Cannabinoid and Opioid Receptor Affinity and Modulation of Cancer-Related Signaling Pathways of Machaeriols and Machaeridiols from Pers.

Machaeriols and machaeridiols are unique hexahydrodibenzopyran-type aralkyl phytocannabinoids isolated from Pers. Earlier studies of machaeriol A () and B () did not show any affinity for cannabinoid receptor 1 (CB1 or CNR1), although they are structural analogs of psychoactive hexahydrocannabinol. This study comprehensively reports on the affinities of isolated Pers.

In Vitro and In Silico Studies of Neolignans from L. Seeds against Human Cannabinoids and Opioid Receptors.

L. (Magnoliaceae) is a plant of considerable medicinal significance; its flowers and seeds have been used in various traditional remedies. Radioligand binding assays of -hexane seeds extract showed displacement of radioligand for cannabinoid (CB1 and CB2) and opioid δ (delta), κ (kappa), and µ (mu) receptors.

Antiplasmodial and antimicrobial activities of e-abietane diterpenoids from the roots of .

The root extract of Baill. afforded six previously described -abietane diterpenoids, namely 7-oxo--abieta-5(6),8(14),13(15)-trien-16,12-olide (), mangiolide (), 8,14:11,12-diepoxy-13(15)-abietane-16,12-olide (), 7,11,12-trihydroxy--abieta-8(14),13(15)-diene-16,12-olide (), 8α,14-dihydro-7-oxo-jolkinolide E (), jolkinolide A (), together with 3-sitosterol (), scopoletin () and vanillin (). Their structures were deduced through 1D and 2D NMR spectroscopic techniques, and HRESIMS, as well as by comparison of the NMR data with those reported in the literature.

Synthesis and Inhibitory Activity of Machaeridiol-Based Novel Anti-MRSA and Anti-VRE Compounds and Their Profiling for Cancer-Related Signaling Pathways.

Three unique 5,6-seco-hexahydrodibenzopyrans (seco-HHDBP) machaeridiols A−C, reported previously from Machaerium Pers., have displayed potent activities against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium, and E. faecalis (VRE).

Natural Products Inhibitors of Monoamine Oxidases-Potential New Drug Leads for Neuroprotection, Neurological Disorders, and Neuroblastoma.

Monoamine oxidase inhibitors (MAOIs) are an important class of drugs prescribed for treatment of depression and other neurological disorders. Evidence has suggested that patients with atypical depression preferentially respond to natural product MAOIs. This review presents a comprehensive survey of the natural products, predominantly from plant sources, as potential new MAOI drug leads.

Hepatoprotective Plants from Bangladesh: A Biophytochemical Review and Future Prospect.

Liver diseases are quite prevalant in many densely populated countries, including Bangladesh. The liver and its hepatocytes are targeted by virus and microbes, as well as by chemical environmental toxicants, causing wide-spread disruption of metabolic fuctions of the human body, leading to death from end-stage liver diseases. The aim of this review is to systematically explore and record the potential of Bangladeshi ethnopharmacological plants to treat liver diseases with focus on their sources, constituents, and therapeutic uses, including mechanisms of actions (MoA).

Ethiopian Medicinal Plants Traditionally Used for the Treatment of Cancer; Part 3: Selective Cytotoxic Activity of 22 Plants against Human Cancer Cell Lines.

Medicinal plants have been traditionally used to treat cancer in Ethiopia. However, very few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro-ecological zones of Ethiopia. Hence, the main aim of this study was to screen the cytotoxic activities of 80% methanol extracts of 22 plants against human peripheral blood mononuclear cells (PBMCs), as well as human breast (MCF-7), lung (A427), bladder (RT-4), and cervical (SiSo) cancer cell lines.

Schottiin, a new prenylated isoflavones from and antibacterial synergism studies between methicillin and fremontone against methicillin-resistant ATCC 1708.

Bioactivity guided isolation of an ethanol extract of the root of (Family Fabaceae) afforded a new prenylated isoflavone, named schottiin (5,7,5'-trihydroxy-4'--methyl-6'-(3,3-dimethylallyl)-isoflavone) (), together with four other isoflavones, including fremontone (), 5,7,4',5'-tetrahydroxy-2'-(3,3-dimethylallyl)-isoflavone (), glycyrrhisoflavone () and fremontin (), of which and identified as isomeric mixture. Structures of - were determined by full spectroscopic analyses. A comprehensive 2 D NMR spectral data has allowed revising the structure of fremontone as from previously reported Compound showed weak antibacterial activity against methicillin-resistant (MRSA).

Therapeutic Intervention of COVID-19 by Natural Products: A Population-Specific Survey Directed Approach.

