Anticancer effect of petroleum ether extract from Bidens pilosa L and its constituent's analysis by GC-MS.

Bidens pilosa L, belonging to the family of Acanthaceae, has been used as an anticancer medicine in folk in China. In our preliminary experiments, the petroleum ether extract from B. pilosa showed good cytotoxic activity to human lung cancer A549 cell. However, to date, it's lack of the further study on antitumor effect, mechanism and active substances composition of the petroleum ether extract of B. pilosa. The study aimed to evaluate the anti-lung cancer efficacy of the petroleum ether extract from B. pilosa (PEEBP) in vitro and in vivo, explore the possible anticancer mechanisms, and further disclose the chemical composition of the extract. B. pilosa was extracted with 75% ethanol (v/v), followed by extracted with petroleum ether to obtain the objective fraction. Antiproliferation effect of the petroleum ether extract in HepG2, A549, CNE and B16 cells was evaluated by MTT assay. The in vivo anticancer effect was examined by A549 cells nude mice xenograft tumor model. The possible effect mechanism was studied by western blot assay. The chemical constituents of the extract was analyzed by GC-MS. The petroleum ether extract showed favorable antiproliferation activity against the four human cancer cell lines, especially for A549 cells with an IC50 of 49.11 ± 2.72 μg/mL. The extract inhibited the growth of A549 cell in mice with the inhibitory rates of 24.76%, 35.85% and 53.07% for 90, 180 and 360 mg/kg oral dosages, respectively. The B. pilosa extract could significantly down-regulate the expression of apoptosis-related protein Bcl-2 and up-regulate the protein expression of Bax and Caspase-3. 138 compounds were identified by GC-MS in the extract and the main chemical components were triterpenes, including 4,22-cholestadien-3-one (4.82%), stigmasterol (4.56%), friedelan-3-one (3.28%), etc. The PEEBP is abundant of triterpenes and has significant anti-tumor activities against human A549 cells in vitro and in vivo, indicating it a potential anticancer agent.

Shen Y ，Sun Z ，Shi P ，Wang G ，Wu Y ，Li S ，Zheng Y ，Huang L ，Lin L ，Lin X ，Yao H ... -  《-》

Ethyl acetate extract from Selaginella doederleinii Hieron inhibits the growth of human lung cancer cells A549 via caspase-dependent apoptosis pathway.

Selaginella doederleinii Hieron has been used as a folk medicine for the treatment of different cancers, especially for nasopharyngeal carcinoma, lung cancer and trophoblastic tumor in China. Previously, the ethyl acetate extract from S. doederleinii (SDEA extract) showed favorable anti-cancer potentials. However, the main chemical composition and anticancer mechanism of the SDEA extract were still not very clear. Until now, there are no reports available about the oral toxicity of the extract. The present study was to further elucidate the chemical composition and anti-lung cancer mechanism of the SDEA extract, and evaluate the acute oral toxicity of the extract. The SDEA extract was separated and analysed by HPLC to disclose its main chemicals. The effects of the extract were then investigated in vitro on cell viability, apoptosis and cell cycle using fluorescence microscopy and flow cytometry, and the molecular mechanism against human lung cancer cells A549 was further studied by western blot assays. The in vivo anti-cancer effect of the extract was evaluated in A549 xenograft mice model by histochemical assay, and tumor growth, microvascular density (MVD) and Ki67 expression were also measured. In addition, acute oral toxicity test of the extract was executed in mice. SDEA extract mainly contained eight biflavonoids. The extract caused the loss of mitochondrial membrane potential and induced cell apoptosis by upregulating Bax, downregulating Bcl-2, activating caspase-9 and caspase-3 and blocked the cell cycle in S phase. The extract reduced expression of antigen Ki67, decreased MVD, and significantly inhibited the tumor growth. The extract did not show apparent oral acute toxicity in healthy mice. The SDEA extract exerted anti-tumor effect through activating mitochondrial pathways and reducing Ki67 expression and MVD. Low oral acute toxicity suggested it a promising chemotherapy agent.

Sui Y ，Li S ，Shi P ，Wu Y ，Li Y ，Chen W ，Huang L ，Yao H ，Lin X ... -  《-》

Pharmacological potential of Bidens pilosa L. and determination of bioactive compounds using UHPLC-QqQ(LIT)-MS/MS and GC/MS.

Singh G ，Passsari AK ，Singh P ，Leo VV ，Subbarayan S ，Kumar B ，Singh BP ，Lalhlenmawia H ，Kumar NS ... -  《BMC Complementary and Alternative Medicine》

The petroleum ether extracts of Chloranthus fortunei(A. Gray) Solms-Laub.with bioactivities: A rising source in HCC drug treatment.

