Triflic Anhydride-Mediated Unprecedented Reactivities of Diacetonide Endoglucofuranose and Ribose Tetracetate: Direct Access to γ-Butenolides and Oxazoles.

Herein, we present two unprecedented reactions for the synthesis of γ-butenolides and oxazoles, leveraging TfO's promoted reactivity of nitriles with diacetonide endoglucofuranose and 1,2,3,5-tetra--acetyl-β-d-ribofuranose. This method is highly efficient and straightforward and employs a one-step, metal-free protocol. It is effective with both aromatic and aliphatic nitriles and demonstrates a broad substrate scope.

A novel mutation in non-constitutive lycopene beta cyclase (CstLcyB2a) from Crocus sativus modulates carotenoid/apocarotenoid content, biomass and stress tolerance in plants.

Mutation at A in lycopene-β-cyclase of Crocus (CstLcyB2a) sterically hinders its binding of δ-carotene without affecting lycopene binding, thereby diverting metabolic flux towards β-carotene and apocarotenoid biosynthesis. Crocus sativus, commonly known as saffron, has emerged as an important crop for research because of its ability to synthesize unique apocarotenoids such as crocin, picrocrocin and safranal. Metabolic engineering of the carotenoid pathway can prove a beneficial strategy for enhancing the quality of saffron and making it resilient to changing climatic conditions.

Design, synthesis, , and evaluation of pyrrol-2-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE/BACE 1 dual inhibitors.

Alzheimer's disease (AD) manifests as a progressive decline in cognitive function and mental behavior. Targeting two crucial enzymes associated with AD, acetylcholinesterase (AChE) and BACE 1 (Beta-site APP Cleaving Enzyme), in combination, holds promise for therapeutic breakthroughs. In this study, 40 derivatives of pyrrol-2-yl-phenyl allylidene hydrazine carboximidamide were designed based on prior research.

2,3-Difunctionalization of quinones: a gold-catalyzed cascade approach for trifluoromethyl-amination or sulfoximination.

A one-pot domino protocol employing gold(I) catalysis has been developed for the cascade trifluoromethyl-amination/sulfoximination of quinones. Togni I serves as the trifluoromethyl installing precursor, while amine or sulfoximine serves as the aminating source. Preliminary investigations suggest a mutual activation of Togni I and the amine precursor, facilitating the facile difunctionalization of quinones with excellent regioselectivity.

Fluvoxamine maleate alleviates amyloid-beta load and neuroinflammation in 5XFAD mice to ameliorate Alzheimer disease pathology.

Introduction: Alzheimer pathology (AD) is characterized by the deposition of amyloid beta (Aβ) and chronic neuroinflammation, with the NLRP3 inflammasome playing a significant role. This study demonstrated that the OCD drug fluvoxamine maleate (FXN) can potently ameliorate AD pathology in 5XFAD mice by promoting autophagy-mediated clearance of Aβ and inhibiting the NLRP3 inflammasome.

Methods: We used mice primary astrocytes to establish the mechanism of action of FXN against NLRP3 inflammasome by using various techniques like ELISA, Western blotting, confocal microscopy, Immunofluorescence, etc.

Synthesis of aryl enopyranones directly from glycals and aromatic halides to access 2-deoxy-β-C-aryl glycosides.

An efficient synthesis of aryl enopyranones an oxidative Heck-type coupling reaction between ether protected D/L-glycals and different aryl halides is developed. This one-step method attaches an aryl group at the C-1 position keeping the C-1/C-2 double bond intact the Saegusa-Ito type oxidation, thus facilitating the synthesis of medicinally important 2-deoxy-β-aryl-C-glycosides after Pd/C reduction.

Chromatographic fingerprinting of epiphytic fungal strains isolated from and biological evaluation of isolated okaramine H.

Medicinal plants are "goldmines" of natural products, and continue to provide key scaffolds for drug development. They have immense therapeutic potential, encapsulating a plethora of metabolites within them, which have yet to be explored. (L.

