Extracts of six Rubiaceae species combined with rifampicin have good in vitro synergistic antimycobacterial activity and good anti-inflammatory and antioxidant activities.
Extracts of six Rubiaceae species combined with rifampicin have good in vitro synergistic antimycobacterial activity and good anti-inflammatory and antioxidant activities.
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DOI：
10.1186/s12906-016-1355-y
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发表时间：
2016-10-03
影响因子：
--
通讯作者：
McGaw LJ
中科院分区：
文献类型：
--
作者：
Aro AO;Dzoyem JP;Eloff JN;McGaw LJ
Rubiaceae家族通过提供具有潜在用途的分子作为用于开发治疗药物的模板而在药物发现中发挥了重要作用。本研究旨在研究六种茜草科植物与已知抗结核药物组合的体外协同作用。还评价了这些物种的抗氧化和抗炎活性，以研究抗分枝杆菌治疗的额外益处。采用棋盘格法测定了植物提取物与利福平联用的抗分枝杆菌增效作用。采用2，2-二苯基-1-苦基肼（DPPH）法测定提取物的抗氧化活性。使用Griess测定法在LPS活化的RAW 264.7巨噬细胞中进行通过抑制一氧化氮（NO）产生的抗炎活性。利福平与粗提物的组合导致提取物的活性增加4至256倍。其中三花Cremaspora粗提物与利福平的协同作用最好，对金黄分枝杆菌的FIC指数为0.08。九节提取物的抗氧化活性最好，其IC 50值为1.77 μg/mL，低于曲洛昔和抗坏血酸的IC 50值（分别为5.67 μg/mL和4.66 μg/mL）。所有供试提取物均以浓度依赖性方式抑制一氧化氮（NO）的产生，抑制率为6.73%~ 86.27%。研究的某些茜草科植物与利福平具有显著的体外协同作用，并且具有良好的自由基清除能力和抗炎活性。这些初步结果保证了对这些植物的进一步研究，以确定从这些物种中分离的化合物是否可以导致生物活性化合物的开发，这些生物活性化合物可以增强利福平的活性，甚至对抗耐药分枝杆菌。
The Rubiaceae family has played a significant role in drug discovery by providing molecules with potential use as templates for the development of therapeutic drugs. This study was designed to study the in vitro synergistic effect of six Rubiaceae species in combination with a known anti-TB drug. The antioxidant and anti-inflammatory activity of these species were also evaluated to investigate additional benefits in antimycobacterial treatment. The checkerboard method was used to determine the antimycobacterial synergistic activity of plant extracts combined with rifampicin. The antioxidant activity of extracts was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. Anti-inflammatory activity via inhibition of nitric oxide (NO) production was performed in LPS-activated RAW 264.7 macrophages using the Griess assay. Combination of rifampicin with the crude extracts resulted in a 4 to 256-fold increase of activity of extracts. The crude extract of Cremaspora triflora produced the best synergistic effect with rifampicin, with a fractional inhibitory concentration (FIC) index of 0.08 against Mycobacterium aurum. Extracts of Psychotria zombamontana had the best antioxidant activity with an IC50 value of 1.77 μg/mL, lower than the IC50 of trolox and ascorbic acid (5.67 μg/mL and 4.66 μg/mL respectively). All the extracts tested inhibited nitric oxide (NO) production in a concentration dependent manner with the percentage of inhibition varying from 6.73 to 86.27 %. Some of the Rubiaceae species investigated have substantial in vitro synergistic effects with rifampicin and also good free radical scavenging ability and anti-inflammatory activity. These preliminary results warrant further study on these plants to determine if compounds isolated from these species could lead to the development of bioactive compounds that can potentiate the activity of rifampicin even against resistant mycobacteria.
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