Xiaomin Yi

Anticancer activities of harmine by inducing a pro-death autophagy and apoptosis in human gastric cancer cells

BACKGROUND Harmine, a β-carboline alkaloid from Peganum harmala, has multiple anti-tumor activities, especially for its folk therapy for digestive system neoplasm. However, the underlying mechanism of harmine on gastric cancer remains unclear. PURPOSE To illuminate the potential anti-tumor activity and mechanism of harmine against gastric cancer cells. METHODS/STUDY DESIGNS The anti-proliferative activity of harmine in vitro was evaluated by MTT assay. The autophagic activity induced by harmine was assessed using GFP-LC3 transfection. FITC/PI double staining was applied for the apoptosis inspection. The mitochondrial membrane potential was detected by JC-1 fluorescence probe. The potential mechanisms for proteins level in autophagy and apoptosis were analyzed by Western blot. RESULTS Harmine exhibited potent effects on both autophagy and apoptosis. Treatment with harmine could enhance dots of GFP-LC3 in cells. Meanwhile, the process had connection with Beclin-1, LC3-II, and p62 by the inhibition of Akt/mTOR/p70S6K signaling. However, high concentration of harmine led to apoptosis characterized by the propidium/Annexin V-positive cell pollution, cell shrunk and the collapse of mitochondrial membrane potential. The regulation of Bcl-2, Bax and the gathering of cleaved-PARP, cleaved-caspase 3 and cleaved-caspase 9 contributed to the induction of apoptosis. In addition, 10μM LY294002 (a specific inhibitor of PI3K/Akt) combination with 40μM harmine significantly increased the cytotoxicity to the gastric cancer cells and up-regulated both the apoptosis-related protein (cleaved-PARP, cleaved-caspase-3) and autophagy-related protein (Beclin-1, LC3-II, and p62). Adding the inhibitor of autophagy, 3-MA or BafA1, increased the viability of harmine-exposured gastric cancer cells, which confirmed the role of autophagy played in the gastric cancer cell death induced by harmine. CONCLUSION Harmine might be a potent inducer of apoptosis and autophagy, which offered evidences to therapy of harmine in gastric carcinoma in the folk medicine.

Antiproliferative and anti-inflammatory furostanol saponins from the rhizomes of Tupistra chinensis

Phytochemical investigations of the rhizome of Tupistra chinensis led to the isolation of ten new furostanol saponins along with fourteen known spirostanols. Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against FaDu and Detroit 562 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compound 14 exhibited significant antiproliferative effects against FaDu and Detroit 562 cells with IC50 values of 1.1±0.1 and 1.2±0.1μM, respectively. Compounds 1, 2, 6, 13, 16, 19 and 24 exhibited inhibitory effects on NO production with IC50 values ranging from 15.7 to 46.2μM.

Antiproliferative and anti-inflammatory polyhydroxylated spirostanol saponins from Tupistra chinensis.

Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Its chemical identity of potent antiproliferative and anti-inflammatory constituents has been carried out in this study. Twenty-three polyhydroxylated spirostanol saponins, including nine novels, were isolated and identified. The new spirostanol saponins were elucidated as spirost-25(27)-en-1β,2β,3β,4β,5β-pentol-2-O-β-D-xylopyranoside (1), spirost-25(27)- en-1β,2β,3β,4β,5β-pentol-2-O-α-L-arabinopyranoside (2), spirost-25(27)-en- 1β,3α,5β-triol (12), spirost-25(27)-en-1β,3α,4β,5β,6β-pentol (13), spirost-25(27)-en- 1β,2β,3β,5β-tetraol-5-O-β-D-glucopyranoside (16), 5β-spirost-25(27)-en-1β,3β-diol- 3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (17), (25R)-5β-spirostan- 1β,3β-diol-3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranoside (18), (25R)-5β- spirostan-1β,3β-diol-3-O-β-D-fructofuranosyl-(2 → 6)-β-D-glucopyranoside (19), 5β-spirost-25(27)-en-3β-ol-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (20). The antiproliferative effects against seven human cancer cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compounds 17, 19 and 21 exhibited potential antiproliferative activities against all of human cancer cell lines tested. Compounds 21 showed significant inhibition on NO production with IC50 values of 11.5 μM. These results showed that the spirostanol saponins isolated from the dried rhizomes of T. chinensis have potent antiproliferative and anti-inflammatory activities and T. chinensis might be used as anticancer and.anti-inflammatory supplement.

Bioactive spirostanol saponins from the rhizome of Tupistra chinensis.

Phytochemical investigations of the rhizome of Tupistra chinensis led to the isolation of six new spirostanol saponins, one new spirostanol, along with eight known spirostanols. Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against five human cancer cell lines were assayed for all the isolated compounds. Compounds 8, 12 and 15 showed potent cytotoxic activities against K562 cells. The isolated compounds were evaluated for their inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in a macrophage cell line RAW 264.7. Compounds 2 and 12 showed significant inhibition on NO production with IC50 values of 16.1±1.8 and 13.5±1.2 μM, respectively.

