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戟叶酸模中分离出的粗皂苷及其不同组分的抗肿瘤和抗血管生成潜力

Antitumor and anti-angiogenic potentials of isolated crude saponins and various fractions of Rumex hastatus D. Don.

作者信息

Ahmad Sajjad, Ullah Farhat, Ayaz Muhammad, Zeb Anwar, Ullah Farman, Sadiq Abdul

机构信息

Department of Pharmacy, University of Malakand, Chakdara, Dir (L), Khyber-Pakhtunkhwa (KPK), 18000, Pakistan.

Department of Pharmacy, Kohat University of Science and Technology, Kohat, Khyber-Pakhtunkhwa (KPK), 26000, Pakistan.

出版信息

Biol Res. 2016 Mar 12;49:18. doi: 10.1186/s40659-016-0079-2.

DOI:10.1186/s40659-016-0079-2
PMID:26969307
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4788867/
Abstract

BACKGROUND

Cancer, being the foremost challenge of the modern era and the focus of world-class investigators, gargantuan research is in progress worldwide to explore novel therapeutic for its management. The exploitation of natural sources has been proven to be an excellent approach to treat or minify the excessive angiogenesis and proliferation of cells. Similarly, based the ethnomedicinal uses and literature survey, the current study is designed to explore the anti-tumor and anti-angiogenic potentials of Rumex hastatus. Anti-tumor and anti-angiogenic activities were carried out using potato-disc model and chorioallantoic membrane (CAM) assay respectively. Moreover, R. hastatus was also assessed for antibacterial activity against Agrobacterium tumefaciens (tumor causing bacterial strain). The positive controls used in anti-tumor, anti-angiogenic and antibacterial activities were vincristine sulphate, dexamethasone and cefotaxime respectively.

RESULTS

The crude saponins (Rh.Sp), methanolic extract (Rh.Cr) and other solvent extracts like n-hexane (Rh.Hex), chloroform (Rh.Chf), ethylacetate (Rh.EtAc) and aqueous fraction (Rh.Aq) exhibited notable anti-tumor and anti-angiogenic activities. In potato tumor assay, the chloroform and saponin fractions were observed to be the most effective showing 86.7 and 93.3 % tumor inhibition at 1000 µg/ml with IC50 values 31.6 and 18.1 µg/ml respectively. Similarly, these two samples i.e., chloroform and saponins also excelled among the entire test samples in anti-angiogenic evaluation exhibiting 81.6 % (IC50 = 17.9 µg/ml) and 78.9 % (IC50 = 64.9 µg/ml) at 1000 µg/ml respectively. In contrast, the antibacterial investigations revealed a negligible potential against A. tumefaciens.

CONCLUSION

Based on our results we can claim that R. hastatus possesses both anti-tumor and anti-angiogenic potentials. In all of the solvent fractions, Rh.Chf and Rh.Sp were most effective against tumor and angiogenesis while having negligible activity against A. tumefaciens. It can be concluded that Rh.Chf and Rh.Sp might be potential targets in the isolation of natural product having anti-neoplastic action.

摘要

背景

癌症是现代社会面临的首要挑战,也是世界级研究人员关注的焦点。全球范围内正在进行大量研究,以探索新的癌症治疗方法。利用天然资源已被证明是治疗或减少细胞过度血管生成和增殖的有效途径。同样,基于民族药用用途和文献调查,本研究旨在探索戟叶酸模的抗肿瘤和抗血管生成潜力。分别使用马铃薯圆盘模型和鸡胚绒毛尿囊膜(CAM)试验进行抗肿瘤和抗血管生成活性研究。此外,还评估了戟叶酸模对根癌土壤杆菌(致瘤细菌菌株)的抗菌活性。抗肿瘤、抗血管生成和抗菌活性研究中使用的阳性对照分别为硫酸长春新碱、地塞米松和头孢噻肟。

结果

粗皂苷(Rh.Sp)、甲醇提取物(Rh.Cr)以及其他溶剂提取物,如正己烷(Rh.Hex)、氯仿(Rh.Chf)、乙酸乙酯(Rh.EtAc)和水相部分(Rh.Aq)均表现出显著抗肿瘤和抗血管生成活性。在马铃薯肿瘤试验中,氯仿和皂苷部分最为有效,在1000μg/ml时肿瘤抑制率分别为86.7%和93.3%,IC50值分别为31.6和18.1μg/ml。同样,在抗血管生成评估中,这两个样品,即氯仿和皂苷,在所有测试样品中也表现出色,在1000μg/ml时分别表现出81.6%(IC50 = 17.9μg/ml)和78.9%(IC50 = 64.9μg/ml)的抑制率。相比之下,抗菌研究表明其对根癌土壤杆菌的抗菌潜力可忽略不计。

结论

根据我们的研究结果,可以认为戟叶酸模具有抗肿瘤和抗血管生成潜力。在所有溶剂部分中,Rh.Chf和Rh.Sp对肿瘤和血管生成最为有效,而对根癌土壤杆菌的活性可忽略不计。可以得出结论,Rh.Chf和Rh.Sp可能是分离具有抗肿瘤作用天然产物的潜在靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/5125737acb82/40659_2016_79_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/b719549e1d10/40659_2016_79_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/b6c024f06939/40659_2016_79_Fig2_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/133a7e781c7c/40659_2016_79_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/5125737acb82/40659_2016_79_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/b719549e1d10/40659_2016_79_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/b6c024f06939/40659_2016_79_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/4f6b12e7de03/40659_2016_79_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/133a7e781c7c/40659_2016_79_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baad/4788867/5125737acb82/40659_2016_79_Fig5_HTML.jpg

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