@article {46625,
	title = {Approach to nigericin derivatives and their therapeutic potential},
	journal = {RSC Advances},
	volume = {10},
	year = {2020},
	month = {NOV },
	pages = {43085-43091},
	type = {Article},
	abstract = {<p>A new nigericin analogue that has been chemically modified was synthesized through a fluorination process from the parent nigericin, produced from a novel Streptomyces strain DASNCL-29. Fermentation strategies were designed for the optimised production of nigericin molecule and subjected for purification and structural analysis. The fermentation process resulted in the highest yield of nigericin (33\% (w/w)). Initially, nigericin produced from the strain DASNCL-29 demonstrated polymorphism in its crystal structure, i.e., monoclinic and orthorhombic crystal lattices when crystallised with methanol and hexane, respectively. Furthermore, nigericin produced has been subjected to chemical modification by fluorination to enhance its efficacy. Two fluorinated analogues revealed that they possess a very potent antibacterial activity against Gram positive and Gram negative bacteria. To date, the nigericin molecule has not been reported for any reaction against Gram-negative bacteria, which are increasingly becoming resistant to antibiotics. For the first time, fluorinated analogues of nigericin have shown promising activity. In vitro cytotoxicity analysis of fluorinated analogues demonstrated tenfold lesser toxicity than the parent nigericin. This is the first type of study where the fluorinated analogues of nigericin showed very encouraging activity against Gram-negative organisms; moreover, they can be used as a candidate for treating many serious infections.</p>
},
	doi = {10.1039/d0ra05137c},
	author = {Sahu, Amit Kumar and Said, Madhukar S. and Hingamire, Tejashri and Gaur, Megha and Khan, Abujunaid and Shanmugam, Dhanasekaran and Barvkar, Vitthal T. and Dharne, Mahesh S. and Bharde, Atul A. and Dastager, Syed G.}
}
@article {48993,
	title = {Antimalarial activity of anacardium occidentale leaf extracts against plasmodium falciparum transketolase (PfTK)},
	journal = {Acta Parasitologica},
	volume = {68},
	year = {2023},
	month = {DEC},
	pages = {832-841},
	type = {Article},
	abstract = {<p>
	BackgroundAs per estimates by WHO in 2021 almost half of the world{\textquoteright}s population was at risk of malaria and \&gt; 0.6 million deaths were attributed to malaria. Therefore, the present study was aimed to explore the antimalarial activity of extracts derived from the leaves of the plant Anacardium occidentale L., which has been used traditionally for the treatment of malaria. Different extracts of A.occidentale leaves were prepared and tested for their inhibitory activity against recombinant P. falciparum transketolase (rPfTK) enzyme, in vitro. Further, growth inhibitory activity against cultivated blood stage P. falciparum parasites (3D7 strain), was studied using SYBR Green fluorescence-based in vitro assays. Acute toxicity of the hydro alcoholic extracts of leaves of A. occidentale (HELA) at different concentrations was evaluated on mice and Zebra fish embryos. HELA showed 75.45 +/- 0.35\% inhibitory activity against the recombinant PfTk and 99.31 +/- 0.08\% growth inhibition against intra-erythrocytic stages of P. falciparum at the maximum concentration (50 mu g/ml) with IC50 of 4.17 +/- 0.22 mu g/ml. The toxicity test results showed that the heartbeat, somite formation, tail detachment and hatching of embryos were not affected when Zebra fish embryos were treated with 0.1 to 10 mu g/ml of the extract. However, at higher concentrations of the extract, at 48 h (1000 mu g/ml) and 96 h (100 mu g/ml and 1000 mu g/ml, respectively) there was no heartbeat in the fish embryos. In the acute oral toxicity tests performed on mice, the extract showed no toxicity up to 300 mg/kg body weight in mice.ConclusionThe hydro-alcoholic extract of leaves of A. occidentale L. showed potent antimalarial activity against blood stage P. falciparum. Based on the observed inhibitory activity on the transketolase enzyme of P. falciparum it is likely that this enzyme is the target for the development of bioactive molecules present in the plant extracts. The promising anti-malarial activity of purified compounds from leaves of A. occidentale needs to be further explored for development of new anti-malarial therapy.</p>
},
	keywords = {Anacardium occidentale L, Antimalarial activity, malaria, Plasmodium falciparum, Transketolase},
	issn = {1230-2821},
	doi = {10.1007/s11686-023-00718-6},
	author = {Kaushik, Meenakshi and Hoti, Sugeerappa L. and Saxena, Jitendra Kumar and Hingamire, Tejashri and Shanmugam, Dhanasekaran and Joshi, Rajesh K. and Metgud, Sharada C. and Ungar, Banappa and Singh, Ishwar and Hegde, Harsha V.}
}
