Modern Pharmacology and the Role of Natural Products and Leads in Ethnomedicine

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: closed (20 May 2023) | Viewed by 6332

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Molecular Pharmacology Program, Laboratory of Signal Transduction, Mortimer B. Zuckerman Research Center, 417 East 68th Street, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA
Interests: molecular pharmacology; cancer pharmacology; natural products; ethnomedicine
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Special Issue Information

Dear Colleagues,

We wish to concentrate on current developments, novel therapeutic techniques, and the ethnomedicinal significance of natural products, natural compounds, and their novel derivatives in our Special Issue on modern pharmacology. All of these actions point to a significant issue in human sickness and health. We need to identify the target pharmaceuticals so they can only be utilized for use in very good herbal remedies and for their pharmacological benefits, as the expense of healthcare continues to be a significant concern and a financial burden on low-income families. According to the WHO, most pharmaceuticals are available on the market but are very expensive and out of the reach of all patients. The number of these fatalities is increasing daily. Moreover, the prevalence of infections and diseases that are resistant to drugs is rising.

The WHO produced a report in 2019 to prevent a potentially catastrophic drug-resistance catastrophe; they forecast that, by 2050, drug-resistant infections will be responsible for around 10 million annual deaths, and that by 2030, drug resistance will lead to 24 million people into extreme poverty. Lastly, according to the WHO, cancer is the largest cause of mortality across the globe (in 2020 caused about 10 million deaths worldwide). Breast, lung, colon and rectum, prostate, skin, and stomach cancers were the most prevalent in 2020.

Thus, pharmacological repositioning or repurposing as well as natural leads and their derivatives can be used to discover novel and more effective treatments for the aforementioned disorders. Natural leads and their derivatives are examples of natural products that have anti-inflammatory, anti-bacterial, anti-fungal, anti-cancer, neuroprotective, cardioprotective, chemo-preventative, antimicrobial, and antimalarial properties.

Dr. Arjun Singh
Guest Editor

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Keywords

  • modern pharmacology
  • natural products
  • natural compounds
  • ethnomedicine

Published Papers (3 papers)

