常规的治疗剂不再足以对抗利什曼病。这种复杂的情况继续具有高死亡率和公共卫生影响。本研究旨在探索一系列广泛的实验来监测6-shogaol的生物活性,生姜的主要成分,和锑酸葡甲胺(MA或Gluantime®)。6-shogaol与诱导型一氧化氮合酶(iNOS)的结合亲和力,从L-精氨酸中催化一氧化氮(NO)的主要酶是对接概述的来源。6-shogaol的抑制作用,MA,和混合物使用比色和巨噬细胞测定法进行评估。通过紫外可见分光光度法推断抗氧化活性。通过可定量的实时聚合酶链反应测量可变表达的基因。通过流式细胞术分析凋亡和细胞周期谱。此外,通过电泳进行DNA片段化测定,抗氧化代谢产物包括超氧化物歧化酶(SOD),过氧化氢酶(CAT),以及通过酶联免疫吸附测定的一氧化氮(NO)。6-shogaol和MA表现出多种协同作用机制。这些包括显著的利什曼杀菌作用,有效的抗氧化活性,安全指数高,M1巨噬细胞/Th1相关细胞因子的上调(包括,γ-干扰素,白细胞介素-12p40,肿瘤坏死因子-α,和相关的iNOS),在亚G0/G1期明显的细胞分裂捕获,通过核成分的DNA片段化的高凋亡率。此外,经处理的细胞内amastigotes显著提高了NO的活性,而SOD和CAT活性显著降低。这项研究是排他性的,因为以前没有进行过类似的调查。这些全面的机械动作为额外的高级学习奠定了逻辑基础。
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.