Abstract
Objectives. To evaluate the in vitro leishmanicidal activity of nine flavonoid derivatives from Delphinium staphisagria against L. infantum and L. braziliensis. Design and Methods. The in vitro activity of compounds 1–9 was assayed on extracellular promastigote and axenic amastigote forms and on intracellular amastigote forms of the parasites. Infectivity and cytotoxicity tests were carried on J774.2 macrophage cells using Glucantime as the reference drug. The mechanisms of action were analysed performing metabolite excretion and transmission electronic microscope ultrastructural alteration studies. Results. Nine flavonoids showed leishmanicidal activity against promastigote as well as amastigote forms of Leishmania infantum and L. braziliensis. These compounds were nontoxic to mammalian cells and were effective at similar concentrations up to or lower than that of the reference drug (Glucantime). The results showed that 2″-acetylpetiolaroside (compound 8) was clearly the most active. Conclusion. This study has demonstrated that flavonoid derivatives are active against L. infantum and L. braziliensis.
Highlights
Leishmaniasis is an infection caused by different species of the protozoan genus Leishmania, which is transmitted by dipterans of the genera Phlebotomus in the Old World and Lutzomyia in the New World
Drug treatment for leishmaniasis has been available since the beginning of the 20th Century [1], but only a few drugs have been developed for use and there are numerous drawbacks to each of the treatments
L. infantum (MCAN/ES/ 2001/UCM-10) and L. braziliensis (MHOM/BR/1975/ M2904) were cultivated in vitro in trypanosomes liquid medium (MTL) with 10% inactive fetal bovine serum and were kept in an air atmosphere at 28◦C, in Roux flasks (Corning, USA) with a surface area of 75 cm2, according to the methodology described by Gonzalez et al [4]
Summary
Leishmaniasis is an infection caused by different species of the protozoan genus Leishmania, which is transmitted by dipterans of the genera Phlebotomus in the Old World and Lutzomyia in the New World.Leishmaniasis represents one of the most significant of a collection of neglected tropical diseases. Two pentavalent antimonials are available (meglumine antimoniate or Glucantime and sodium stibogluconate or pentostan), but they have common side effects such as anorexia, vomiting, nausea, abdominal pain, malaise, and myalgia. They are available in several formulations, which are administered by intravenous infusion, including liposomal amphotericin B, amphotericin B lipid complex, and amphotericin B colloidal dispersion. The alkyl phospholipid (hexadecylphosphocholine), commonly known as miltefosine, induces gastrointestinal side effects such as anorexia, nausea, vomiting (38%) and diarrhea (20%), and skin allergies, elevated hepatic transaminase concentrations, and, occasionally, renal failure It is used in combination with different classes of azole oral antifungal agents including ketoconazole, fluconazole, and itraconazole
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
