Department of Biomedical Science, Kyung Hee University School of Medicine, 26 Kyunghee-daero, Dongdaemun-gu, Seoul 130-701, Republic of Korea; Department of Medical Zoology, Kyung Hee University School of Medicine, 26 Kyunghee-daero, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Asian Pac J Trop Med. 2016 Feb;9(2):125-9. doi: 10.1016/j.apjtm.2016.01.021. Epub 2016 Jan 11.
To evaluate a new pharmacological activity/effect of linolenic acid (α- and γ-form) and conjugated-linoleic acid (CLA) causing antibacterial activity against Mycobacterium tuberculosis (Mtb).
The anti-Mtb activity/effect of linolenic acid and CLA were determined using different anti-Mtb indicator methods such as resazurin microtiter assay (REMA) and MGIT 960 system assay. The Mtb was incubated with various concentrations (12.5-200 μg/mL) of the compounds and anti-Mtb first-line drugs for 5 d in the REMA, and for 3 wk in MGIT 960 system assay.
Linolenic acid and CLA obviously indicated their anti-Mtb activity/effect by strongly inhibiting the growth/proliferation of Mtb in a dose-dependent manner in the REMA and the MGIT 960 system assay. Interestingly, linolenic acid and CLA consistently induced anti-Mtb activity/effect by effectively inhibiting the growth/proliferation of Mtb in MGIT 960 system for 21 d with a single treatment, and their minimum inhibitory concentrations were measured as 200 μg/mL respectively.
These results demonstrate that linolenic acid and CLA not only have effective anti-Mtb activity/properties, but also induce the selective-anti-Mtb effects by strongly inhibiting and blocking the growth/proliferation of Mtb through a new pharmacological activity/action. Therefore, this study provides novel perspectives for the effective use of them and the potential that can be used as potent anti-Mtb candidate drugs, as well as suggests the advantage of reducing the cost and/or time for developing a new/substantive drug by effectively repurposing the existing drugs or compounds as one of new strategies for the global challenge of tuberculosis.
评估亚麻酸(α-和γ-形式)和共轭亚油酸(CLA)的新药理活性/作用,其具有抗分枝杆菌(Mtb)的抗菌活性。
使用不同的抗 Mtb 指示剂方法(如 Resazurin 微量滴定法(REMA)和 MGIT 960 系统检测法)来确定亚麻酸和 CLA 的抗 Mtb 活性/作用。将 Mtb 与不同浓度(12.5-200μg/ml)的化合物和抗 Mtb 的一线药物在 REMA 中孵育 5 天,在 MGIT 960 系统中孵育 3 周。
亚麻酸和 CLA 在 REMA 和 MGIT 960 系统中均以剂量依赖性方式强烈抑制 Mtb 的生长/增殖,明显表现出抗 Mtb 活性/作用。有趣的是,亚麻酸和 CLA 连续地以单一治疗方式在 MGIT 960 系统中有效地抑制 Mtb 的生长/增殖,诱导出抗 Mtb 活性/作用,其最小抑菌浓度分别为 200μg/ml。
这些结果表明,亚麻酸和 CLA 不仅具有有效的抗 Mtb 活性/特性,而且通过强烈抑制和阻断 Mtb 的生长/增殖,产生选择性的抗 Mtb 作用,通过一种新的药理活性/作用。因此,本研究为有效利用亚麻酸和 CLA 提供了新的视角,以及作为有潜力的抗 Mtb 候选药物的可能性,并提示了通过有效重新利用现有药物或化合物作为新策略之一,为全球结核病挑战提供了降低开发新药物/实质性药物的成本和/或时间的优势。