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In the present study, we isolated linalool, geraniol, carvacrol, thymol, menthol and eugenol; synthesised their phenoxyacetic acid derivatives; and assessed their phytotoxic and genotoxic potentials against weeds and agricultural crops. Moreover, the fungicidal activity of both categories of compounds against 12 fungi was examined. Finally, using probabilistic assessment based on Risk Quotient (RQ) by the Monte Carlo simulation (MCS) method, we examined human health risks via oral exposure to these compounds. Toxic potencies to plants demonstrated that all parameters and related indices including germination percentage, mean germination time, germination rate, root length, shoot length, seedling length and vigour index dose-dependently decreased in both weeds and agricultural crops. Based on the comet assay, DNA damage was observed in the root meristems of the plants. Consequently, a significant decrease was observed in head DNA, whereas a significant increase in tail DNA was observed in response to treatments. Besides, the natural components and semisynthetic molecules showed a broad spectrum of fungicidal traits. However, eugenol and eugenoxyacetic acid inhibitory effects on the growth of the tested fungi were similar to that of benomyl. Our probabilistic health risk assessment indicated di minimis risk for natural components and their phenoxyacetic acid derivatives. Sensitivity analysis showed that concentrations of residues of the compounds had the most significant effect on risk. Current findings could offer a platform for developing sustainable approaches to reduce chemical residues and their consequent risks to the environment and human health. [ABSTRACT FROM AUTHOR]

This review aimed to identify preclinical and clinical studies examining the effects of rosmarinic acid (RA), carnosic acid (CaA), rosmanol (RO), carnosol (CA), and ursolic acid (UA) against allergic and immunologic disorders. Various online databases, including PubMed, Science Direct, EMBASE, Web of Sciences, Cochrane trials, and Scopus, were searched from inception until October 2022. Due to the suppression of the nuclear factor‐κB (NF‐κB) pathway, the main factor in allergic asthma, RA may be a promising candidate for the treatment of asthma. The other ingredients comprising CA and UA reduce the expression of interleukin (IL)‐4, IL‐5, and IL‐13 and improve airway inflammation. Rosemary's anti‐cancer effect is mediated by several mechanisms, including DNA fragmentation, apoptosis induction, inhibition of astrocyte‐upregulated gene‐1 expression, and obstruction of cell cycle progression in the G1 phase. The compounds, essentially found in Rosemary essential oil, prevent smooth muscle contraction through its calcium antagonistic effects, inhibiting acetylcholine (ACH), histamine, and norepinephrine stimulation. Additionally, CA exhibits a substantially greater interaction with the nicotinic ACH receptor than a family of medications that relax the smooth muscles, making it a potent antispasmodic treatment. The components have demonstrated therapeutic effects on the immune, allergy, and respiratory disorders. [ABSTRACT FROM AUTHOR]

Objective(s): Biofilm-associated infections are challenging to manage or treat since the biofilm matrix is impenetrable to most antibiotics. Therefore, the best approach to deal with biofilm infections is to interrupt the construction during the initial levels. Biofilm formation has been regulated through the quorum sensing (QS) network, making it an attractive target for any antibacterial therapy. Materials and Methods: Here, some coumarin members, including umbelliprenin, 4-farnesyloxycoumarin, gummosin, samarcandin, farnesifrol A, B, C, and auraptan, have been assessed as QS inhibitors in silico and in vitro. Their potential inhibitory effects on biofilm formation and virulence factor production of Pseudomonas aeruginosa PAO1 were evaluated. Results: First, the interaction of these compounds was investigated against one of the major transcriptional regulator proteins, PqsR, using molecular docking and structural analysis methodology. After that, in vitro evaluations indicated that 4-farnesyloxycoumarin and farnesifrol B showed considerable reduction in biofilm formation (62% and 56%, respectively), virulence factor production, and synergistic effects with tobramycin. Moreover, 4-farnesyloxycoumarin significantly (99.5%) reduced PqsR gene expression. Conclusion: The biofilm formation test, virulence factors production assays, gene expression analysis, and molecular dynamic simulations data demonstrated that coumarin derivatives are a potential antiQS family through PqsR inhibition. [ABSTRACT FROM AUTHOR]

The SARS‐CoV‐2 COVID‐19 pandemic has emerged as an unprecedented emergency state in healthcare system and global challenge. In recent decade, the function of exogenous H2S in the treatment of respiratory diseases has been investigated using H2S‐donor agents. Ferula foetida is a medicinal plant that is traditionally used in respiratory diseases including asthma and viral respiratory diseases. The oleo‐gum of this plant is a rich source of several organic sulfides including thiophenes, disulfides and polysulfide derivatives, which can act as H2S‐donor agents. The purpose of this study was to investigate the efficacy of Covexir® (F. foetida oleo‐gum) treatment as a rich source of H2S‐donor compounds in clinical presentations of patients with COVID‐19. The efficacy of Covexir® was evaluated in a randomized, double‐blind, placebo‐controlled trial in outpatients with COVID‐19. Covexir® could significantly inhibit cough when compared to the placebo group (p <.01 and p < 001, respectively). Moreover, there was a significant difference (p < 001) between the two groups in dyspnea symptom at follow‐up interval of 7 day after receiving Covexir®. Furthermore, on days 3 and 7, statistically significant differences were observed in myalgia, anorexia, anosmia, and sense of taste severity between two groups. Our findings revealed that Covexir® was very safe in the treatment of COVID‐19 patients with mild to moderate symptoms and it can be recommended to improve clinical presentations of patients with COVID‐19 such as cough, shortness of breath, myalgia, anorexia, anosmia, and sense of taste. [ABSTRACT FROM AUTHOR]