To date very few promising leads from natural products (NP) secondary metabolites with antiviral and immunomodulatory properties have been identified for promising/potential intervention for COVID-19. Using in-silico docking studies and genome based various molecular targets, and their in vitro anti-SARS CoV-2 activities against whole cell and/or selected protein targets, we select a few compounds of interest, which can be used as potential leads to counteract effects of uncontrolled innate immune responses, in particular those related to the cytokine storm. A critical factor for prevention and treatment of SARS-CoV-2 infection relates to factors independent of viral infection or host response.

Crosstalk of Cancer Signaling Pathways by Cyclic Hexapeptides and Anthraquinones from .

The anticancer activities of and its constituents have been reported earlier, but their influence on the crosstalk of complex cancer-related signaling metabolic pathways (i.e., transcription factors; TF) has not yet been fully investigated.

Antimicrobial Constituents from Pers.: Inhibitory Activities and Synergism of Machaeriols and Machaeridiols against Methicillin-Resistant , Vancomycin-Resistant , and Permeabilized Gram-Negative Pathogens.

Two new epimeric bibenzylated monoterpenes machaerifurogerol () and 5--machaerifurogerol (), and four known isoflavonoids (+)-vestitol (), 7--methylvestitol (), (+)-medicarpin (), and 3,8-dihydroxy-9-methoxypterocarpan () were isolated from Pers. This plant was previously assigned as Spruce, from which machaeriols A-D (-) and machaeridiols A-C (-) were reported, and all were then re-isolated, except the minor compound , for a comprehensive antimicrobial activity evaluation. Structures of the isolated compounds were determined by full NMR and mass spectroscopic data.

Selective Interactions of -Methylated Flavonoid Natural Products with Human Monoamine Oxidase-A and -B.

A set of structurally related -methylated flavonoid natural products isolated from (), ( and ), (), (), and () plant species were characterized for their interaction with human monoamine oxidases (MAO-A and -B) in vitro. Compounds , , and showed selective inhibition of MAO-A, while and showed selective inhibition of MAO-B. Compound showed ~2-fold selectivity towards inhibition of MAO-A.

Synthesis of a pyrrolidine derivative of a carvotacetone and monoterpenes for anti-methicillin-resistant and anti-cryptococcal properties.

Monoterpene derivatives are of great biological relevance in the pharmaceutical industry. In the present study, pyrrolidine derivative of a carvotacetone, 3-benzylcarvotacetone (), and selected monoterpenes (3-hydroxy-2-isopropyl-5-methyl--benzoquinone () and piperitol ()) were prepared to provide ()-1-(4-(benzyloxy)-5-isopropyl-2-methylcyclohexa-1,3-dien-1-yl)-pyrrolidine (), 2-isopropyl-5-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl acetate (), 3-hydroxypiperitone () and carvacrol (). Structure of was determined based on NMR and HRMS spectral data.

Ethiopian Medicinal Plants Traditionally Used for the Treatment of Cancer, Part 2: A Review on Cytotoxic, Antiproliferative, and Antitumor Phytochemicals, and Future Perspective.

This review provides an overview on the active phytochemical constituents of medicinal plants that are traditionally used to manage cancer in Ethiopia. A total of 119 articles published between 1968 and 2020 have been reviewed, using scientific search engines such as ScienceDirect, PubMed, and Google Scholar. Twenty-seven medicinal plant species that belong to eighteen families are documented along with their botanical sources, potential active constituents, and in vitro and in vivo activities against various cancer cells.

Synthesis, structural assignments and antiinfective activities of 3--benzyl-carvotacetone and 3-hydroxy-2-isopropyl-5-methyl--benzoquinone.

In an attempt to synthesize carvotacetone analogues, new 3--benzyl-carvotacetone ( and previously reported 3-hydroxy-2-isopropyl-5-methyl--benzoquinone () were synthesized from piperitone (). In this work, we describe the synthesis of and other analogues from . Luche reduction of to -piperitol (, followed by benzylation yielded 3--benzyl-piperitol ().

Selective Inhibition of Human Monoamine Oxidase B by Acacetin 7-Methyl Ether Isolated from (Damiana).

The investigation of the constituents that were isolated from (damiana) for their inhibitory activities against recombinant human monoamine oxidases (MAO-A and MAO-B) in vitro identified acacetin 7-methyl ether as a potent selective inhibitor of MAO-B (IC = 198 nM). Acacetin 7-methyl ether (also known as 5-hydroxy-4', 7-dimethoxyflavone) is a naturally occurring flavone that is present in many plants and vegetables. Acacetin 7-methyl ether was four-fold less potent as an inhibitor of MAO-B when compared to acacetin (IC = 50 nM).

4--Methylhonokiol Influences Normal Cardiovascular Development in Medaka Embryo.

