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1.
Acta Parasitol ; 67(2): 640-647, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35380401

RESUMO

PURPOSE: Leishmaniasis is a major public health problem worldwide in many parts of the world. Current anti-leishmanial drugs have only limited clinical efficacy. Aurothiomalate derivatives are useful for treating rheumatoid arthritis, but have emerged as a promising therapeutic candidate for leishmaniasis. This paper gives a review of the literature about the usefulness of aurothiomalate derivatives against leishmaniasis. METHODS: In this study, we reviewed the proposed mechanisms of action of aurothiomalate and related compounds on the metabolism of L. major and collected data by searching relevant articles. RESULTS: Aurothiomalate-based drugs could be effective against leishmaniasis through two direct and indirect mechanisms: first, cytotoxic effects on parasites via thiomalate's false substrate role in the citric acid cycle against malate; and second, immunosuppressive and anti-inflammatory effects of aurothiomalate derivatives with prostaglandin production inhibitory effects. CONCLUSIONS: The current study documented that aurothiomalate-based drugs could be effective against leishmaniasis through two direct and indirect mechanisms of action. Gold thiomalate as a promising hit should be evaluated against L. major in vitro and in vivo conditions in the future.


Assuntos
Leishmania major , Leishmaniose , Tiomalato Sódico de Ouro/metabolismo , Tiomalato Sódico de Ouro/farmacologia , Tiomalato Sódico de Ouro/uso terapêutico , Humanos , Leishmaniose/tratamento farmacológico
2.
Medicines (Basel) ; 5(1)2018 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-29301240

RESUMO

Background: The serum glucose lowering, normalization animal body weight, and antioxidative stress effects of Mespilus germanica L. leaf extract were investigated in normal and streptozotocin-induced Balb/C mice. Methods: The phenol and flavonoid of the leaves of M. germanica were extracted by percolation and concentrated using a rotary evaporator. Its total phenol and flavonoid content was determined using folin and aluminum chloride methods, respectively. The study was conducted on 48 matured male Balb/C mice (20-30 g) divided into 6 groups (n = 8). Diabetes mellitus was induced by single intraperitoneal injection of 35 mg/kg of streptozotocin (STZ). Extracts of Mespilus germanica were used orally at the dose of 50, 100, and 200 mg/kg body weight per day for 21 days. Results: Oral administrations of the M. germanica L. leaf extract significantly decreased serum glucose, oxidative stress, and lipid peroxidation and maintained animal body weight during treatment period (p < 0.05) compared to metformin (200 mg/kg) in over 100 mg/kg, 200 mg/kg, and 50 mg/kg dosages, respectively. Conclusions: The present study indicated that the Mespilus germanica leaf extract significantly decreased serum glucose and maintained normal body weight in Balb/C diabetic mice.

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