5% and 25.18 ± 1%, respectively. The highest percentage of biofilm inhibition was recorded at 10 mg/mL for S. typhimurium ATCC 14028 (53.96 ± 4.21%) and L. monocytogenes ATCC 7644 (49.54 ± 4.5 mg/mL). The in silico docking study revealed that the observed antimicrobial, antioxidant, and anticancer activities of the constituent compounds of T. musilii are thermodynamically feasible, notably, such as those of the tripeptides (Asn-Met-His, His-Cys-Asn, and Phe-His-Gln), isoprenoids (10-Hydroxyloganin), and diterpene glycosides (4-Ketoretinoic acid glucuronide). Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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16 pages, 2622 KiB

Open AccessArticle

Green Synthesis and Characterization of Silver Nanoparticles Using a Lythrum salicaria Extract and In Vitro Exploration of Their Biological Activities

by Andreia Corciovă, Cornelia Mircea, Ana Flavia Burlec, Adrian Fifere, Ioana Turin Moleavin, Alexandra Sarghi, Cristina Tuchiluș, Bianca Ivănescu and Irina Macovei

Life 2022, 12(10), 1643; https://doi.org/10.3390/life12101643 - 19 Oct 2022

Cited by 13 | Viewed by 3001

Abstract

This research describes an eco-friendly green route for the synthesis of AgNPs using an aqueous extract of Lythrum salicaria. Taguchi design was used to optimize the synthesis method, taking into account various working conditions. The optimum parameters were established using a 3 [...] Read more.

This research describes an eco-friendly green route for the synthesis of AgNPs using an aqueous extract of Lythrum salicaria. Taguchi design was used to optimize the synthesis method, taking into account various working conditions. The optimum parameters were established using a 3 mM AgNO₃ concentration, a 1:9 extract:AgNO₃ volume ratio, a pH value of 8, 60 ℃ temperature, and 180 min reaction time. The synthesized AgNPs were characterized using UV-Vis and FTIR spectroscopy, and TEM and EDX analysis. The SPR band at 410 nm, as well as the functional groups of biomolecules identified by FTIR and the EDX signals at ~3 keV, confirmed the synthesis of spherical AgNPs. The average AgNPs size was determined to be 40 nm, through TEM, and the zeta potential was −19.62 mV. The antimicrobial assay showed inhibition against S. aureus and C. albicans. Moreover, the results regarding the inhibition of lipoxygenase and of peroxyl radical-mediated hemolysis assays were promising and justify further antioxidant studies. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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15 pages, 2862 KiB

Open AccessArticle

Self-Assembled Nanomicellar Formulation of Docetaxel as a Potential Breast Cancer Chemotherapeutic System

by Meshal Alshamrani, Navid J. Ayon, Abdullah Alsalhi and Omowumi Akinjole

Life 2022, 12(4), 485; https://doi.org/10.3390/life12040485 - 27 Mar 2022

Cited by 8 | Viewed by 2836

Abstract

Docetaxel (DTX) is classified as a class IV drug that exhibits poor aqueous solubility (6–7 µg/mL in water) and permeability (P-glycoprotein substrate). The main objective of this study was to construct, characterize, and evaluate docetaxel loaded nanomicellar formulation in vitro for oral delivery [...] Read more.

Docetaxel (DTX) is classified as a class IV drug that exhibits poor aqueous solubility (6–7 µg/mL in water) and permeability (P-glycoprotein substrate). The main objective of this study was to construct, characterize, and evaluate docetaxel loaded nanomicellar formulation in vitro for oral delivery to enhance the absorption and bioavailability of DTX, as well as to circumvent P-gp efflux inhibition. Formulations were prepared with two polymeric surfactants, hydrogenated castor oil-40 (HCO-40) and D-α-Tocopherol polyethylene glycol 1000 succinate (VIT E TPGS) with solvent evaporation technique, and the resulting DTX nanomicellar formulations were characterized by proton nuclear magnetic resonance spectroscopy (1H NMR), Fourier Transform Infrared Spectroscopy (FT–IR), X-ray powder diffraction (XRD), and transmission electron microscopy (TEM). Proton NMR, FT–IR, and XRD data indicated that DTX was completely encapsulated within the hydrophobic core of the nanomicelles in its amorphous state. TEM data revealed a smooth spherical shape of the nanomicellar formulation. The optimized formulation (F-2) possessed a mean diameter of 13.42 nm, a zeta potential of −0.19 mV, with a 99.3% entrapment efficiency. Dilution stability study indicated that nanomicelles were stable up to 100-fold dilution with minimal change in size, poly dispersity index (PDI), and zeta potential. In vitro cytotoxicity study revealed higher anticancer activity of DTX nanomicelles at 5 µM compared to the native drug against breast cancer cell line (MCF-7) cells. The LC–MS data confirmed the chemical stability of DTX within the nanomicelles. In vitro drug release study demonstrated faster dissolution of DTX from the nanomicelles compared to the naked drug. Our experimental results exhibit that nanomicelles could be a drug delivery system of choice to encapsulate drugs with low aqueous solubility and permeability that can preserve the stability of the active constituents to provide anticancer activity. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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Review