Objective: The present study was conducted to find cytotoxic compounds from oleo-gum-resin of Ferula assa-foetida (asafoetida). Materials and Methods: A dichloromethane extract of asafoetida was subjected to different chromatography analyses (including column chromatography, preparative thin layer chromatography and high performance liquid chromatography) to isolate its bioactive sesquiterpene coumarins. The structures of isolated compounds were elucidated through 1H-NMR spectra interpretation and comparison with those reported in the literature. To measure the cytotoxic activity of pure compounds, a non-fluorescent substrate called resazurin (alamarBlue®) was used in this study. Human breast and prostate cancer cell lines (MCF-7 and PC-3, respectively) and a normal human embryonic stem cell (NIH) were treated with different concentrations (50, 25, 12.5 and 6.25 µg/mL) of pure compounds. Results: In this study, 10 sesquiterpene coumarins were isolated from oleo-gum-resin of F. assa-foetida and cytotoxic activity of 6 compounds was tested against MCF-7 and PC-3 cell lines and NIH cells. Badrakemin acetate (7), ferukrinone (8) and deacetyl kellerin (10) were found for the first time in the oleo-gum-resin of F. assafoetida. Gummosin (4) showed moderate cytotoxic activity with IC50 values of 30 and 32.1 µg/mL against PC-3 and MCF-7 cell lines, respectively. None of the isolated compounds showed toxicity against NIH as a normal human cell line. Conclusion: The preferential cytotoxic activity of gummosin against cancer cell lines is reported for the first time in this study. [ABSTRACT FROM AUTHOR]

Based on World Health Organization reports, resistance of bacteria to well-known antibiotics is a major global health challenge now and in the future. Different strategies have been proposed to tackle this problem including inhibition of multidrug resistance pumps and biofilm formation in bacteria and development of new antibiotics with novel mechanism of action. Flavonoids are a large class of natural compounds, have been extensively studied for their antibacterial activity, and more than 150 articles have been published on this topic since 2005. Over the past decade, some promising results were obtained with the antibacterial activity of flavonoids. In some cases, flavonoids (especially chalcones) showed up to sixfold stronger antibacterial activities than standard drugs in the market. Some synthetic derivatives of flavonoids also exhibited remarkable antibacterial activities with 20- to 80-fold more potent activity than the standard drug against multidrug-resistant Gram-negative and Gram-positive bacteria (including Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus). This review summarizes the ever changing information on antibacterial activity of flavonoids since 2005, with a special focus on the structure-activity relationship and mechanisms of actions of this broad class of natural compounds. [ABSTRACT FROM AUTHOR]

ABSTRACT Asafoetida is an oleo–gum‐resin mainly obtained from Ferula foetida in eastern Iran, which is employed for the treatment of stomachaches, acid reflux, nervous system disorders and respiratory diseases. Asafoetida has attracted the attention of researchers due to its sulfide compounds and their proven effects on respiratory illnesses. In this study, the shelf stability of supplement of F. foetida's oleo–gum‐resin by quantifying two key sulfide compounds including E/Z‐sec‐butyl propenyl disulfane and E/Z‐(methylthio)propyl 1‐propenyl disulfane was evaluated by 1H NMR (qH NMR) and gas chromatography–mass spectrometry (GC–MS). The similar results were obtained in both qH NMR and GC–MS methods. The qH NMR method showed good linearity in the ranges of 2–12 mg/mL for E/Z‐sec‐butyl propenyl disulfane and 2.2–17 mg/mL for E/Z‐(methylthio) propyl 1‐propenyl disulfane with a correlation coefficient of 0.99 and acceptable stability (RSD% ≤ 2.72%) for the quantification of the compounds. Therefore, despite the volatility of disulfide compounds and according to the results, the qH NMR method could be considered adequate method for quantifying these compounds in supplements containing the volatile components that requires extra extraction steps before analyses by other method. [ABSTRACT FROM AUTHOR]

The gradual emergence of new bacterial strains impervious to one or more antibiotics necessitates discovering and applying natural alternatives. Among natural products, various polyphenols exhibit antibacterial activity. However, polyphenols with biocompatible and potent antibacterial characteristics are limited due to low aqueous solubility and bioavailability; therefore, recent studies are considering new polyphenol formulations. Nanoformulations of polyphenols, especially metal nanoparticles, are currently being investigated for their potential antibacterial activity. Nanonization of such products increases their solubility and helps attain a high surface-to-volume ratio and, therefore, a higher reactivity of the nanonized products with better remedial potential than nonnanonized products. Polyphenolic compounds with catechol and pyrogallol moieties efficiently bond with many metal ions, especially Au and Ag. These synergistic effects exhibit antibacterial pro-oxidant ROS generation, membrane damage, and biofilm eradication. This review discusses various nano-delivery systems for considering polyphenols as antibacterial agents., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)