Although 4--Methylhonokiol (MH) effects on neuronal and immune cells have been established, it is still unclear whether MH can cause a change in the structure and function of the cardiovascular system. The overarching goal of this study was to evaluate the effects of MH, isolated from , on the development of the heart and vasculature in a Japanese medaka model in vivo to predict human health risks. We analyzed the toxicity of MH in different life-stages of medaka embryos.

Tetra-glucopyranosyl Diterpene ent-Kaur-16-en-19-oic Acid and ent-13(S)-Hydroxyatisenoic Acid Derivatives from a Commercial Extract of Stevia rebaudiana (Bertoni) Bertoni.

and its diterpene glycosides are one of the main focuses of food companies interested in developing novel zero calorie sugar substitutes since the recognition of steviol glycosides as Generally Recognized as Safe (GRAS) by the United States Food and Drug Administration. Rebaudioside A, one of the major steviol glycosides of the leaves is more than 200 times sweeter than sucrose. However, its lingering aftertaste makes it less attractive as a table-top sweetener, despite its human health benefits.

Efficacy of Prosopilosidine from var. against Infection in a Murine Model.

In this study, 2,3-dihydro-1-indolizinium alkaloid-prosopilosidine (PPD), that was isolated from , was evaluated against in a murine model of cryptococcosis. In vitro and in vivo toxicity of indolizidines were also evaluated. Mice were infected via the tail vein with live .

Antimycoplasmal Activities of Compounds from and against Strains from the Cluster.

Infections caused by species belonging to the cluster' negatively affect the agricultural sector through losses in livestock productivity. These strains are resistant to many conventional antibiotics due to the total lack of cell wall. Therefore, there is an urgent need to develop new antimicrobial agents from alternative sources such as medicinal plants to curb the resistance threat.

Quantitative Determination of Betaine, Choline, Acetylcholine, and 20-Hydroxyecdysone Simultaneously from Atriplex Species by UHPLC-UV-MS.

A simple, rapid, and sensitive UHPLC-UV-MS method was developed for the quantitative determination of betaine (1), choline (2), acetylcholine (3), and 20-hydroxyecdysone (4) from various species of Atriplex. The baseline separation of the four analytes was achieved on a reversed phase C 18 column within nine minutes. The mobile phase was composed of 50 mM ammonium formate in 2% methanol-water containing 5 mM sodium dodecyl sulfate (pH = 8.

Compounds from Terminalli brownii Extracts with Toxicity against the Fish Pathogenic Bacterium Flavobacterium columnare.

The pond-raised channel catfish (Ictaluruspunctatus) industry in the United States of America can incur losses of over a $100 million annually due to bacterial diseases including columnaris disease caused by Flavobacterium columnare. One management approach available to catfish producers is the use of medicated- feed containing antibiotics. However, the negative attributes of antibiotic use in agriculture include public concerns and the potential development of antibiotic-resistant bacteria.

Bioactive Formylated Flavonoids from Eugenia rigida: Isolation, Synthesis, and X-ray Crystallography.

Two new flavonoids, rac-6-formyl-5,7-dihydroxyflavanone (1) and 2',6'-dihydroxy-4'-methoxy-3'-methylchalcone (2), together with five known derivatives, rac-8-formyl-5,7-dihydroxyflavanone (3), 4',6'-dihydroxy-2'-methoxy-3'-methyldihydrochalcone (4), rac-7-hydroxy-5-methoxy-6-methylflavanone (5), 3'-formyl-2',4',6'-trihydroxy-5'-methyldihydrochalcone (6), and 3'-formyl-2',4',6'-trihydroxydihydrochalcone (7), were isolated from the leaves of Eugenia rigida. The individual (S)- and (R)-enantiomers of 1 and 3, together with the corresponding formylated flavones 8 (6-formyl-5,7-dihydroxyflavone) and 9 (8-formyl-5,7-dihydroxyflavone), as well as 2',4',6'-trihydroxychalcone (10), 3'-formyl-2',4',6'-trihydroxychalcone (11), and the corresponding 3'-formyl-2',4',6'-trihydroxydihydrochalcone (7) and 2',4',6'-trihydroxydihydrochalcone (12), were synthesized. The structures of the isolated and synthetic compounds were established via NMR, HRESIMS, and electronic circular dichroism data.

New ent-Clerodane and Abietane Diterpenoids from the Roots of Kenyan Croton megalocarpoides Friis & M. G. Gilbert.

The roots of the endangered medicinal plant Croton megalocarpoides collected in Kenya were investigated and twenty-two compounds isolated. Among them were twelve new ent-clerodane (1-12) and a new abietane (13) diterpenoids, alongside the known crotocorylifuran (4 a), two known abietane and four known ent-trachylobane diterpenoids, and the triterpenoids, lupeol and acetyl aleurotolic acid. The structures of the compounds were determined using NMR, HRMS and ECD.