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金叶风铃木叶乙醇提取物的抗疟原虫活性及其对血红素解毒的抑制作用。

Antiplasmodial activity of Ethanolic extract of Cassia spectabilis DC leaf and its inhibition effect in Heme detoxification.

机构信息

Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Universitas Airlangga, Campus C, Mulyorejo Street, Surabaya, 60115, Indonesia.

Department of Medical Parasitology, Faculty of Medicine, Universitas Airlangga, Campus A, Surabaya, 60132, Indonesia.

出版信息

BMC Complement Med Ther. 2021 Feb 19;21(1):71. doi: 10.1186/s12906-021-03239-9.

DOI:10.1186/s12906-021-03239-9
PMID:33607987
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7896390/
Abstract

BACKGROUND

In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial.

METHODS

The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method.

RESULTS

The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D-D) + artesunate (D) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml).

CONCLUSION

C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

摘要

背景

在之前的研究中,翅荚决明叶已显示出良好的抗疟原虫活性。因此,本研究是对翅荚决明叶提取物进行体外和体内抗疟原虫活性和机制的后续研究,作为一种抗疟药物。

方法

对提取物进行分段、亚分段和分离,以获得纯化的化合物。进行体外抗疟原虫活性测试,以发现活性化合物。对感染伯氏疟原虫 ANKA 的小鼠进行体内测试,以确定单独或与青蒿琥酯联合使用的预防活性和抗疟原虫活性。采用 Basilico 法进行血红素解毒抑制测试,作为一种抗疟机制。

结果

结果表明,从翅荚决明叶中分离出的活性抗疟化合物具有与(-)-7-羟基卡辛相同的结构模式。90%乙醇提取物对感染伯氏疟原虫 ANKA 的小鼠进行单独预防测试,获得的最高抑制率为 68.61%,而阳性对照(强力霉素 13mg/kg)为 73.54%。与青蒿琥酯联合使用时,每天 3 次,150mg/kg 的翅荚决明 DC(D-D)+青蒿琥酯(D)的效果优于标准的阿莫地喹+青蒿琥酯组合,抑制率分别为 99.18%和 92.88%。提取物对血红素解毒抑制的 IC 为 0.375mg/ml,优于磷酸氯喹(0.682mg/ml)。

结论

翅荚决明叶具有很强的抗疟原虫活性,可能为有效和负担得起的抗疟植物药物提供潜在的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/c414bebcac2b/12906_2021_3239_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/3b3d52fd11f6/12906_2021_3239_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/aecba90f655b/12906_2021_3239_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/df83b560a1c5/12906_2021_3239_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/b2ca18060eb4/12906_2021_3239_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/e836195e4fe2/12906_2021_3239_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/c414bebcac2b/12906_2021_3239_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/3b3d52fd11f6/12906_2021_3239_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/aecba90f655b/12906_2021_3239_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/df83b560a1c5/12906_2021_3239_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/b2ca18060eb4/12906_2021_3239_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/e836195e4fe2/12906_2021_3239_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ab8/7896390/c414bebcac2b/12906_2021_3239_Fig6_HTML.jpg

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