Department of Biotechnology, Indian Institute of Technology Guwahati, Assam-781039, India.
J Ethnopharmacol. 2011 Apr 12;134(3):996-8. doi: 10.1016/j.jep.2011.01.044. Epub 2011 Feb 1.
Nyctanthes arbortristis L. (Oleaceae) is widely used in the traditional medicine of India. The plant is shown to have antibacterial and antileishmanial activities.
Evaluation of iridoid glucosides from the plant as inhibitor of trypanothione reductase (TryR), a validated drug target enzyme of the Leishmania parasite. The study contributes towards understanding mechanism of antileishmanial effect of the plant.
TryR of Leishmania parasite is expressed and purified. Iridoid glucosides are isolated from the plant and tested as inhibitor of TryR enzyme of the parasite.
Inhibitory constant (K(i)) of various iridoid glucosides ranges from 3.24±0.05 μM to 6.49±0.05 μM. Thus, the molecular mechanism underlying antileishmanial activity of these compounds is mediated through inhibition of TryR.
The current study also points out towards potential application of iridoid glucosides as novel drugs against the disease.
Nyctanthes arbortristis L.（木犀科）在印度传统医学中被广泛应用。该植物已被证明具有抗菌和抗利什曼原虫的活性。
评估该植物中的环烯醚萜葡萄糖苷作为利什曼原虫的三磷酸鸟苷还原酶（TryR）的抑制剂，TryR 是利什曼原虫寄生虫的一种已验证的药物靶点酶。该研究有助于了解植物抗利什曼原虫作用的机制。
寄生虫的 TryR 被表达和纯化。从植物中分离出环烯醚萜葡萄糖苷，并测试其作为寄生虫 TryR 酶的抑制剂的效果。
各种环烯醚萜葡萄糖苷的抑制常数（K(i)）范围为 3.24±0.05 μM 至 6.49±0.05 μM。因此，这些化合物抗利什曼原虫活性的分子机制是通过抑制 TryR 介导的。
本研究还指出，环烯醚萜葡萄糖苷作为治疗该疾病的新型药物具有潜在的应用前景。
