In-Vivo Testing Laboratory, Molecular Bioprospection Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow 226015, Uttar Pradesh, India.
J Ethnopharmacol. 2013 Oct 7;149(3):797-802. doi: 10.1016/j.jep.2013.08.003. Epub 2013 Aug 14.
Many of the effective therapeutic strategies have been derived from ethnopharmacologically used natural products. Pluchea lanceolata is an herb employed in Indian folk medicine for malaria like fever but it lacks proper pharmacological intervention.
To evaluate antimalarial and safety profile of Pluchea lanceolata: an in-vitro, in-vivo for its ethnopharmacological validation.
Methanol, butanol, ethyl acetate, chloroform, hexane extracts and its isolate, taraxasterol acetate (TxAc) were obtained from air dried aerial part of Pluchea lanceolata. These were tested in-vitro against chloroquine-sensitive strain of Plasmodium falciparum NF54 by measuring the parasite specific lactate dehydrogenase activity. The most potent hexane extract and TxAc were further validated for in-vivo antimalarial and safety evaluation. TxAc, a pentacyclic-triterpene isolated from the most active fraction was further evaluated with special emphasis on inflammatory mediators involved in malaria pathogenesis. Murine malaria was induced by intra-peritoneal injection of Plasmodium berghei infected red blood cells to the male Swiss inbred mice. Mice were orally treated following Peters 4-Day suppression test. In-vivo antimalarial efficacy was examined by evaluating the parasitaemia, percent survival, mean survival time, blood glucose, haemoglobin and pro-inflammatory mediators involved in malaria pathogenesis.
Hexane extract and TxAc showed promising antimalarial activity in-vitro and in-vivo condition. TxAc attributed in inhibition of the pro-inflammatory cytokines as well as afford to significant increase in the blood glucose and haemoglobin level when compared with vehicle treated infected mice. We have not observed the synergistic action of combinations of chloroquine and TxAc from our experimental results. In-vitro and in-vivo safety evaluation study revealed that hexane extract is non toxic at higher concentration.
Present study further validates the ancient Indian traditional knowledge and use of Pluchea lanceolata as an antimalarial agent. Study confirms the suitability of Pluchea lanceolata as a candidate for further studies to obtain a prototype for antimalarial medicine.
许多有效的治疗策略都源自于经过民族药理学验证的天然产物。白花丹是一种在印度民间医学中用于治疗疟疾样发热的草药,但缺乏适当的药理学干预。
评估白花丹的抗疟作用和安全性,并对其进行体内、体外研究,以验证其民族药理学的有效性。
从白花丹的干燥地上部分中提取甲醇、丁醇、乙酸乙酯、氯仿、正己烷提取物及其分离物,蒲公英甾醇乙酸酯(TxAc)。通过测量寄生虫特异性乳酸脱氢酶活性,在体外对氯喹敏感的恶性疟原虫 NF54 株进行测试。进一步验证了最有效的正己烷提取物和 TxAc 的体内抗疟作用和安全性。从最活跃的部分分离出的五环三萜 TxAc 进一步用于评估其对疟疾发病机制中涉及的炎症介质的影响。通过向雄性瑞士近交系小鼠腹腔内注射感染的伯氏疟原虫红细胞来诱导鼠疟。按照彼得斯 4 天抑制试验对小鼠进行口服治疗。通过评估寄生虫血症、存活率、平均存活时间、血糖、血红蛋白和疟疾发病机制中涉及的促炎介质,来检查体内抗疟疗效。
正己烷提取物和 TxAc 在体内和体外均表现出有希望的抗疟活性。与用载体处理的感染小鼠相比,TxAc 可抑制促炎细胞因子,并显著提高血糖和血红蛋白水平。从我们的实验结果来看,没有观察到氯喹和 TxAc 的联合作用具有协同作用。体内和体外安全性评估研究表明,正己烷提取物在较高浓度下无毒性。
本研究进一步验证了印度古代传统知识和将白花丹用作抗疟药物的用途。研究证实,白花丹适合进一步研究,以获得抗疟药物的原型。