AELCe showed a moderate bacteriostatic activity and promoted an immunomodulatory status through higher production of Th1 cytokines, nitric oxide release and T CD8 lymphocytes stimulation.
Background:
Leishmaniasis, a still important public health problem, exhibits environmental risk factors such as
massive migrations, urbanization, and deforestation. WHO research for Leishmaniasis has been mainly focused on the development
of new tools, such as diagnostic tests, drugs, and vaccines. During the drug development strategy, only a few
compounds seem promising and call for further study after the in vitro and in vivo preclinical tests.
Objective:
In this review, our group aimed to highlight the utmost research done during 2014 to 2019 in the fields of natural
and synthetic compounds, as well as repurposed drugs and new formulations tested in vivo for Leishmania spp.
Method:
Based on the literature search, we used the databases MEDLINE, PUBMED, CAPES PERIODIC and ELSEVIER
to delineate an interval of the last 5 years of research on each field.
Results:
Among the natural compounds tested, allicin and a fraction of potato tuber extract showed the most promising antileishmanial
activity. Concerning synthetic compounds, quinolines, bornyl ester, thymol, benzoxaborole and nitroimidazole
derivatives exhibited encouraging results. Moreover, repositioned alternatives involved combinations with known drugs and
monotherapy protocols as well. In these years, new formulations were widely assessed as drug delivery systems, such as nanoparticles,
micelles and liposomes in polymer conjugations.
Conclusion:
Drug repurposing and new formulations of already-known drugs are worthwhile approaches to promptly introduce
new treatment schemes to Leishmaniasis. Nevertheless, the interest in new synthetic compounds and new formulations
brings light to new treatment proposals and are notable lines of research.
<i>Rhipsalis baccifera</i> (Sol.) Stearn is a typical cactus from tropical regions with wide geographic distribution, and its therapeutic potential is not yet fully understood, such as antitumoral property. Thus, this study evaluated the cytotoxic ethanolic extract of <i>R. baccifera</i> (EERB) and its antitumor activity against Erlich's tumor in mice. The EERB was obtained, and its phytochemical profile was filed by thin-layer chromatography. The toxicity was evaluated in vitro and in vivo using the microcrustacean<i> Artemia salina</i> Leach and mice. The lethal dose was determined after implantation of a tumor cell suspension, with subsequent treatment with EERB (200 mg/kg and 100 mg/kg) 48h after implantation. These values represent the tenth part of the DL<sub>50</sub> and CL<sub>50</sub>, respectively. The presence of phenols, tannins and triterpenes were demonstrated in the phytochemical results. Toxicity was dose-dependent, and the tumor inhibition was 84.1% and 75.8% at doses of 200 mg/kg and 100 mg/kg, respectively. We can highlight that the growth of Erlich's carcinoma suffered inhibitory effects against the EERB. EERB was found to have low acute toxicity and a high potential for use in antitumor therapy. Thus, new studies involving pre-clinical and clinical analyses of the extract are essential to determine the safe dose.
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