Anti-Leishmania amazonensis Activity, Cytotoxic Features, and Chemical Profile of Allium sativum (Garlic) Essential Oil

被引:3
作者
Garcia, Andreza R. [1 ]
Amorim, Mariana M. B. [2 ]
Amaral, Ana Claudia F. [3 ]
da Cruz, Jefferson D. [3 ]
Vermelho, Alane B. [4 ]
Nico, Dirlei [4 ]
Rodrigues, Igor A. [1 ,5 ]
机构
[1] Univ Fed Rio Janeiro, Fac Farm, Programa Pos Graduacao Ciencias Farmaceut, BR-21941902 Rio De Janeiro, Brazil
[2] Inst Municipal Vigilancia Sanit, Vigilancia Zoonoses & Inspecao Agr, BR-22290240 Rio De Janeiro, Brazil
[3] Farmanguinhos Fiocruz, Dept Prod Nat, BR-21041250 Rio De Janeiro, Brazil
[4] Univ Fed Rio Janeiro, Dept Microbiol Geral, Inst Microbiol Paulo Goes, BR-21941902 Rio De Janeiro, Brazil
[5] Univ Fed Rio Janeiro, Fac Farm, Dept Prod Nat & Alimentos, BR-21941902 Rio De Janeiro, Brazil
关键词
tegumentary leishmaniasis; antileishmanial activity; organosulfur compounds; cytotoxicity; computational analysis; IN-VITRO; ANTILEISHMANIAL ACTIVITY; DISULFIDE; ACTIVATION; EXTRACT; VIVO;
D O I
10.3390/tropicalmed8070375
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Human tegumentary leishmaniasis (HTL) is a serious tropical disease caused by Leishmania amazonensis. Developing new leishmanicidal agents can help overcome current treatment challenges, such as drug resistance and toxicity. Essential oils are a source of lipophilic substances with diverse therapeutic properties. This study aimed to determine the anti-L. amazonensis activity, cytotoxicity, and chemical profile of Allium sativum essential oil (ASEO). The effect of ASEO on parasite and mammalian cells viability was evaluated using resazurin and MTT assays, respectively. The oil's effect against intracellular amastigotes was also determined. Transmission electron microscopy was used to assess the ultrastructural changes induced by ASEO. In addition, the chemical constituents of ASEO were identified by gas chromatography-mass spectrometry (GC-MS). The cytotoxic potential was evaluated in vitro and in silico. The oil displayed IC50 of 1.76, 3.46, and 3.77 & mu;g/mL against promastigotes, axenic, and intracellular amastigotes, respectively. Photomicrographs of treated parasites showed plasma membrane disruption, increased lipid bodies, and autophagic-like structures. ASEO chemical profiling revealed 1,2,4,6-tetrathiepane (24.84%) and diallyl disulfide (16.75%) as major components. Computational pharmacokinetics and toxicological analysis of ASEO's major components demonstrated good oral bioavailability and better toxicological endpoints than the reference drugs. Altogether, the results suggest that ASEO could be an alternative drug candidate against HTL.
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页数:19
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