Hepatocellular Carcinoma (HCC) is an aggressive killer worldwide with high incidence and mortality. The herb Chloranthus fortunei (A. Gray) Solms-Laub is known as "Si Ji Feng" and is classified as a Feng-type medicine in classic Yao medicines. According to Yao's medical beliefs, Chloranthus fortunei has the functions of dispelling Feng, regulating qi, detoxifying, promoting blood circulation, etc. Folk uses its decoctions to treat stagnant liver conditions, such as liver abscesses, cirrhosis, hepatitis, and liver cancer. However, the bioactivity and mechanisms of Chloranthus fortunei extract against HCC have not been reported. To investigate the anti-HCC bioactivity and potential mechanism of the extract of Chloranthus fortunei (CFS). Using 70% ethanol for reflux extraction of CFS resulted in the CFS ethanol extract, followed by sequential extractions with petroleum ether, chloroform, ethyl acetate, and n-butanol, yielding four fractions. The CCK-8 assay was utilized to examine the cytotoxic effects of 4 fractions on MHCC97-H and HepG2 cells, exploring the most effective component, namely petroleum ether extracts of CFS (PECFS). The major active ingredients of PECFS were identified using LC/MS technology, and the impact on cell proliferation and apoptosis in HCC cells was studied. The key genes and proteins in the pathway were validated using RT-PCR and Western blotting. BALB/c nude mice were chosen for tumor xenotransplantation and PECFS therapy. hinders the proliferation of HCC cells and promotes apoptosis. Among the four fractions, it was found that PECFS have the highest antiproliferative activity against MHCC97-H and HepG2 cells (IC50 = 13.86, 10.55 μg/mL), with sesquiterpene compounds being the primary active constituents. The antiproliferative activity of PECFS on HCC cells was linked to the inhibition of cell cloning, invasion, and metastasis abilities, as well as the arrest of the cell cycle at the G2/M phase. Additionally, exerts pro-apoptotic effects on HCC cells by upregulating the pro-apoptotic protein Bax, downregulating the anti-apoptotic protein Bcl-2, and activating the expression of the Caspase family. Moreover, protein and m-RNA expression data showed that PECFS inhibits HCC cell proliferation and promotes apoptosis by regulating the PI3K/AKT/mTOR pathway. Besides, after PECFS treatment, tumor growth in nude mice was suppressed. PECFS can inhibit the viability of HCC cells by acting on the PI3K/AKT/mTOR pathway, demonstrating anti-tumor potential. This study's findings suggest that PECFS may represent a promising source of novel agents for liver cancer treatment, providing scientific evidence for the traditional application of CFS in treating HCC.

Gong X ，Zhou Y ，Wu P ，He L ，Ou C ，Xiao X ，Hou X ，Shen Y ，Li M ，Tan Z ，Xia X ，Wang S ... -  《-》

Antitumor effects and chemical compositions of Eupolyphaga sinensis Walker ethanol extract.

Eupolyphaga sinensis Walker popularly known as "preferred drug to regulate blood flow" are traditionally used in folk medicine in the treatment of ecchymoma, posttraumatic wound, hepatic fibrosis and tumor. To characterize chemical compositions and to evaluate the antitumor and immunomodulatory of Eupolyphaga sinensis Walker ethanol extract (ESEE) in hepatocarcinoma H(22) bearing mice. ESEE was obtained by ethanol reflux extraction and analyzed by gas chromatography-mass spectrometry (GC-MS) after methylation. ICR mice were treated with ESEE for 14 consecutive days at doses of 31mg/kg (low-dose), 62mg/kg (mid-dose) and 124mg/kg (high-dose) after H(22) tumor cells were implanted. At the end of the experiments, the tumor weight of each mouse was measured. Levels of serum TNF-α and IFN-γ was assayed by ELISA. Protein expressions of Bax, Bcl-2 and caspases-3 were detected by immunohistochemistry. Chemical analysis revealed the presence of 6 components that account for 97.55% of fatty acids, indicating the occurrence of saturated and polyunsaturated fatty acids. Oral administration of ESEE could inhibit tumor growth, promote Th1 type cytokine productions (TNF-α and IFN-γ) and induce apoptosis of hepatocarcinoma via increase of Bax/Bcl-2 ratio and activation of caspases-3. Oral administration of ESEE in a dosage of 6.2g/kg did not lead to toxic effects in mice. ESEE was effective in inhibiting tumor growth in vivo and could also serve as immunoadjuvant for tumor therapy.

Ge GF ，Yu CH ，Yu B ，Shen ZH ，Zhang DL ，Wu QF ... -  《-》