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23 pages, 4811 KiB

Open AccessReview

Chitosan-Polyphenol Conjugates for Human Health

by Ananya Pattnaik, Sanghamitra Pati and Sangram Keshari Samal

Life 2022, 12(11), 1768; https://doi.org/10.3390/life12111768 - 2 Nov 2022

Cited by 11 | Viewed by 3096

Abstract

Human health deteriorates due to the generation and accumulation of free radicals that induce oxidative stress, damaging proteins, lipids, and nucleic acids; this has become the leading cause of many deadly diseases such as cardiovascular, cancer, neurodegenerative, diabetes, and inflammation. Naturally occurring polyphenols [...] Read more.

Human health deteriorates due to the generation and accumulation of free radicals that induce oxidative stress, damaging proteins, lipids, and nucleic acids; this has become the leading cause of many deadly diseases such as cardiovascular, cancer, neurodegenerative, diabetes, and inflammation. Naturally occurring polyphenols have tremendous therapeutic potential, but their short biological half-life and rapid metabolism limit their use. Recent advancements in polymer science have provided numerous varieties of natural and synthetic polymers. Chitosan is widely used due to its biomimetic properties which include biodegradability, biocompatibility, inherent antimicrobial activity, and antioxidant properties. However, due to low solubility in water and the non-availability of the H-atom donor, the practical use of chitosan as an antioxidant is limited. Therefore, chitosan has been conjugated with polyphenols to overcome the limitations of both chitosan and polyphenol, along with increasing the potential synergistic effects of their combination for therapeutic applications. Though many methods have been evolved to conjugate chitosan with polyphenol through activated ester-modification, enzyme-mediated, and free radical induced are the most widely used strategies. The therapeutic efficiency of chitosan-polyphenol conjugates has been investigated for various disease treatments caused by ROS that have shown favorable outcomes and tremendous results. Hence, the present review focuses on the recent advancement of different strategies of chitosan-polyphenol conjugate formation with their advantages and limitations. Furthermore, the therapeutic applicability of the combinatorial efficiency of chitosan-based conjugates formed using Gallic Acid, Curcumin, Catechin, and Quercetin in human health has been described in detail. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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19 pages, 515 KiB

Open AccessReview

Dietary Polyphenols as Natural Inhibitors of α-Amylase and α-Glucosidase

by Ina Ćorković, Dajana Gašo-Sokač, Anita Pichler, Josip Šimunović and Mirela Kopjar

Life 2022, 12(11), 1692; https://doi.org/10.3390/life12111692 - 25 Oct 2022

Cited by 57 | Viewed by 6982

Abstract

It is well known that carbohydrates are the main source of calories in most diets. However, by inhibiting carbohydrases, intake of calories is reduced and weight loss is improved. α-amylase is an enzyme that hydrolyses α-1,4 glycosidic linkages of α-linked polysaccharides, resulting in [...] Read more.

