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1.
Adv Pharm Bull ; 11(3): 543-556, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-34513630

RESUMEN

Purpose: Biosurfactants are applied in drug formulations to improve drug solubility and in some cases, treat diseases. This study is focused on generating, extracting, purifying and then characterizing biosurfactants from bacterial isolates of palm oil wastes and abattoir soil origins. Methods: Eight bacteria were isolated from the soil and sludge samples, out of which four (50%) were found to produce biosurfactants. Bacillus subtilis (37.5%) and Pseudomonas aeruginosa (50%) were isolated and identified from these samples using mineral salt medium, nutrient agar and Cetrimide agar. Mutant isolates of B. subtilis BS3 and P. aeruginosa PS2 were used to produce biosurfactants using mineral salt medium as enrichment medium and extraction was done using membrane filter. Results: The mutant strains B. subtilis BS3 and P. aeruginosa PS2 generated biosurfactants that displayed significant solubility and dissolution properties by enhancing the percentage solubility of piroxicam to 62.86 and 54.29% respectively, and achieved 51.71 and 48.71% dissolution of the drug in 0.1N HCl. Conclusion: From the results obtained, the produced biosurfactants could serve as a better alternative to conventional surfactants. Notably, the study indicated that the biosurfactant produced by mutant strain of B. subtilis produced more potent activities (surface tension reduction ability, high emulsification) than those of P. aeruginosa.

2.
Biochem Biophys Res Commun ; 308(4): 736-43, 2003 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-12927780

RESUMEN

Major blood stage antimalarial drugs like chloroquine and artemisinin target the heme detoxification process of the malaria parasite. Hemozoin formation reactions in vitro using the Plasmodium falciparum histidine-rich protein-2 (Pfhrp-2), lipids, and auto-catalysis are slow and could not explain the speed of detoxification needed for parasite survival. Here, we show that malarial hemozoin formation is a coordinated two component process involving both lipids and histidine-rich proteins. Hemozoin formation efficiency in vitro is 1-2% with Pfhrp-2 and 0.25-0.5% with lipids. We added lipids after 9h in a 12h Pfhrp-2 mediated reaction that resulted in sixfold increase in hemozoin formation. However, a lipid mediated reaction in which Pfhrp-2 was added after 9h produced only twofold increase in hemozoin production compared to the reaction with Pfhrp-2 alone. Synthetic peptides corresponding to the Pfhrp-2 heme binding sequences, based on repeats of AHHAAD, neither alone nor in combination with lipids were able to generate hemozoin in vitro. These results indicate that hemozoin formation in malaria parasite involves both the lipids and the scaffolding proteins. Histidine-rich proteins might facilitate hemozoin formation by binding with a large number of heme molecules, and facilitating the dimer formation involving iron-carboxylate bond between two heme molecules, and lipids may then subsequently assist the mechanism of long chain formation, held together by hydrogen bonds or through extensive networking of hydrogen bonds.


Asunto(s)
Antimaláricos/farmacología , Hemoproteínas/química , Malaria/metabolismo , Proteínas/química , Acetona/química , Animales , Catálisis , Cristalografía por Rayos X , Dimerización , Histidina/química , Enlace de Hidrógeno , Metabolismo de los Lípidos , Lípidos/química , Masculino , Ratones , Péptidos/química , Plasmodium falciparum/metabolismo , Unión Proteica , Proteínas/metabolismo , Proteínas Recombinantes/química , Factores de Tiempo
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