Department of Pharmaceutical Analysis, School of Pharmaceutical Sciences, Siksha O Anusnadhan Deemed to Be University, Kalinga Nagar, Bhubaneswar, Odisha, 751003, India.
J Ethnopharmacol. 2021 Jul 15;275:114113. doi: 10.1016/j.jep.2021.114113. Epub 2021 Apr 20.
Heliconia rostrata Ruiz and Pav. belongs to the family Heliconiaceae. Plant was traditionally used to cure jaundice, intestinal pain, diabetes and hypertension.
Present study evaluated hepatoprotective efficacy of ethanol (REE) and methanol (RME) extracts of H. rostrata rhizomes in HepG2 cell lines and rats. Antioxidant efficacy of extracts was determined using ex vivo and in vivo methods.
Before conducting efficacy studies, safety of REE and RME was established using toxicity studies which included Oral acute-fixed dose toxicity using OECD TG420, 28-days repeated dose oral toxicity by OECD TG407 and cytotoxicity studies by brine shrimp lethality (BSL) bioassay and MTT assay taking HepG2 cell line. Ex vivo (Extracts: 0-250 μg/ml) and in vivo (Extracts: 50, 100 and 200 mg/kg) antioxidant studies were performed on fresh goat liver and rats (N = 45) of either sex, respectively. In vitro hepatoprotective efficacy of extracts was evaluated against ethanol induced toxicity in HepG2 cell line. In vivo study was performed at 50, 100 and 200 mg/kg/day doses in rats by CCl-induced hepatotoxicity study.
No mortality was observed during single and repeated dose toxicity studies. 50% lethal dose >2000 mg/kg, confirmed category 5 toxicity level of extracts, according to Globally Harmonized System. No signs of toxicity and treatment or dose related changes recorded in rats under repeated dose toxicity study. No-observed-adverse effect-level of 200 mg/kg/day was observed for both extracts. Median lethal concentration of REE and RME were 1291.30 and 1045.89 μg/ml, respectively in BSL bioassay and 50% cytotoxicity concentration >1000 μg/ml was obtained for both extracts from MTT assay. Calculated 50% inhibitory concentration and median effective dose of extracts obtained from different antioxidant assays in ex vivo and in vivo antioxidant studies, respectively indicated REE has more antioxidant efficacy than RME. In in vitro hepatoprotective efficacy study, extracts demonstrated dose dependent protection against ethanol induced hepatotoxicity. At 400 μg/ml, REE and RME demonstrated percentage protection of 65.53% and 57.98%, respectively. Results of liver function test and histopathological evaluation of liver in in vivo hepatoprotective study confirmed dose dependent protection provided by the extracts against CCl -induced hepatotoxicity.
Both REE and RME were found safe to be considered for therapeutic uses. Both REE and RME were found to exhibit antioxidant efficacy in ex vivo and in vivo models. Results ascertained that H. rostrata rhizomes possess significant hepatoprotective potency.
Heliconia rostrata Ruiz and Pav. 属于 Heliconiaceae 科。该植物传统上用于治疗黄疸、腹痛、糖尿病和高血压。
本研究评估了 Heliconia rostrata 根茎的乙醇（REE）和甲醇（RME）提取物在 HepG2 细胞系和大鼠中的保肝作用。使用体外和体内方法测定提取物的抗氧化功效。
在进行功效研究之前，通过 OECD TG420 口服急性固定剂量毒性研究、OECD TG407 28 天重复口服毒性研究和使用盐水虾致死（BSL）生物测定和 HepG2 细胞系的 MTT 测定的细胞毒性研究，确定 REE 和 RME 的安全性。在新鲜山羊肝（提取物：0-250μg/ml）和大鼠（各性别，n=45）中进行体外（提取物：50、100 和 200mg/kg）和体内抗氧化研究。评估提取物对 HepG2 细胞系乙醇诱导毒性的体外保肝作用。在 CCl 诱导的肝毒性研究中，以 50、100 和 200mg/kg/天的剂量在大鼠中进行体内研究。
在单次和重复剂量毒性研究中未观察到死亡。根据全球协调系统，50%致死剂量>2000mg/kg，证实提取物的毒性类别为 5 级。在重复剂量毒性研究中，大鼠未出现毒性和治疗或剂量相关变化的迹象。两种提取物的无观察到不良效应水平（NOAEL）为 200mg/kg/天。REE 和 RME 在 BSL 生物测定中的半数致死浓度分别为 1291.30 和 1045.89μg/ml，MTT 测定中两种提取物的 50%细胞毒性浓度均>1000μg/ml。从不同的体外和体内抗氧化研究中获得的抗氧化测定的 50%抑制浓度和中效剂量表明，REE 的抗氧化功效强于 RME。在体外保肝作用研究中，提取物对乙醇诱导的肝毒性表现出剂量依赖性保护作用。在 400μg/ml 时，REE 和 RME 分别显示出 65.53%和 57.98%的保护率。体内保肝研究中肝功能试验和肝组织病理学评价的结果证实，提取物对 CCl 诱导的肝毒性具有剂量依赖性的保护作用。
REE 和 RME 均被发现安全，可考虑用于治疗用途。REE 和 RME 均在体外和体内模型中表现出抗氧化功效。结果证实，Heliconia rostrata 根茎具有显著的保肝作用。