It is well known that carbohydrates are the main source of calories in most diets. However, by inhibiting carbohydrases, intake of calories is reduced and weight loss is improved. α-amylase is an enzyme that hydrolyses α-1,4 glycosidic linkages of α-linked polysaccharides, resulting in low-molecular-weight products such as glucose, maltose and maltotriose, while α-glucosidase catalyzes the hydrolysis of nonreducing α-1,4-linked glucose moieties from disaccharides or oligosaccharides. Currently, one of the most common nutritional disorders in the world is hyperglycemia. One of the new therapeutic approaches to treat this disease is the application of natural inhibitors, such as polyphenols, that control starch digestion and regulate blood glucose level. Dietary polyphenols showed potential inhibitory activity against α-amylase and α-glucosidase and this review summarizes the recently published literature that studied inhibition mechanisms and the structure–activity relationship between individual dietary polyphenols and mentioned digestive enzymes. It is known that higher binding interactions cause higher inhibitory activities; thus, different polyphenols can affect different steps in the digestion of polysaccharides. The aim of this review is to clarify these mechanisms and to introduce polyphenol-rich functional foods as potential tools for the inhibition of α-amylase and α-glucosidase. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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19 pages, 4362 KiB

Open AccessReview

Polyphenols and Their Nanoformulations: Protective Effects against Human Diseases

by Santosh Anand, Ramachandregowda Sowbhagya, Mohammad Azam Ansari, Mohammad A. Alzohairy, Mohammad N. Alomary, Asiyah I. Almalik, Wasim Ahmad, Takshashila Tripathi and Abozer Y. Elderdery

Life 2022, 12(10), 1639; https://doi.org/10.3390/life12101639 - 19 Oct 2022

Cited by 25 | Viewed by 3058

Abstract

Polyphenols are the secondary metabolites synthesized by the plants as a part of defense machinery. Owing to their antioxidant, anti-inflammatory, anticancerous, antineoplastic, and immunomodulatory effects, natural polyphenols have been used for a long time to prevent and treat a variety of diseases. As [...] Read more.

Polyphenols are the secondary metabolites synthesized by the plants as a part of defense machinery. Owing to their antioxidant, anti-inflammatory, anticancerous, antineoplastic, and immunomodulatory effects, natural polyphenols have been used for a long time to prevent and treat a variety of diseases. As a result, these phytochemicals may be able to act as therapeutic agents in treating cancer and cardiovascular and neurological disorders. The limited bioavailability of polyphenolic molecules is one issue with their utilization. For the purpose of increasing the bioavailability of these chemicals, many formulation forms have been developed, with nanonization standing out among them. The present review outlines the biological potential of nanoformulated plant polyphenolic compounds. It also summarizes the employability of various polyphenols as nanoformulations for cancer and neurological and cardiovascular disease treatment. Nanoencapsulated polyphenols, singular or in combinations, effective both in vitro and in vivo, need more investigation. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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22 pages, 1945 KiB

Open AccessReview

Prospective Role of Bioactive Molecules and Exosomes in the Therapeutic Potential of Camel Milk against Human Diseases: An Updated Perspective

by Farheen Badrealam Khan, Mohammad Azam Ansari, Shahab Uddin, Abdul Rasheed Palakott, Irfa Anwar, Ahmad Almatroudi, Mohammad N. Alomary, Faris Alrumaihi, Faris F. Aba Alkhayl, Saad Alghamdi, Khalid Muhammad, Chih-Yang Huang, Jayasimha Rayalu Daddam, Haroon Khan, Sajid Maqsood and Mohammed Akli Ayoub

Life 2022, 12(7), 990; https://doi.org/10.3390/life12070990 - 4 Jul 2022

Cited by 6 | Viewed by 3827

Abstract

Camel milk (CM) constitutes an important dietary source in the hot and arid regions of the world. CM is a colloidal mixture of nutritional components (proteins, carbohydrates, lipids, vitamins, and minerals) and non-nutritional components (hormones, growth factors, cytokines, immunoglobulins, and exosomes). Although the [...] Read more.

Camel milk (CM) constitutes an important dietary source in the hot and arid regions of the world. CM is a colloidal mixture of nutritional components (proteins, carbohydrates, lipids, vitamins, and minerals) and non-nutritional components (hormones, growth factors, cytokines, immunoglobulins, and exosomes). Although the majority of previous research has been focused on the nutritional components of CM; there has been immense interest in the non-nutritional components in the recent past. Reckoning with these, in this review, we have provided a glimpse of the recent trends in CM research endeavors and attempted to provide our perspective on the therapeutic efficacy of the nutritional and non-nutritional components of CM. Interestingly, with concerted efforts from the research fraternities, convincing evidence for the better understanding of the claimed traditional health benefits of CM can be foreseen with great enthusiasm and is indeed eagerly anticipated. Full article

(This article belongs to the Special Issue Polyphenolic Compounds and Their Nanoformulation: Metabolism and Impact on Human Health)

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