Efficient Ru-Catalyzed Electrochemical Homo- and Heterocoupling Reaction of Terminal Alkynes: Synthesis, In Vitro Anticancer Activity, and Docking Study.

With the objective to identify novel anticancer leads, herein ruthenium-catalyzed electrochemical homo- and heterocoupling reactions of terminal alkynes have been developed for the synthesis of the desired products. Among the synthesized 1,3-diynes, some of them were rigorously examined for possible in vitro anticancer activity against HeLa (human cervical cancer) and L6 normal (rat skeletal muscle) cell lines. Additionally, the docking study was also performed toward 16 ovarian cancer targets with binding affinity calculations with respect to the standard. To the best of our knowledge, this is the first scientific report on the ruthenium-catalyzed electrochemical homocoupling reaction between terminal alkynes with its in vitro anticancer and in silico docking studies.

Chemical composition, antimicrobial activity and cytotoxicity of Murraya paniculata (L.) Jack leaf essential oil from Assam, India: the effect of oil on cellular morphology of micro-organisms.

Murraya paniculata (L.) Jack is commonly cultivated as ornamental plant in Assam and has been used as spice and phytomedicine traditionally for many healthcare purposes. The therapeutic potential and chemical constituents of the essential oil of M. paniculata leaf was investigated against several pathogenic microbial species and human cancer cell lines. 29 chemical compounds were identified by GC-MS analysis from the essential oil representing 97.62% of the oil. The major compound identified was caryophyllene (20.93%). Leaf essential oil exhibited promising antibacterial activity against Mycobacterium smegmatis (MIC = 4 µg/mL) and Pseudomonas aeruginosa (MIC = 4 µg/mL). Best anticancer activity of the oil was observed for HeLa cells (IC50 = 6.28 µg/mL). Further, scanning electron microscopic studies revealed that the oil kills micro-organisms with the deformation of cellular morphology on treatment of the oil. Thus, the essential oil of M. paniculata leaf can be an excellent alternative for development of new antimicrobials and anticancer chemotherapeutic agents for the pharmaceutical industries.

Integrated Genomic and Functional Characterization of the Anti-diabetic Potential of Arthrobacter sp. SW1.

For decades, bacterial natural products have served as valuable resources for developing novel drugs to treat several human diseases. Recent advancements in the integrative approach of using genomic and functional tools have proved beneficial in obtaining a comprehensive understanding of these biomolecules. This study presents an in-depth characterization of the anti-diabetic activity exhibited by a bacterial isolate SW1, isolated from an effluent treatment plant. As a primary screening, we assessed the isolate for its potential to inhibit alpha-amylase and alpha-glucosidase enzymes. Upon confirmation, we further utilized LC-MS, ESI-MS/MS, and NMR spectroscopy to identify and characterize the biomolecule. These efforts were coupled with the genomic assessment of the biosynthetic gene cluster involved in the anti-diabetic compound production. Our investigation discovered that the isolate SW1 inhibited both α-amylase and α-glucosidase activity. The chemical analysis suggested the production of acarbose, an anti-diabetic biomolecule, which was further confirmed by the presence of biosynthetic gene cluster "acb" in the genome. Our in-depth chemical characterization and genome mining approach revealed the potential of bacteria from an unconventional niche, an effluent treatment plant. To the best of our knowledge, it is one of the first few reports of acarbose production from the genus Arthrobacter.

Anticancer and antimicrobial compounds from Croton caudatus Gieseler and Eurya acuminata DC: Two edible plants used in the traditional medicine of the Kuki tribes.

Eurya acuminata DC and Croton caudatus Gieseler are two ethno-medicinal plants used by Kuki community of North East India. From these plants, we have characterized fifteen phytochemicals (1-15) by extensive use of chromatographic and spectroscopic methods. They were also tested for in vitro cytotoxic effects against A549 and MIAPACA2 cell lines and antimicrobial activities against Mycobacterium smegmatis and Candida albicans. All compounds showed moderate activity against the MIAPACA2 cell lines. Compounds tricosan-1-ol (6), octacosanoic acid (7), ß-sitosterol (10) and (E)-dodec-3-en-1-ol (14) exhibited promising activity against A549 cell lines with IC50 of 16.72, 4.5, 4.42 and 4.5 µg/ml respectively. Further, hexatriacontan-1-ol (2) exhibited lowest MIC of 50 µg/ml against C. Albicans and henicosan-1-ol (3) at 25 µg/ml against M. smegmatis. They were also screened through docking analysis against two Phosphatidylinositol-3-Kinase nodal proteins and three feedback loop proteins of cancers. Thus, this study validates their traditional uses as herbal anticancer and antimicrobial agents.

Chemical composition and antibacterial activity of essential oil from fruit of Micromelum integerrimum (Buch.-Ham. ex DC.) Wight & Arn. ex M. Roem.

The essential oil extracted from fruit of Micromelum integrrimum were evaluated through gas chromatography and gas chromatography-mass spectroscopy. 52 compounds were identified from the fruit oil representing 99.98% of the oil. The major components of the total fruit oil are monoterpene hydrocarbons (72.23%), oxygenated monoterpenes (14.78%) and sesquiterpene (11.54%) which were predominated by terpinolene (32.21%), α-pinene (17.24%), ß-pinene (17.24%), and camphene (4.05%). Moreover, other components that present in 1.45% were aromatic compounds, fatty acid, etc. The essential oil exhibited broad spectrum antimicrobial activity which is concentration dependent and 100 µL of the fruit oil showed the inhibition zones ranging from 7-16 mm. Fruit oil exhibited strong inhibition activity compared to standard anti-bacterial drug neomycin B (22 mm) against Bacillus subtilis MTCC 441 and Bacillus spizizenii ATCC 6633. This is the first hand report on the chemical profiles and promising anti-microbial activity of Micromelum integrrimum fruit essential oil towards Basillus Sp.