Background: Gonorrhea is a major sexually transmitted disease worldwide and for its control, effective treatment is essential. However as more strains of Neisseria gonorrhoeae continuously develop resistance to several drugs, this strategy obliges scientists to discover newer effective drugs. Objectives: To ascertain whether crude leaf and root extracts of Cassia alata (Caesalpiniaceae) have antimicrobial activity against clinically resistant Neisseria gonorrhoeae bacteria. To determine and compare the MICs of their ether and methanol extracts. Materials and methods: Ether and methanol extracts were prepared from the plant parts. 12-375mg/ml of serially diluted ether extracts in DMSO and methanol extracts in water were tested using agar-well diffusion method against Neisseria gonorrhea clinical isolate cultured on MTM agar. MICs were determined from corresponding concentration-response curves. Ceftriaxone was used as positive control, whereas DMSO and water as negative controls. Results: All the crude extracts showed concentration-dependent Neisseria gonorrhea inhibition. Ether extracts for both leaves and roots gave lower MICs compared to those of methanol. Ether root extract showed the highest potency. Conclusions: Both the leaf and the root of Cassia alata plant have activity against clinically resistant Neisseria gonorrhoeae; the root having the higher activity. Lipophilic solvent, ether, give more potent antigonorrhoeal extracts. As expected Cassia alata plant in Central Uganda also has antibacterial activity.
RESUMO: "Plantas tradicionalmente utilizadas contra malária: investigação fi toquímica e farmacológica de Momordica foetida". Folhas de Momordica foetida tradicionalmente usadas para tratar sintomas de malária em partes da África Oriental foram estudadas in vitro com respeito à sua atividade antimalárica. Utilizando-se o teste de incorporação de hipoxantina [ 3 H] a atividade antiplasmódica dos extratos hidrofílico e lipofílico contra a cepa sensíveis a cloroquina poW e o clone multiresistente Dd2 de Plasmodium falciparum foi determinada. O extrato éter de petróleo/ acetato de etila mostrou atividade signifi cativa com valores de CI 50 de 7,3 g/mL (poW) e 13,0 g/mL (Dd2). A citotoxicidade foi estimada em duas linhas de células humanas HepG2 e ECV-304 e o índice de seletividade (IS) foi calculado, variando entre 12 e 15. A análise fi toquímica levou ao isolamento de um número de glicosídeos fenólicos, por exemplo eriodictiol-, 5,7,4'-triidroxifl avanona, kaempferol e 5,7-diidroxicromona-7-O-ß-D-glicopiranosideo, descritos pela primeira vez de M. foetida. Na tentativa de provar um possível modo de ação foi avaliada a infl uência dos extratos brutos bem como dos compostos isolados sobre a degradação da heme usando-se cloroquina como composto de referência. O extrato acetato de etila mostrou inibição da degradação da heme em torno de 88%, bastante similar a cloroquina (84%) e também o eriodictiol-7-O-ß-D-glicopiranosideo (2) inibiu a degradação da heme em 86%. Unitermos:Momordica foetida, Cucurbitaceae, glicosídeos de fl avonóides, teste de GSH-haemin, malária, medicina tradicional. ABSTRACT:Leaves from Momordica foetida traditionally used to treat symptoms of malaria in parts of East Africa were studied for in vitro antimalarial activity. Using an [ 3 H] hypoxanthineincorporation assay the antiplasmodial activity of hydrophilic and lipophilic extracts against the chloroquine-sensitive strain poW and the multiresistant clone Dd2 of Plasmodium falciparum was determined. The petrol ether/ethyl acetate extract showed signifi cant activity with IC 50 values of 7.3 g/mL (poW) and 13.0 g/mL (Dd2). Cytotoxicity was estimated on two human cell lines HepG2 and ECV-304 and a selectivity index (SI) was calculated, ranging between 12 and 15. Phytochemical analysis led to the isolation of a number of phenolic glycosides, e.g. eriodictyol-, 5,7,4'-trihydroxyfl avanone-, kaempferol-and 5,7-dihydroxychromone-7-O-ß-D-glucopyranoside, not previously known from M. foetida. In order to prove one possible mode of action the infl uence of the crude extracts as well as the isolated compounds on the heme degradation with chloroquine as reference compound was evaluated. The ethyl acetate extract showed about 88% inhibition of heme degradation, quite similar to chloroquine (84 %), and also eriodictyol-7-O-ß-D-glucopyranoside (2) inhibited heme degradation by 86 %.
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