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Natural Products Structures and Analysis of the Cerrado Flora in Goiás
Published in Luzia Valentina Modolo, Mary Ann Foglio, Brazilian Medicinal Plants, 2019
Lucilia Kato, Vanessa Gisele Pasqualotto Severino, Aristônio Magalhães Teles, Aline Pereira Moraes, Vinicius Galvão Wakui, Núbia Alves Mariano Teixeira Pires Gomides, Rita de Cássia Lemos Lima, Cecilia Maria Alves de Oliveira
The β-carboline alkaloids from P. prunifolia and from Rubiaceae and Apocynaceae species have been assayed against inhibitors of malate synthase, an important enzyme from Paracoccidioides spp. (PbMSL) (Costa et al., 2015). The β-carboline alkaloids are crucial for stability in the binding pocket of PbMSL and were chosen as candidate molecules after virtual screening and molecular docking studies were obtained through studies of receptor-ligand interactions. In addition, the alkaloids 29, 30, 31 and 21 (Figure 11.10) were assayed and the alkaloids 29 and 30 showed no cytotoxicity in A549 and MRC5 cells. This result is concomitant with bioassays described by Costa et al. (2015) where alkaloid 29, isolated from Galianthe ramosa E.L. Cabral (Freitas et al., 2014), another Rubiaceae species, is a good candidate for antifungal development.
Drug targets in dormant Mycobacterium tuberculosis: can the conquest against tuberculosis become a reality?
Published in Infectious Diseases, 2018
Vivek Kumar Gupta, M. Madhan Kumar, Dharmendra Singh, Deepa Bisht, Shweta Sharma
Dormant bacilli face depletion of oxygen and nutrients which are the main factors responsible for NRP stage of Mtb. The stress environment causes a massive metabolic shunt and down regulates tricarboxylic acid (TCA) cycle enzymes [21]. In this carbon deficient environment, Mtb cannot use TCA cycle for generation of energy. So, at this stage carbon conserving glyoxylate cycle is up regulated in order to continue generating energy from an alternative carbon source namely lipids. The ICL is a glyoxylate cycle enzyme which converts isocitrate to succinate and glyoxylate, followed by the addition of acetyl-CoA to glyoxylate to form malate by malate synthase. ICL plays an important role in the survival of latent Mtb during chronic stage of infection [22]. The glyoxylate pathway is absent in host and has been identified as potential and selective drug target in dormant bacilli.