Synthesis and antimycobacterial activity of highly functionalized tetrahydro-4(1H)-pyridinones

A series of 35 2e,3e,6e-triaryltetrahydro-4(1H)-pyridinones, 2e,3e,5e,6e-tetraaryltetrahydro-4(1H)-pyridinones and their N-nitroso and N-cyano analogs have been prepared. All these 35 compounds obtained were screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB). Among them, the N-nitrosopyridinones are found to be more active against MTB than the corresponding N-CN analogs, which, in turn, were slightly more active than NH analogs. In particular, the N-nitroso compounds, 3d, 4b and 4e with halogen-bearing phenyl rings at 2,6-positions showed maximum activity with MIC values of 3.97, 3.11 and 3.11 μM, being more efficacious than the first line anti-TB drugs, ciprofloxacin, ethambutol and pyrazinamide. A general trend has also been discerned in all the three classes of NH, N-CN and N-NO compounds, in each of which those bearing four aryl rings display higher activity than that having three analogously substituted aryl rings disclosing that lipophilicity could be an important factor underlying antimycobacterial activity.     

Molecular markers linked with bruchid resistance in Vigna radiata var. Sublobata and their validation

Bruchid, Callosobruchus chinensis (L.) is an important pest of Vigna radiata during storage. RFLP and PCR based markers identified, linked with bruchid resistance gene in wild accession of greengram (V. radiata var. Sublobata) either collected from Madagaskar or Australia. Whether these markers will be useful for marker assisted introgression of bruchid resistance gene from the Indian accession into the existing cultivars are not known. Here, we employed two STS based markers which were found earlier, to be linked with bruchid resistance gene in Australian accession ACC41. Only one primer pair, STSbr1 showed polymorphism among Indian Sublobata accession (Sub2) and other twelve green gram cultivars. Analysis of 113 segregating lines (F₆) of a cross between a popular cultivar of West Bengal, B1 and Sub2 showed a cent percent co-segregation of resistant locus with the polymorphic fragment. STSbr1 behave as a dominant marker among Indian genotypes although it has been shown earlier a co-dominant banding pattern between ACC41 and other Australian Susceptible cultivars. Other STS marker, STSbr2, does not produce any polymorphic fragment among Sub2 and 18 greengram genotypes. STSbr1 employed in screening of 50 green gram accessions and found high efficiency in screening of bruchid resistant genotypes also. So STSbr1 will be useful for marker assisted selection and germplasm screening for development of bruchid resistant greengram.     

Production Enhancement of an Anticoagulant Trypsin Inhibitor from Oceanimonas sp. BPMS22 and Its Anti-cancer Activity

International Journal of Peptide Research and Therapeutics - The significant role of proteases in the cancer progression exposed them as potential targets for drug discovery. Regulating protease...     

A trypsin and chymotrypsin inhibitor from Caesalpinia bonduc seeds: isolation, partial characterization and insecticidal properties.

Evolution of proteinase inhibitor diversity in leguminous plants of tropical rainforests is under immense pressure from the regular upregulation of proteolytic machinery of their pests. The present study illustrates the isolation and bioinsecticidal potency of a serine proteinase inhibitor from the seeds of Caesalpinia bonduc (CbTI), inhabiting Great Nicobar Island, India. Following initial fractionation by ammonium sulfate precipitation, CbTI was purified to homogeneity by ion exchange, gel filtration and trypsin affinity chromatography. SDS-PAGE of gel filtrated CbTI showed a couple of proteins CbTI-1 ( approximately 16kDa) and CbTI-2 (20kDa) under non-reducing conditions, which subsequent to trypsin affinity chromatography yielded only CbTI-2. Both Native PAGE as well as iso-electric focusing showed 2 iso-inhibitors of CbTI-2 (pI values of 5.35 and 4.6). CbTI exhibited tolerance to extremes of temperatures (0-60 degrees C) and pH (1-12). A 1:1 stoichiometric ratio was noted during CbTI-2-trypsin complex formation, which was absent on binding with chymotrypsin. Further, SDS-PAGE analysis also showed that CbTI-1 has affinity only towards chymotrypsin, whereas both trypsin and chymotrypsin formed complexes with CbTI-2. Dixon plot analysis of CbTI-2 yielded inhibition constants (K(i)) of 2.75 x 10(-10)M and 0.95 x 10(-10)M against trypsin and chymotrypsin activity respectively. Preliminary investigations on the toxicological nature of CbTI revealed it to be a promising bioinsecticidal candidate.     

Sujiol, a new potent insect growth regulator from Juniperus communis L. against last instar larvae of Spodoptera litura

Sujiol, a terpenoid isolated from the berries of Juniperus communis , exhibited growth regulating activity in the last instar larvae of Spodoptera litura. The larvae were treated with 0.1, 0.25, 0.5, 0.75, 1, 2 and 4% concentrations of Sujiol, in solvent acetone. Formation of non-viable adults, interference in ecdysis and development of mosaics were the important morphogenetic peculiarities observed. The resultant forms were ruled out from further development and reproduction.