Optimization of indole acetic acid produced by plant growth promoting fungus, aided by response surface methodology.

Indole acetic acid (IAA) is one of the prime communicator playing a chief role in the interaction between host plant and endophytes. IAA produced by the endophytes primarily contributes to plant growth and development. Here, we optimized IAA production by an endophytic fungus GG3F6 isolated from the asymptomatic rhizome of employing response surface methodology (RSM) and exploring its effect on the host plant biology.

Divergent Synthesis of Unsymmetrical Bis-heteroaryl Ketones via Base-Promoted Cascade Reactions of 1,2-Alkynedione-Derived -Propargylic β-Enaminones.

Herein we disclose a transition-metal-free, one-pot two-step strategy for the synthesis of unsymmetrical bis-heteroaryl ketones. -propargylic β-enaminones generated by the Michael addition of propargylamines onto heteroaryl 1,2-alkynediones have been utilized as synthetic equivalents of pyridine or pyrrole scaffolds. The use of alcohol as a solvent resulted in the formation of 2-alkoxylated pyridine scaffold, whereas the use of DMSO promoted the formation of a pyrrole motif.

TRPV4 facilitates the reprogramming of inflamed macrophages by regulating IL-10 production via CREB.

Background: Transient receptor potential vanilloid type 4 (TRPV4) is a versatile ion channel with diverse roles in immune cells, including macrophages. While its function in inflammation remains debated, we investigated its role in regulating IL-10 production and its impact on macrophage reprogramming during inflammation.

Methods: We investigated the connection between TRPV4 activation and CREB-mediated IL-10 production during inflammation.

Microbial transformation of some phytochemicals into value-added products: A review.

Phytochemicals, plant-derived compounds, are the major components of traditional medicinal plants. Some phytochemicals have restricted applications, due to low bioavailability and less efficacy. However, their medicinal properties can be enhanced by converting them into value-added products for different bioactivities like anti-oxidant, neuroprotective, anti-obesity, anti-neuroinflammatory, anti-microbial, anti-cancer and anti-inflammatory.

Micelle-mediated synthesis of quinoxaline, 1,4-benzoxazine and 1,4-benzothiazine scaffolds from styrenes.

A range of heterocycles based on quinoxalines, 1,4-benzoxazines and 1,4-benzothiazines have been accessed from styrenes by reacting them with benzene-1,2-diamine, 2-aminophenol and 2-aminothiophenol respectively in micellar medium. This reaction occurring in a less explored cetylpyridinium bromide (CPB) micellar medium operates in the presence of NBS through a tandem hydrobromination-oxidation cascade, converting styrenes to phenacyl bromides. Its subsequent nucleophilic addition with aromatic 1,2-dinucleophiles and further transformations led to the formation of heterocyclic constructs.

Repurposing FDA approved drugs against Sterol C-24 methyltransferase of Leishmania donovani: A dual in silico and in vitro approach.

Leishmaniasis is a disease caused by the parasite Leishmania donovani affecting populations belonging to developing countries. The present study explores drug repurposing as an innovative strategy to identify new uses for approved clinical drugs, reducing the time and cost required for drug discovery. The three-dimensional structure of Leishmania donovani Sterol C-24 methyltransferase (LdSMT) was modeled and 1615 FDA-approved drugs from the ZINC database were computationally screened to identify the potent leads.

Unveiling the potential of novel indol-3-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE/BACE 1 dual inhibitors: a combined , synthesis and study.

Considering the failure of many enzyme inhibitors for Alzheimer's disease (AD), research is now focused on multi-target directed drug discovery. In this paper, inhibition of two essential enzymes implicated in AD pathologies, acetylcholinesterase (AChE) and BACE 1 (Beta-site APP Cleaving Enzyme), has been explored. Taking clues from our previous work, 41 novel indol-3-yl phenyl allylidene hydrazine carboximidamide derivatives were synthesized.

