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Antitumor Effects and Related Mechanisms of Ethyl Acetate Extracts of Polygonum perfoliatum L.

ABSTRACT: Polygonum perfoliatum L. belongs to the genus Polygonaceae and has a long history to be used as a Chinese medicinal herb to reduce swelling, control body temperature, and promote detoxification. However, its anticancer activity and mechanisms of action have not been evaluated yet. In the present study, we used several cell lines and xenograft models from different cancers to demonstrate the broad-spectrum anticancer activity of P. perfoliatum L as well as its underlying mechanisms of action in vitro and in vivo. The ethyl acetate extract of P. perfoliatum L showed good anticancer activity and was further fractioned to obtain five active components, including PEA to PEE. Among these fractions, PEC showed the strongest cytotoxicities against various cancer cell lines. It was further observed that PEC inhibited cancer cell growth, arrested cells at G2 phase, and induced apoptosis in vitro and suppressed tumor growth and angiogenesis in vivo in a dose- and time-dependent manner. Furthermore, PEC decreased the expression of vascular endothelial growth factor (VEGF) and micro-vascular density (MVD) in tumor tissues in vivo. It also promoted the proliferation of T and B lymphocytes, increased the activities of natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), enhanced the secretion of interleukin 2 (IL-2) by spleen cells, and raised the levels of IgG, IgG2a, and IgG2b antibodies in tumor-bearing mice in vivo, which were at least partially responsible for the anticancer activity of PEC. In summary, PEC has shown broad-spectrum anticancer activities without causing any host toxicity in vitro and in vivo and may be developed as a preventive and therapeutic agent against human cancer. Further studies are urgently needed to determine the anticancer compounds in PEC and their detailed molecular mechanisms.

SUBMITTER: Li Q

PROVIDER: S-EPMC6621420 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Antitumor Effects and Related Mechanisms of Ethyl Acetate Extracts of Polygonum perfoliatum L.

Li Qinglin Q Fu Xiaoxuan X Ge Xinyang X Tao Feng F Huang Ping P Ge Minghua M Jin Hongchuan H

Frontiers in oncology 20190704

Polygonum perfoliatum L. belongs to the genus Polygonaceae and has a long history to be used as a Chinese medicinal herb to reduce swelling, control body temperature, and promote detoxification. However, its anticancer activity and mechanisms of action have not been evaluated yet. In the present study, we used several cell lines and xenograft models from different cancers to demonstrate the broad-spectrum anticancer activity of P. perfoliatum L as well as its underlying mech ...[more]

PMID: 31334112

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Project description:Conventional and modern cancer treatment were reported to manifest adverse effects to the patients. More researches were conducted to search for selective cytotoxic agent of plant natural product on cancer cells. The presences of wide range phytochemicals in Quercus infectoria (QI) extract have been implicated with the cytotoxic effect against various types of cancer cell which remain undiscovered. This present study aimed to evaluate cytotoxic effect of QI extracts on selected human cancer cells and then, the most potent extract was further analysed for general phytochemical constituents. QI galls were extracted successively with n-hexane, ethyl acetate and methanol yielded three main extracts; n-hexane (QIH), ethyl acetate (QIEA) and methanol (QIM), respectively. The most potent extract was qualitatively analysed for the present of tannin, alkaloids, glycosides, saponins, terpenoids, flavonoids and phenolic compounds. Next, the extracts were tested to determine the cytotoxic activity against cervical cancer cells (HeLa), breast cancer cells (MDA-MB-231) and liver cancer cells (Hep G2) using MTT assay. Cytotoxic activity of QI extracts against normal fibroblast (L929) cell line was also evaluated to determine the cytoselective property. Meanwhile, DMSO-treated cells served as negative control while cisplatin-treated cells served as positive control. The most potent extract then chosen to be further investigated for DNA fragmentation as hallmark of apoptosis using Hoechst staining. Qualitative phytochemical analysis revealed the presence of tannin, alkaloids, glycosides, saponins, terpenoids, flavonoids and phenolic compounds. QIEA extract exhibited the most potent cytotoxic activity against HeLa cells with (IC50 value = 6.33 ± 0.33 ?g/mL) and showed cytoselective property against L929 cells. DNA fragmentation revealed QIEA induced apoptosis in the treated cells. The richness of phytochemical constituents in QIEA extract might contribute to the potency of cytotoxic activity towards HeLa cells.

Project description:BackgroundCancer is a horrific disease relentlessly affecting human population round the globe. Genus Datura encompasses numerous species with reported medicinal uses. However, its potential as a source of natural anticancer agents is yet to be determined. Datura stramonium (DS) and Datura inoxia (DI) are the two species chosen for this study.MethodsTotal phenolic and flavonoid content (TPC and TFC) as well as antioxidant activity were assessed through colorimetric method. Polyphenolic quantification was done by RP-HPLC. Following extract standardization ethyl acetate leaf extracts of both species (DSL-EA and DIL-EA) were chosen for anticancer studies. In vitro cytotoxicity using various models including cancer cell lines was monitored. Following toxicity studies, benzene (0.2 ml) was used to induce leukemia in Sprague-Dawley rats. Extracts were orally administered to preventive (100 and 200 mg/kg) and treatment (200 mg/kg only) groups. The antileukemic potential of extracts was assessed through haematological, biochemical, endogenous antioxidants and histological parameters.ResultsSignificant TPC and TFC were estimated in DSL-EA and DIL-EA. RP-HPLC quantified (μg/mg extract) rutin (0.89 ± 0.03), gallic acid (0.35 ± 0.07), catechin (0.24 ± 0.02) and apigenin (0.29 ± 0.09) in DSL-EA while rutin (0.036 ± 0.004) and caffeic acid (0.27 ± 0.03) in DIL-EA. Both extracts exhibited significant brine shrimp cytotoxicity (LC50 < 12.5 μg/ml). DIL-EA exhibited greater cytotoxicity against PC-3, MDA-MB 231 and MCF-7 cell lines (IC50 < 3 μg/ml in each case) as well as higher protein kinase inhibitory action (MIC: 25 μg/disc) compared to DSL-EA. Leukemia induced in rats was affirmed by elevated serum levels of WBCs (7.78 ± 0.012 (× 103) /μl), bilirubin (7.56 ± 0.97 mg/dl), Thiobarbituric acid reactive substances (TBARs) (133.75 ± 2.61 nM/min/mg protein), decreased RBCs (4.33 ± 0.065 (× 106)/μl), platelets (344 ± 3.19 (× 103)/μl), total proteins (2.14 ± 0.11 g/dl), Glutathione S-transferases (GST) (81.01 ± 0.44 nM/min/ml), endogenous antioxidant enzymes levels and abnormal liver and kidney functionality in disease control rats. Both species revealed almost identical and significant (p < 0.05) alleviative effects in benzene induced leukemia.ConclusionComprehensive screening divulged the tremendous potential of selected species as potent source of natural anticancer agents in a variety of cancers particularly leukemia. Present study might provide useful finger prints in cancer research and mechanistic studies are prerequisite in logical hunt of this goal.

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Antitumor Effects and Related Mechanisms of Ethyl Acetate Extracts of Polygonum perfoliatum L.

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Antitumor Effects and Related Mechanisms of Ethyl Acetate Extracts of <i>Polygonum perfoliatum</i> L.

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