Anti-inflammatory lignanamides and monoindoles from Alocasia macrorrhiza

Five new lignanamides (1-5), and one new monoindole alkaloid (6), along with eight known compounds (7-14) were isolated and identified from the rhizomes of Alocasia macrorrhiza (giant taro). All purified compounds were evaluated for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, and the antiproliferative activities against human nasopharyngeal carcinoma epithelial (CNE-1), human gastric carcinoma (MGC-803), and human breast cancer (MCF-7) cell lines by MTT method. Compounds 2, 4, 7 and 8 exhibited significant inhibitory effects on NO production with the IC50 values of 2.35±0.38, 9.20±0.94, 3.45±0.39 and 7.96±0.56μM, respectively. The results suggested the lignanamides and monoindoles might be responsible for the anti-inflammatory activity of giant taro and might be potential anti-inflammatory candidates.

Anti-inflammatory steroidal glycosides from the berries of Solanum nigrum L. (European black nightshade)

Seven previously undescribed steroidal glycosides, along with three known congeners were isolated from the unripe berries of Solanum nigrum L. (Solanaceae). Their structures were elucidated on basis of 1D and 2D NMR, HR-ESI-MS spectroscopic data and GC analysis after acid hydrolysis. The potential inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide in RAW 264.7 cell line and the anti-proliferative activities against five cancer cell lines (HL-60, U-937, Jurkat, K562 and HepG2) were evaluated. Seven compounds exhibited inhibition activities on NO production with IC50 values ranging from 11.33 to 49.35 μM. Structure-activity relationships of the isolated compounds were also discussed.

Novel triterpenoids and glycosides from durian exert pronounced anti-inflammatory activities

Durian, known for its abundant nutrition, is a delicious fruit from Southeast Asia with increasing popularity worldwide. In this study, a series of chromatographic methods and bioactivity assays were applied to identify major compounds from durian shells. Two new triterpenoids, two new phenolics, and seven new glycoside esters, as well as sixteen known compounds, were isolated and identified. Anti-inflammatory activities were assayed and evaluated for the isolated compounds. Most of the isolated compounds exhibited pronounced inhibitory activities on lipopolysaccharides-induced NO production in RAW 264.7 cells. The results indicated that durian shells could serve as anti-inflammatory agents for functional food or medicinal use. This study additionally provided motivation for the ecological protection of durian shells.

Anti-inflammatory phenylpropanoids and phenolics from Ficus hirta Vahl.

Four new phenylpropanoids (1-4) along with ten known phenolics were isolated and purified from the roots of hairy fig (Ficus hirta Vahl.). Their structures were elucidated by the extensive spectroscopic analysis and chemical degradation. The anti-inflammatory activities of the purified compounds were evaluated. Results indicated that the extracts and some purified compounds exhibited pronounced inhibitory effects on the lipopolysaccharides (LPS) induced nitric oxide (NO) production in murine macrophage RAW 264.7 compared to indomethacin, which suggested that hairy fig could be served as an anti-inflammatory agent for health products.

Hepatoprotective and Antioxidant Effects of Total Triterpenoids from Poria cocos

Aims: To prepare the Poria cocos total triterpenoids (PCTT) from the surface layer of Poria cocos and evaluate its pharmacological effect on alcohol induced-liver injury. Study Design: PCTT was prepared from the surface layer of Poria cocos and characterized. Its effects on alcohol induced-liver injury models were investigated in vitro and in vivo. Place and Duration of Study: School of Pharmacy, Guangdong Pharmaceutical University, between January 2014 and March 2014. Methodology: PCTT was prepared via D101 macroporous resin chromatography and characterized by high performance liquid chromatography. The hepatoprotective and antioxidant effects of PCTT against alcohol induced-liver injury were investigated in L-02 cell line and mice. Results: PCTT containing 63.95% triterpenoids showed potent radical-scavenging activities in vitro. PCTT (10 μg/mL and 20 μg/mL) treatments increased the viability of cells significantly in alcohol-treated L-02 cells. In vivo, pretreated with PCTT suppressed the acute ethanol gavage induced increase of the serum aminotransferase (AST), aminotransferase (ALT) levels and liver triacylglycerol (TG) level in mice. Simultaneously, PCTT also enhanced the glutathione peroxidase Original Research Article Wang et al.; EJMP, 21(2): 1-9, 2017; Article no.EJMP.37908 2 (GSH-Px) activity and restored glutathione (GSH) level in liver. Conclusion: This study suggests that PCTT, containing 63.95% triterpenoids, could significantly improve the impairments of liver induced by alcohol and suitable for alcohol induced-liver injury patients as medicine or functional food, which would be a new candidate for the treatment of alcohol liver disease (ALD).