Phytochemical Characterization, Antioxidant and Anti-Proliferative Properties of Rubia cordifolia L. Extracts Prepared with Improved Extraction Conditions

none11sìRubia cordifolia L. (Rubiaceae) is an important plant in Indian and Chinese medical systems. Extracts prepared from the root, stem and leaf have been used traditionally for the management of various diseases. Some of the known effects are anti-inflammation, neuroprotection, anti-proliferation, immunomodulation and anti-tumor. A comparative account of the extracts derived from different organs that lead to the identification of the most suitable solvent is lacking. We explored the presence of phytochemicals, antioxidant activity and anti-proliferative properties of a variety of solvent-based extracts of root, and methanol extracts of stem and leaf of R. cordifolia L. The antioxidant potential was determined by DPPH, hydrogen peroxide, nitric oxide and total antioxidant assays. The anti-proliferative nature was evaluated by MTT assay on HeLa, ME-180 and HepG2 cells. The composition of the extracts was determined by UPLC-UV-MS. We found that the root extracts had the presence of higher amounts of antioxidants over the stem and leaf extracts. The root extracts prepared in methanol exhibited the highest cytotoxicity in HepG2 cells. The main compounds identified through UPLC-UV-MS of the methanol extract give credibility to the previous results. Our comprehensive study corroborates the preference given to the root over the stem and leaf for extract preparation. In conclusion, we identified the methanol extract of the root to be the most suited to have bioactivity with anti-cancer potential.Humbare, Ravikiran B; Sarkar, Joyita; Kulkarni, Anjali A; Juwale, Mugdha G; Deshmukh, Sushil H; Amalnerkar, Dinesh; Chaskar, Manohar; Albertini, Maria C; Rocchi, Marco B L; Kamble, Swapnil C; Ramakrishna, SeeramHumbare, Ravikiran B; Sarkar, Joyita; Kulkarni, Anjali A; Juwale, Mugdha G; Deshmukh, Sushil H; Amalnerkar, Dinesh; Chaskar, Manohar; Albertini, Maria C; Rocchi, Marco B L; Kamble, Swapnil C; Ramakrishna, Seera

Naphthoquinones and Their Derivatives: Emerging Trends in Combating Microbial Pathogens

In the current era, an ever-emerging threat of multidrug-resistant (MDR) pathogens pose serious health challenges to mankind. Researchers are uninterruptedly putting their efforts to design and develop alternative, innovative strategies to tackle the antibiotic resistance displayed by varied pathogens. Among several naturally derived and chemically synthesized compounds, quinones have achieved a distinct position to defeat microbial pathogens. This review unleashes the structural diversity and promising biological activities of naphthoquinones (NQs) and their derivatives documented in the past two decades. Further, realizing their functional potentialities, researchers were encouraged to approach NQs as lead molecules. We have retrieved information that is dedicated on biological applications (antibacterial, antifungal, antiparasitic) of NQs. The multiple roles of NQs offer them a promising armory to combat microbial pathogens including MDR and the ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) group. In bacteria, NQs may exhibit their function in the following ways (1) plasmid curing, (2) inhibiting efflux pumps (EPs), (3) generating reactive oxygen species (ROS), (4) the inhibition of topoisomerase activity. Sparse but meticulous literature suggests the mechanistic roles of NQs. We have highlighted the possible mechanisms of NQs and how the targeted drug synthesis can be achieved via molecular docking analysis. This bioinformatics-oriented approach will explicitly lead to the development of effective and most potent drugs against targeted pathogens. The mechanistic approaches of emerging molecules like NQs might prove a milestone to defeat the battle against microbial pathogens

ProHSO4: An efficient catalyst for solvent-free synthesis of bis(indolyl)methanes and their in silico screening for potential biological activity

A simple, mild, and efficient protocol has been developed for the synthesis of 3,3′-bis(indolyl)methanes (BIMs) using prolinium hydrogen sulfate (ProHSO4) as a catalyst under solvent-free and support-free conditions. This mechanochemical method undergoes electrophilic substitution reaction of indole with diverse aldehydes to afford the desired BIMs in high yields at room temperature. Due to diverse pharmacological utility, the synthesized BIMs were subjected to in silico studies. The structure activity analysis of BIMs revealed their ability to bind Eg5 kinesin, Human p38 α MAP Kinase, and Human 3 alpha HSD type 3 as a potential protein target for anticancer activity. The compounds exhibited higher binding affinities with Eg5 kinesin having hydrophobic interactions with α2, α3 helices and loop5 amino acid residues. Moreover, molecular docking with Human p38 α MAP Kinase protein depicted compounds as ATP-competitive molecules interacting with hydrophobic region I, II and allosteric DFG motif. A total of 13 derivatives were synthesized and subjected for in silico screening for predicting potential biological activity. Among them, 3b, 3d, 3f, 3 g, 3i, 3j, and 3 k compounds were identified as potential inhibitors of Eg5 kinesin, Human p38 α MAP Kinase, and Human 3 alpha HSD type 3, and their evaluation in the biological experimental system is warranted

Sustainable Agriculture through Multidisciplinary Seed Nanopriming: Prospects of Opportunities and Challenges

The global community decided in 2015 to improve people's lives by 2030 by setting 17 global goals for sustainable development. The second goal of this community was to end hunger. Plant seeds are an essential input in agriculture; however, during their developmental stages, seeds can be negatively affected by environmental stresses, which can adversely affect seed vigor, seedling establishment, and crop production. Seeds resistant to high salinity, droughts and climate change can result in higher crop yield. The major findings suggested in this review refer nanopriming as an emerging seed technology towards sustainable food amid growing demand with the increasing world population. This novel growing technology could influence the crop yield and ensure the quality and safety of seeds, in a sustainable way. When nanoprimed seeds are germinated, they undergo a series of synergistic events as a result of enhanced metabolism: modulating biochemical signaling pathways, trigger hormone secretion, reduce reactive oxygen species leading to improved disease resistance. In addition to providing an overview of the challenges and limitations of seed nanopriming technology, this review also describes some of the emerging nano-seed priming methods for sustainable agriculture, and other technological developments using cold plasma technology and machine learning