Aims Glycyrrhiza glabra is a high‐value medicinal plant thriving in biodiversity rich Kashmir Himalaya. The present study was designed to explore the fungal endophytes from G. glabra as a source of bioactive molecules. Methods and Results The extracts prepared from the isolated endophytes were evaluated for anti‐microbial activities using broth micro‐dilution assay. The endophytic strain coded as A2 exhibiting promising anti‐bacterial as well as anti‐tuberculosis activity was identified as Fusarium solani by ITS‐5.8S ribosomal gene sequencing technique. This strain was subjected to large‐scale fermentation followed by isolation of its bioactive compounds using column chromatography. From the results of spectral data analysis and comparison with literature, the molecules were identified as 3,6,9‐trihydroxy‐7‐methoxy‐4,4‐dimethyl‐3,4‐dihydro‐1H‐benzo[g]isochromene‐5,10‐dione (1), fusarubin (2), 3‐O‐methylfusarubin (3) and javanicin (4). Compound 1 is reported for the first time from this strain. All the four compounds inhibited the growth of various tested bacterial strains with MIC values in the range of <1 to 256 μg ml−1. Fusarubin showed good activity against Mycobacterium tuberculosis strain H37Rv with MIC value of 8 μg ml−1, whereas compounds 1, 3 and 4 exhibited moderate activity with MIC values of 256, 64, 32 μg ml−1, respectively. Conclusions To the best of our knowledge, this is the first study that reports significant anti‐tuberculosis potential of bioactive molecules from endophytic F. solani evaluated against the virulent strain of M. tuberculosis. This study sets background towards their synthetic intervention for activity enhancement experiments in anti‐microbial drug discovery programme. Significance and Impact of the Study Due to the chemoprofile variation of same endophyte with respect to source plant and ecoregions, further studies are required to explore endophytes of medicinal plants of all unusual biodiversity rich ecoregions for important and or novel bioactive molecules.

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In the presence of NBS and a catalytic amount of a Lewis acid, 2,3-unsaturated allyl glycosides [6-(allyloxy)-3,6-dihydro-2-(hydroxymethyl)-2H-pyran-3-ol] have been successfully used as versatile glycosyl donors for the stereoselective α-glycosylation of a variety of alcohols comprising sensitive functions such as acetonide, keto, nitro, and ester in 50-90% yields. The methodology offers an equally facile alternative to 4-pentenyl replacement in unsaturated sugars.

BackgroundResistance to chemotherapy represents a major obstacle in correcting colorectal carcinomas (CRC). Inspite of recent advances in the treatment of metastatic disease, the prognosis of the patients remains poor. RLX, a vasicinone analogue has been reported to possess potent bronchodilator, anti-asthmatic and anti-inflammatory properties. However, its anti-cancer activity is unknown.ResultsHere, we report for the first time that RLX has anti-cancer property against panel of human cancer cell lines and most potent activity was found against HCT-116 cells with IC50 value of 12 μM and have further investigated the involvement of NFκB and caspase-3 in RLX action in CRC apoptosis. Following RLX and BEZ-235 treatment in HCT-116, we observed significant down-regulation of NFκB (1 to 0.1 fold) and up-regulation of caspase-3 (1 to 2 fold) protein expressions. Additionally, morphological studies revealed membrane blebbing, cell shrinkage, chromatin condensation and finally apoptosis in HCT-116 cells.ConclusionsOverall, these findings indicate that RLX is a potent small molecule which triggers apoptosis, and promising potential candidate to be a chemotherapeutic agent.

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