Shahsavari Saeid, Sharifi Iraj, Salarkia Ehsan, Keyhani Alireza, Sharifi Fatemeh, Babaei Zahra
Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran.
Research Center of Tropical and Infectious Diseases, Kerman University of Medical Sciences, Kerman, Iran.
Immunol Res. 2024 Dec;72(6):1313-1326. doi: 10.1007/s12026-024-09530-4. Epub 2024 Aug 18.
Conventional therapeutic agents are no longer adequate against leishmaniasis. This complex condition continues to have a high mortality rate and public health impact. The present study aimed to explore an extensive array of experiments to monitor the biological activities of 6-shogaol, a major component of ginger, and meglumine antimoniate (MA or Glucantime®). The binding affinity of 6-shogaol and inducible nitric oxide synthase (iNOS), a major enzyme catalyzing nitric oxide (NO) from L-arginine was the source for the docking outline. The inhibitory effects of 6-shogaol, MA, and mixture were assessed using colorimetric and macrophage assays. Antioxidant activity was inferred by UV-visible spectrophotometry. Variably expressed genes were measured by quantifiable real-time polymerase chain reaction. Apoptotic and cell cycle profiles were analyzed by flow cytometry. Moreover, a DNA fragmentation assay was performed by electrophoresis and antioxidant metabolites include superoxide dismutase (SOD), catalase (CAT), and also nitric oxide (NO) by enzyme-linked immunosorbent assay. 6-shogaol and MA exhibited multiple synergistic mechanisms of action. These included a remarkable leishmanicidal effect, potent antioxidative activity, a high safety index, upregulation of M1 macrophages/Th1-associated cytokines (including, γ-interferon, interleukin-12p40, tumor necrotizing factor-alpha, and associated iNOS), significant cell division capture at the sub-G0/G1 phase, a high profile of apoptosis through DNA fragmentation of the nuclear components. In addition, the activity of NO was substantially elevated by treated intracellular amastigotes, while SOD and CAT activities were significantly diminished. This study is exclusive because no similar investigation has inclusively been conducted before. These comprehensive mechanistic actions form a logical foundation for additional advanced study.
传统治疗药物已不足以应对利什曼病。这种复杂病症的死亡率依然很高,对公共卫生影响重大。本研究旨在开展一系列广泛实验,以监测生姜的主要成分6-姜辣素和葡甲胺锑酸盐(MA或葡醛酯®)的生物活性。6-姜辣素与诱导型一氧化氮合酶(iNOS,一种催化从L-精氨酸生成一氧化氮(NO)的主要酶)的结合亲和力是对接轮廓的来源。使用比色法和巨噬细胞试验评估了6-姜辣素、MA及其混合物的抑制作用。通过紫外可见分光光度法推断抗氧化活性。通过定量实时聚合酶链反应测量差异表达基因。通过流式细胞术分析凋亡和细胞周期概况。此外,通过电泳进行DNA片段化试验,并通过酶联免疫吸附测定法检测抗氧化代谢物,包括超氧化物歧化酶(SOD)、过氧化氢酶(CAT)以及一氧化氮(NO)。6-姜辣素和MA表现出多种协同作用机制。这些机制包括显著的杀利什曼原虫作用、强大的抗氧化活性、高安全指数、上调M1巨噬细胞/Th1相关细胞因子(包括γ-干扰素、白细胞介素-12p40、肿瘤坏死因子-α以及相关的iNOS)、在亚G0/G1期显著捕获细胞分裂、通过细胞核成分的DNA片段化实现高凋亡率。此外,经处理的细胞内无鞭毛体使NO活性大幅升高,而SOD和CAT活性显著降低。本研究具有独特性,因为此前尚未有过类似的全面调查。这些全面的作用机制为进一步的深入研究奠定了合理基础。