研究甜菜红素化合物的毒性:对标准化β-庸俗草提取物的硅学分析和体内预测

Q2 Pharmacology, Toxicology and Pharmaceutics International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI:10.22159/ijap.2024v16i1.49189
S. E. Nugraha, J. M. Keliat, R. A. Syahputra, Sony Eka, Nugraha
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引用次数: 0

摘要

目的:人们对甜菜根的抗氧化、血液保护和心脏保护特性进行了广泛的研究。然而,目前还需要更多与甜菜根提取物毒性评估相关的可用证据。毒性评估采用了硅学和体内方法。测试前,根据印尼食品药品监管局(BPOM)制定的准则对提取物进行了标准化处理:实验对象包括 25 只健康状况良好的雄性 Wistar 大鼠,体重在 150 至 170 克之间。这些大鼠被分成五组,每组五只。第 1 组为对照组,第 2 至第 5 组为治疗组。采用 pK-CSM、SwissADME 和 Pro-Tox II 方法进行化学毒性分析:结果表明,标准化乙醇提取物含水 4.341%,总灰分 3.67%,酸不溶性灰分 1.53%。铅(Pb)和镉(Cd)的浓度为百万分之零(ppm)。随后,总菌落总数和酵母菌数分别为 0.47 5 x 10-4(CFU/g)和 0.382 x 10-4(CFU/g)。这一结果表明该提取物符合 BPOM 的要求。这项研究还测定了红甜菜根中的甜菜红素含量,结果显示总浓度为 11.34 0.37 毫克/100 克样品。血液学实验表明,甜菜根提取物会影响大鼠的血液学。与对照组相比,服用提取物的大鼠红细胞和血小板计数更高。此外,对甜菜根提取物中的活性成分进行的内部毒性测试显示,这些化合物的半数致死剂量为 305 毫克/千克,因此被归类为 IV 类,具有潜在的肝毒性。在体内实验中,肝脏和肾脏参数明显升高。此外,试验对象在服用 5,000 毫克/千克体重的剂量时出现了一次死亡事件:结论:单次口服该提取物的剂量大于每公斤体重 5,000 毫克时不会导致死亡,但对肝脏有潜在毒性。
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INVESTIGATING THE TOXICITY OF BETALAIN COMPOUNDS: IN SILICO ANALYSIS AND IN VIVO PREDICTIONS FOR STANDARDIZED BETA VULGARIS L. EXTRACT
Objective: Extensive research has been conducted on beetroot's antioxidant, hematoprotective, and cardioprotective properties. However, there currently needs to be more available evidence pertaining to the toxicity assessment of the extract. The toxicity assessment was conducted using both in silico and in vivo methods. Prior to testing, the extracts were standardized in accordance with the guidelines set by the Indonesian Food Drug Authority (BPOM), which is the regulatory authority for food and drugs in Indonesia. Methods: The experimental subjects consisted of 25 male Wistar rats in good health, weighing between 150 and 170 grams. These rats were separated into five groups, each including five rats. Group 1 will serve as the control group, while groups 2 through 5 will be designated as the treatment groups. The analysis of chemical toxicity was conducted using pK-CSM, SwissADME, and Pro-Tox II methodologies. Results: The results indicated that the standardized ethanol extract contained 4.341% water, 3.67 % total ash, and 1.53 % acid-insoluble ash. Lead (Pb) and cadmium (Cd) were absent at a concentration of 0 parts per million (ppm). Subsequently, the total plate count and yeast mould count were 0.47 5 x 10-4 (CFU/g) and a of 0.382 x 10-4 (CFU/g) respectively. This finding implies that the extract meets BPOM requirement. This study also measured the betalain content of red beetroot, yielding a total concentration of 11.34 0.37 mg/100 gram of sample. Haematological experiments showed that beetroot extract affected rat blood haematology. Compared to the control group, rats given the extract had higher red blood cell and platelet counts. Additionally, the Insilico toxicity test conducted on the active component derived from beetroot revealed LD50 of the compounds ranged from 305 mg/kg so that were categorized into classes IV and presence of hepatotoxic potential. During the in vivo experiment, there has been a notable rise in hepatic and renal parameters. Furthermore, one mortality event occurred in the test subject at a 5,000 mg/kg body weight dosage. Conclusion: Single oral administration of the extract at a dose larger than 5,000 mg per kilogram of body weight does not result in lethal effects, however showed potential toxicity to the liver.
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来源期刊
International Journal of Applied Pharmaceutics
International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.40
自引率
0.00%
发文量
219
期刊介绍: International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.
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