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Research

17 pages, 2104 KiB  
Article
Selection of a Digitalis purpurea Cell Line with Improved Bioconversion Capacity of Hydroquinone into Arbutin
by Carmen Elena Pop, Ana Coste, Ana-Maria Vlase, Constantin Deliu, Mircea Tămaș, Tibor Casian and Laurian Vlase
Life 2024, 14(1), 84; https://doi.org/10.3390/life14010084 - 4 Jan 2024
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Abstract
This study aimed to investigate the biotransformation capabilities of a hydroquinone-tolerant Digitalis purpurea cell line (DpHQ) for bioconverting hydroquinone (HQ) into arbutin, a compound with significant therapeutic and cosmetic applications. The research evaluated the influence of various HQ concentrations, feeding protocols, and carbon [...] Read more.
This study aimed to investigate the biotransformation capabilities of a hydroquinone-tolerant Digitalis purpurea cell line (DpHQ) for bioconverting hydroquinone (HQ) into arbutin, a compound with significant therapeutic and cosmetic applications. The research evaluated the influence of various HQ concentrations, feeding protocols, and carbon sources on arbutin bioconversion yield. By using HPLC-MS for the quantification of arbutin in biomass and medium, the study revealed that higher precursor (HQ) concentration led to a more pronounced growth inhibition under single dosing than sequential dosing. At lower sugar (3%) and precursor (4 mM HQ) levels, arbutin predominantly remained within the cells, whereas higher sugar (6%) and HQ (5–6 mM) levels promoted its release into the medium. Arbutin production ranged from 591 mg/L under single dosing to 3049 mg/L with sequential dosing, with the highest yield being achieved with 5 mM HQ in divided doses and 6% glucose. This study holds novelty for being the first to demonstrate the DpHQ’s tolerance to high concentrations of HQ and its efficient capabilities to bioconvert HQ to arbutin, indicating that D. purpurea is equipped with the enzymes required for this process. These aspects highlight its potential as a biotechnological source for arbutin synthesis. Full article
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14 pages, 3023 KiB  
Article
Hypolipidemic and Antihyperlipidemic Effects of Holarrhena pubescens Methanolic Extract Is Mediated through Inhibition of Lipase Activity and Lipid Accumulation
by AbdulRahman A. I. Alyahya, Mohammed Asad, Mohammed Alrouji, Kamal Eldin Ahmed Abdelsalam, Adel Mashan Rashed Al-Mutairi and Monjid Ahmed Ibrahim Ahmed
Life 2023, 13(7), 1435; https://doi.org/10.3390/life13071435 - 24 Jun 2023
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Abstract
Holarrhena pubescens seeds are used in the treatment of various diseases, especially diabetes and associated complications, in different parts of the world. The present study was undertaken to determine the hypolipidemic and antihyperlipidemic effects of methanolic extract of H. pubescens seeds in rats. [...] Read more.
Holarrhena pubescens seeds are used in the treatment of various diseases, especially diabetes and associated complications, in different parts of the world. The present study was undertaken to determine the hypolipidemic and antihyperlipidemic effects of methanolic extract of H. pubescens seeds in rats. The extract was subjected to LC-MS analysis to determine the chemical constituents. The hypolipidemic action was studied by determining the effect of 28-day oral administration of seed extract on serum cholesterol, serum triglycerides, and serum HDL-cholesterol levels. The antihyperlipidemic action was studied in rats fed with a high-fat diet containing cholesterol and saturated fat, and the same lipid parameters were estimated during 28-day treatment. To elucidate its probable mechanism of action, in vitro studies on the inhibition of lipid accumulation in preadipocytes, DPP-IV inhibitory effect, and lipase enzyme inhibition were studied. The seed extract reduced serum levels of cholesterol and triglycerides in both normal rats and animals fed with a high-fat diet without a significant effect on HDL-cholesterol levels. The seed extract was highly effective in inhibiting lipase enzyme activity but showed a modest effect on the inhibition of lipid accumulation and DPP-IV. The results demonstrated that H. pubescens seed extract has hypolipidemic and antihyperlipidemic effects mediated probably through inhibition of lipase enzyme activity. Full article
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27 pages, 1783 KiB  
Article
Phytochemical Profile, Antioxidant, Antimicrobial, and Antidiabetic Activities of Ajuga iva (L.)
by Soukaina Saidi, Firdaous Remok, Nadia Handaq, Aziz Drioiche, Aman Allah Gourich, Naoual El Menyiy, Smail Amalich, Mohamed Elouardi, Hanane Touijer, Mohamed Bouhrim, Latifa Bouissane, Hiba-Allah Nafidi, Yousef A. Bin Jardan, Mohammed Bourhia and Touriya Zair
Life 2023, 13(5), 1165; https://doi.org/10.3390/life13051165 - 11 May 2023
Cited by 5 | Viewed by 2977
Abstract
In Morocco, many applications in ethnomedicine on Ajuga iva (L.) have been recognized as able to treat various pathologies such as diabetes, stress, and microbial infections. The objective of this work is to carry out phytochemical, biological, and pharmacological investigations on the extracts [...] Read more.
In Morocco, many applications in ethnomedicine on Ajuga iva (L.) have been recognized as able to treat various pathologies such as diabetes, stress, and microbial infections. The objective of this work is to carry out phytochemical, biological, and pharmacological investigations on the extracts of Ajuga iva leaves in order to confirm its therapeutic effects. The phytochemical screening carried out on the different extracts of Ajuga iva showed its richness in primary (lipids and proteins) and secondary metabolites (flavonoids, tannins, reducing compounds, oses, and holoside. The best contents of polyphenols, flavonoids, and tannins evaluated by spectrophotometric methods were found in the hydroethanolic extract (69.850 ± 2.783 mg EAG/g DE, 17.127 ± 0.474 mg EQ/g DE, 5.566 ± 0.000 mg EQC/g DE), respectively. Analysis of the chemical composition of the aqueous extract by LC/UV/MS revealed 32 polyphenolic compounds including ferulic acid (19.06%), quercetin (10.19%), coumaric acid (9.63%), and apigenin-7-(2-O-apiosylglucoside) (6.8%). The antioxidant activity of Ajuga iva extracts was evaluated by three methods (DPPH*, FRAP, CAT). The hydroethanolic extract recorded the strongest reducing power: DPPH* (IC50 = 59.92 ± 0.7 µg/mL), FRAP (EC50 = 196.85 ± 1.54 (µg/mL), and CAT (199.21 ± 0.37 mg EAG/gE). A strong correlation between phenolic compounds and antioxidant activities was confirmed by the determination of Pearson’s coefficient. The antimicrobial activity of Ajuga iva studied by the microtiter method revealed potent antifungal and antibacterial qualities against Candida parapsilosis and Staphylococcus aureus BLACT. An in vivo oral glucose tolerance test (OGTT) using normal rats revealed that the antihyperglycemic action of the aqueous extract significantly reduced postprandial hyperglycaemia at (30 min, p < 0.01) and area under the curve (AUC glucose), p < 0.01. Similarly, the aqueous extract, tested on pancreatic α-amylase enzyme activity in vitro and in vivo significantly inhibited pancreatic α-amylase activity with IC50 = 1.52 ± 0.03 mg/mL. In conclusion, the extract from Ajuga iva could be a good source of bioactive molecules, which exhibit potent antioxidant and antimicrobial activity, as well as strong antidiabetic activity, for applications in the pharmaceutical industry. Full article
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