Phytochemical screening and antimicrobial activity of Picrorrhiza kurroa, an Indian traditional plant used to treat chronic diarrhea

Phytochemical screening of the rhizomes of Picrorrhiza kurroa Benth revealed the presence of some bioactive components, which have been linked to antimicrobial properties. Various chemical tests and TLC studies showed the presence of glycosides, sterols and phenolic compounds when tested on different extracts of P. kurroa rhizomes. The major chemical constituents found in this plant were iridoid glycosides and cucurbitacins (triterpenoids) present in the methanolic extract. The effects of methanolic and aqueous extracts on some pathogenic bacterial and fungal strains viz.: Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Micrococcus luteus, Escherichia coli and Candida albicans, Aspergillus niger, respectively, showed that the plant part can be used to treat infections caused by these bacteria and fungi. The aqueous and methanolic extracts showed antibacterial activity but the significant antimicrobial activity was shown by methanolic extract only, against P. aeruginosa and S. aureus; while moderate activity against E. coli, B. subtilis and M. luteus. The effectiveness of the crude extract confirmed its use in traditional medicine to treat skin, urinary tract, diarrheal infections and gastrointestinal infections. The aqueous extract was less effective against the microbial strains and no activity against fungal strains. The MICs of the methanolic extract against the test bacteria were high and correlate with sensitivity test results. The effectiveness of the extracts was less than the conventional antibiotic, ciprofloxacin. Further the HPTLC studies were performed to estimate the content of iridoids and it was found to be 3.66 ± 0.11 and 4.44 ± 0.02 for picroside I and kutkoside, respectively

Targeting matrix metalloproteinases with novel diazepine substituted cinnamic acid derivatives: design, synthesis, in vitro and in silico studies

Abstract Lung cancer is the notable cause of cancer associated deaths worldwide. Recent studies revealed that the expression of matrix metalloproteinases (MMPs) is extremely high in lung tumors compared with non-malignant lung tissue. MMPs (-2 and -9) play an important part in tumor development and angiogenesis, which suggests that creating potent MMP-2 and -9 inhibitors, should be an important goal in lung cancer therapy. In the present study, an effort has been made to develop new anti-metastatic and anti-invasive agents, wherein a series of novel diazepine substituted cinnamic acid derivatives were designed, synthesized and assayed for their inhibitory activities on MMP-2 and MMP-9. These derivatives were prepared via microwave assisted reaction of tert-butyl (3-cinnamamidopropyl)carbamate derivatives mixed with 2,3-dibromopropanoic acid and potassium carbonate was added to obtain 4-(tert-butoxycarbonyl)-1-cinnamoyl-1,4-diazepane-2-carboxylic acid derivatives. The newly synthesized compounds were characterized by IR, NMR and mass spectroscopy. All the tested compounds showed good to excellent cytotoxic potential against A549 human lung cancer cells. The active compounds displaying good activity were further examined for the inhibitory activity against MMPs (-2 and -9). In addition, the structure and anticancer activity relationship were further supported by in silico docking studies of the active compounds against MMP-2 and MMP-9