IN VITRO ANTIBACTERIAL ACTIVITY AND GAS CHROMATOGRAPHY-MASS SPECTROMETRY ANALYSIS OF ETHANOLIC EXTRACT OF LEAVES OF ELETTARIA CARDAMOMUM L. MATON

Objective: The objective of the present study is to determine the possible phytoconstituents identified by gas chromatography and mass spectrometry (GC-MS) analysis of an ethanolic leaves extract of Elettaria cardamomum L. Maton.Methods: The extraction of E. cardamomum was done by cold solvent extraction system at room temperature. GC-MS analysis of lyophilized ethanolic leaves extract of plant samples was carried out by GC-MS-GC Clarus 500 Perkin Elmer. Results: In E. cardamomum, 21 phytochemicals were identified among which retinal, 9-cis-showed the highest area (44.86%) and benzeneethanamine, α-methyl- showed the lowest area (0.12%). The major compounds identified were retinal, 9-cis-, 1-heptatriacotanol, phytol, n-hexadecanoic acid, naphthalene,decahydro-1,1,4atrimethyl-6-methylene-5-(3-methyl-2-4-pentadienyl)-[4aS-(4aα,5α,8aα)]-, β-pinene, 2H-pytan-3-ol,6- ethenyltetrahydro-2,2,6-trimethyl-and cyclopropane, trimethanol, (2-methyl-1-propanylidene).Conclusion: GC-MS analysis revealed the presence of hydrocarbon alkane, ester, terpenes, phenolic compounds, steroids, and fatty acids in E. cardamomum. These active phytoconstituents contribute to the medicinal efficacy of the plant, and the plant can be used for the sourcing of these compounds

Naturally Isolated Pyridine Compounds Having Pharmaceutical Applications

Heterocyclic moieties form important constituents of biologically active natural products and synthetic compounds of medicinal interest. Nitrogen heterocycles constitute important pharmacophores in drug design, especially pyridine derivatives, which are among the most frequently cited heterocyclic compounds. The isolated as well as synthesized pyridine compounds exhibited various pharmacological properties due to their diverse physiochemical properties like water solubility, weak basicity, chemical stability, hydrogen bond-forming ability, protein-binding capacity, cell permeability, and size of the molecules attracted the attention of medicinal chemists for the past few years. Their interesting molecular architecture seeks attention to isolate derivatives of medicinal interest from natural source. In this chapter, we plan to describe the isolated natural products having pyridine moiety and their pharmacological importance

Diethyl 1,1-dioxo-3,5-bis­(pyridin-2-yl)-1λ6,4-thio­morpholine-2,6-dicarbox­ylate

The title compound, C20H23N3O6S, crystallizes with two crystallographically independent mol­ecules in the asymmetric unit. The thio­morpholine ring in both mol­ecules adopts a chair conformation. The crystal structure is stabilized by C—H⋯O inter­actions. The amino groups are shielded and, as a result, these groups are not involved in hydrogen bonding

Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells

© 2018 Elsevier Ltd Expression of cytochrome P450-1A1 (CYP1A1) is suppressed under physiologic conditions but is induced (a) by polycyclic aromatic hydrocarbons (PAHs) which can be metabolized by CYP1A1 to carcinogens, and (b) in majority of breast cancers. Hence, phytochemicals or dietary flavonoids, if identified as CYP1A1 inhibitors, may help in preventing PAH-mediated carcinogenesis and breast cancer. Herein, we have investigated the cancer chemopreventive potential of a flavonoid-rich Indian medicinal plant, Pongamia pinnata (L.) Pierre. Methanolic extract of its seeds inhibits CYP1A1 in CYP1A1-overexpressing normal human HEK293 cells, with IC50 of 0.6 µg/mL. Its secondary metabolites, the furanoflavonoids pongapin/lanceolatin B, inhibit CYP1A1 with IC50 of 20 nM. Although the furanochalcone pongamol inhibits CYP1A1 with IC50 of only 4.4 µM, a semisynthetic pyrazole-derivative P5b, has ∼10-fold improved potency (IC50, 0.49 μM). Pongapin/lanceolatin B and the methanolic extract of P. pinnata seeds protect CYP1A1-overexpressing HEK293 cells from B[a]P-mediated toxicity. Remarkably, they also block the cell cycle of CYP1A1-overexpressing MCF-7 breast cancer cells, at the G0-G1 phase, repress cyclin D1 levels and induce cellular-senescence. Molecular modeling studies demonstrate the interaction pattern of pongapin/lanceolatin B with CYP1A1. The results strongly indicate the potential of methanolic seed-extract and pongapin/lanceolatin B for further development as cancer chemopreventive agents