Interaction of silymarin components and their sulfate metabolites with human serum albumin and cytochrome P450 (2C9, 2C19, 2D6, and 3A4) enzymes
In this study, the interactions of five silymarin components (silybin A, silybin B, isosilybin A, silychristin, and 2,3-dehydrosilychristin) and their sulfate metabolites were examined with human serum albumin and CYP (2C9, 2C19, 2D6, and 3A4) enzymes. Our results demonstrate that each compound tested forms stable complexes with albumin, and certain silymarin components/metabolites can inhibit CYP enzymes. Most of the sulfate conjugates were less potent inhibitors of CYP enzymes, but 2,3-dehydrosilychristin-19-O-sulfate showed the strongest inhibitory effect on CYP3A4. Based on these observations, the simultaneous administ...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - March 11, 2021 Category: Drugs & Pharmacology Authors: Zelma Faisal Violetta Mohos Eszter Flisz ár-Nyúl Kate řina Valentová Krist ýna Káňová Be áta Lemli S ándor Kunsági-Máté Mikl ós Poór Source Type: research
Interaction of silymarin components and their sulfate metabolites with human serum albumin and cytochrome P450 (2C9, 2C19, 2D6, and 3A4) enzymes
In this study, the interactions of five silymarin components (silybin A, silybin B, isosilybin A, silychristin, and 2,3-dehydrosilychristin) and their sulfate metabolites were examined with human serum albumin and CYP (2C9, 2C19, 2D6, and 3A4) enzymes. Our results demonstrate that each compound tested forms stable complexes with albumin, and certain silymarin components/metabolites can inhibit CYP enzymes. Most of the sulfate conjugates were less potent inhibitors of CYP enzymes, but 2,3-dehydrosilychristin-19-O-sulfate showed the strongest inhibitory effect on CYP3A4. Based on these observations, the simultaneous administ...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - March 11, 2021 Category: Drugs & Pharmacology Authors: Zelma Faisal Violetta Mohos Eszter Flisz ár-Nyúl Kate řina Valentová Krist ýna Káňová Be áta Lemli S ándor Kunsági-Máté Mikl ós Poór Source Type: research
Molecules, Vol. 26, Pages 1409: SARS-CoV-2 Main Protease Active Site Ligands in the Human Metabolome
In this study, we present an analysis on the substances identified in the human metabolome capable of binding the active site of the SARS-CoV-2 main protease (Mpro). The substances present in the human metabolome have both endogenous and exogenous origins. The aim of this research was to find molecules whose biochemical and toxicological profile was known that could be the starting point for the development of antiviral therapies. Our analysis revealed numerous metabolites—including xenobiotics—that bind this protease, which are essential to the lifecycle of the virus. Among these substances, silybin, a flavolignan com...
Source: Molecules - March 5, 2021 Category: Chemistry Authors: Anna Maria Sardanelli Camilla Isgr ò Luigi Leonardo Palese Tags: Article Source Type: research
Peptides Derived From the α-Core and γ-Core Regions of a Putative Silybum marianum Flower Defensin Show Antifungal Activity Against Fusarium graminearum
In this report, we have cloned the putative antimicrobial protein DefSm2, expressed in flowers of the wild plant Silybum marianum. The cDNA encodes a protein with two fused basic domains of an N-terminal defensin domain (DefSm2-D) and a C-terminal Arg-rich and Lys-rich domain. To further characterize the DefSm2-D domain, we built a 3D template-based model that will serve to support the design of novel antifungal peptides. We have designed four potential antifungal peptides: two from the DefSm2-D α-core region (SmAPα1-21 and SmAPα10-21) and two from the γ-core region (SmAPγ27-44 and SmAPγ29-35). We have chemically syn...
Source: Frontiers in Microbiology - February 17, 2021 Category: Microbiology Source Type: research
Molecules, Vol. 26, Pages 791: Chitosan Elicitation Impacts Flavonolignan Biosynthesis in Silybum marianum (L.) Gaertn Cell Suspension and Enhances Antioxidant and Anti-Inflammatory Activities of Cell Extracts
Haider Abbasi
Silybum marianum (L.) Gaertn is a rich source of antioxidants and anti-inflammatory flavonolignans with great potential for use in pharmaceutical and cosmetic products. Its biotechnological production using in vitro culture system has been proposed. Chitosan is a well-known elicitor that strongly affects both secondary metabolites and biomass production by plants. The effect of chitosan on S. marianum cell suspension is not known yet. In the present study, suspension cultures of S. marianum were exploited for their in vitro potential to produce bioactive flavonolignans in the presence of chitosan. Establi...
Source: Molecules - February 3, 2021 Category: Chemistry Authors: Muzamil Shah Hasnain Jan Samantha Drouet Duangjai Tungmunnithum Jafir Hussain Shirazi Christophe Hano Bilal Haider Abbasi Tags: Article Source Type: research