Synthesis and Biological Evaluation of Colchicine─Aryl/Alkyl Amine Hybrids as Potential Noncytotoxic Cholinesterase Inhibitors: Identification of SBN-284 as a Dual Inhibitor of Cholinesterases and NLRP3 Inflammasome.

Colchicine, one of the oldest anti-inflammatory natural products still used clinically, inhibits NF-κB signaling and NLRP3 inflammasome activation. Despite its cytotoxicity and narrow therapeutic range, colchicine continues to intrigue medicinal chemists exploring its anti-inflammatory potential. This study aimed to investigate the colchicine scaffold for its role in Alzheimer's disease by targeting neuroinflammation and cholinesterases.

Modular access to sulfur substituted analogues of isocytosine photoredox catalysis.

A photoredox approach for synthesizing sulfur-substituted analogues of isocytosine coupling of modular phenyl propargyl chloride with thiourea has been reported. The resulting product with an amine group was found amenable to various late-stage modifications, providing access to a broad range of sulfur-containing isocytosine derivatives.

Canniprene B, a new prenylated dihydrostilbene with cytotoxic activities from the leaves of .

A new, canniprene B (), along with five known (- and -) dihydrostilbenes were isolated from the leaves of collected at CSIR - IIIM, Jammu, India. Structures of all isolated compounds were elucidated by spectroscopic data analysis, including 1D and 2D NMR, and HR-ESI-MS. Canniprene B is a new prenylated dihydrostilbenes, a positional isomer of the known compound canniprene ().

Seabuckthorn pulp extract alleviates UV-B-induced skin photo-damage by significantly reducing oxidative stress-mediated endoplasmic reticulum stress and DNA Damage in human primary skin fibroblasts and Balb/c mice skin.

Skin homeostasis is predominantly compromised by exposure to UV-B irradiation, leading to several physiopathological processes at cellular and tissue levels that deteriorate skin function and integrity. The current study investigated the photo-protective role of seabuckthorn fruit pulp (SBT) extract against UV-B-induced damage in primary human skin fibroblasts (HDFs) and Balb/C mice skin. We subjected HDFs and Balb/C mice to UV-B irradiation and measured multiple cellular damage indicators.

Molecular Docking and Molecular Dynamics Simulations of Synthesized Thiazole-Isatin-1,2,3-triazole Hybrids as Promising Inhibitors for DNA Gyrase and Sterol 14α-Demethylase.

In the present work, a new class of thiazole-isatin-1,2,3-triazole hybrids (5 a-5 p) and precursor alkyne hybrids (6 a-6 d) has been reported with their in-silico studies. After structural identifications using different spectroscopic technique such as FTIR, H and C NMR and HRMS, the synthesized hybrids were explored for their biological potential using molecular docking and molecular dynamics calculations. Molecular docking results revealed that compound 5 j showed maximum binding energy i.

Medicinal plants traditionally used in health care practices by inhabitants of Paddar region of Jammu and Kashmir, India.

Ethnopharmacological Relevance: The present study is the first quantitative assessment of ethno-medicinal plants of Paddar region of Jammu and Kashmir.

Aim Of The Study: The study aimed to document the relative importance of medicinal plants used in human ailments by the villagers in the Paddar region of Jammu and Kashmir, India.

Material And Methods: Data were collected from 132 informants (72 male and 60 female) through semi structured interviews and group discussions.

A review of microbes mediated biosynthesis of silver nanoparticles and their enhanced antimicrobial activities.

In recent decades, biosynthesis of metal and (or) metal oxide nanoparticles using microbes is accepted as one of the most sustainable, cost-effective, robust, and green processes as it does not encompass the usage of largely hazardous chemicals. Accordingly, numerous simple, inexpensive, and environmentally friendly approaches for the biosynthesis of silver nanoparticles (AgNPs) were reported using microbes avoiding conventional (chemical) methods. This comprehensive review detailed an advance made in recent years in the microbes-mediated biosynthesis of AgNPs and evaluation of their antimicrobial activities covering the literature from 2015-till date.