Cardioprotection and mechanism of embelin in sepsis mice model / 预防医学

Objective To observe the effect of embelin on the cardiac injury in sepsis mice model, and to explore whether PPAR-participates in the mechanism of cardioprotection of embelin.Methods Male mice were randomly divided into five groups.Control group were received PBS i.p.injection.Sepsis model group were received LPS (10 mg/kg) i.p.injection.Embelin treatment groups were received LPS (10 mg/kg) i.p.injection, and after 30 min different doses of embelin were given (5, 10, and 20 mg/kg, i.p.).Results The serum cTnI level and TNF-α、NF-κB protein in low dose embelin (5 mg/kg) treatment mice was not different with that of the sepsis mice.But the serum cTnI level and TNF-α、NF-κB protein in middle and high doses embelin (10, 20 mg/kg) treatment mice was lower than that of sepsis mice, and the expression of PPAR-γ was higher(P<0.05).Conclusion Embelin could protect against sepsis-induced cardiac injury.The mechanism might be involved in the upregulation of PPAR-γ protein, inhibition of NF-κB activation,and reduction of TNF-α level.

Quantitative reckoning of embelin from fruits of Embelia tsjeriam- cottam using water bath process as an alternate method of extraction.

The world is culturally endowed with various forms of healing practices having rich medical wisdom of immense importance. One of such pharmacognostically indispensable medicinal plant is Embelia tsjeriam-cottam A. DC. The active principle of E. tsjeriam-cottam is embelin, possessing a range of pharmacognostic activities including anti-cancer, antioxidant, antiinflammation, antibacterial and analgesic effects. Embelin in fruits of E tsjeriam-cottam was extracted using water bath method. For extraction of embelin from fruits of E. tsjeriamcottam, methanol and chloroform were used as solvents. Fruits were collected from five different agro-climatic zones of Odisha. Comparative estimation of embelin was done through spectrophotometer and High Performance Liquid Chromatographic (HPLC) methods. Samples extracted with chloroform and methanol showed embelin content in a range of 2.13- 0.29% dry wt., and 0.95-0.28% dry wt. respectively using spectrophotometer. In case of HPLC analysis, samples extracted in chloroform and methanol showed embelin content in a range of 1.86-0.27% dry wt., and 0.875-0.26% dry wt. respectively. However the water bath method, used as alternative method for extraction, proved to be less time consuming, costeffective in extracting a pretty good amount of embelin as compared to the conventional (soxhlet) methods of extraction.

Synthesis and Evaluation of Analgesic and Anti-inflammatory Activities of Most Active Antioxidant Derivatives of Embelin.

Objective: To evaluate antioxidant, analgesic and anti-inflammatory properties of embelin and its derivatives. Methods: In the present study embelin was condensed with various aliphatic substituted primary amines, hydrazines and amino acids to yield seven new and five reported derivatives. All these compounds along with embelin were evaluated for in vitro antioxidant activity using ABTS and DPPH methods. Potent compounds were selected for in vivo analgesic and anti-inflammatory activities. Results: Hydrazines, amino acids substituted embelin derivatives and phenazines showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and its derivatives almost completely abolished the acetic acid induced writhing. Phenyl alanine and phenazine derivative showed better anti-inflammatory activity than embelin. Conclusion: Further research would be of interest to explain the exact mechanism of these compounds and chemical modifications, biological screening and toxicity studies can also be explored.

Evaluating the effect of embelin combined with paclitaxel on inhibiting A549 lung cancer cell proliferation and tumor growing in tumor-bearing nude mice growing / 中国生化药物杂志

Objective To evaluate the effect of embelin combined with paclitaxel on the inhibition of A 549 lung cancer cell proliferation and tumor growing in tumor bearing nude mice. Methods The anti-proliferation efficiency of embelin combined with paclitaxel were evaluated by MTT assay, and A 549 cell apoptosis were evaluated by lfow cytometry. A 549 cells were xenografted in mice to establish the animal model, which were used to evaluate the effect of anti-tumor. Results compared to saline group、embelin group and paclitaxel group, the (paclitaxel+embelin) group could inhibit the growth of A 549 cells effectively(P<0.05). The embelin combined with paclitaxel induced the apoptosis of A 549 cells more effective than paclitaxel alone. The (paclitaxel+embelin) group significantly inhibited the growth of tumor tissue. Conclusion the paclitaxel can inhibit the growth of A 549 cells, the embelin can induce the apoptosis of A 549 cells, and the combination of paclitaxel and embelin may be a potentially effective treatment for lung cancer.

Effect of embelin and doxorubicin on the proliferation of MCF-7 cell and growth of MCF-7 bearing nude mice / 中国生化药物杂志

Objective To explore the effect of X-linked inhibitor of apoptosis protein(XIAP)combined with doxorubicin on the proliferation of MCF-7 cell and growth of MCF-7 bearing nude mice.Methods The anti-proliferation efficiency of doxorubicin and embelin were determined by MTT assay.MCF-7 cell apoptosis induced by embelin and doxorubicin were detected by Flow cytometry.Anti-tumor ability of embelin and doxorubicin were evalued with tumor spheroids test.MCF-7 cell were xenografted to mice to establish the animal model,which was used to evaluate the effect of anti-tumor. Results Compared with saline group,embelin group and doxorubicin group,the combination(doxorubicin +embelin)group inhibited the growth of MCF-7 cells effectively(P<0.01).The combination group induced the apoptosis of MCF-7 cells more effectively than doxorubicin alone(P<0.01), and significantly inhibit the growth of tumor in vitro and in vivo than other groups(P<0.01).Conclusion The combination of doxorubicin and embelin may be used as a potentially effective treatment method for breast cancer.

The effects of XIAP siRNA and embelin on TRAIL-induced growth inhibition and apoptosis in hepatocarcinoma cells / 中华肝胆外科杂志

ObjectiveTo investigate the effects of X-linked inhibitor of apoptosis (XIAP) siRNA or XIAP antagonist Embelin on the growth inhibition and apoptosis of hepatcellular cancer cell line HepG2,which was treated by tumor necrosis factor-related apoptosis (TRAIL). Methods HepG2 cells were tranfected either by XIAP siRNA or a negative control,followed by treatment with TRAIL,Embelin or a combination of the two.XIAP expression,cell growth,and caspase-3 activity were determined by Western blot,MTT assay and fluorescent caspase-3 assay,respectively.Cleaved PARP expression levels of were measured by Western blot.ResultsThe XIAP protein expression was significantly downregulated by transfection with XIAP siRNA.Compared with the negative control,the XIAP siRNA significantly inhibited the growth of HepG2 cells treated by 100ng/ml(6.8％ ±1.2％ vs.11.8％±4.0％,P＜0.05)and 1000 ng/ml (18.9％ ±2.0％ vs.26.6％ ±1.5％,P＜0.01)by TRAIL.TRAIL-induced caspase-3 activation and PARP cleavage were also increased significantly by XIAP siRNA transfection.In addition,Embelin also significantly inhibited cell growth (P＜0.01),activation of caspase-3 (P＜ 0.01) and TRAIL-induced PARP cleavage.Conclusions Both XIAP siRNA and Embelin may potentially contribute to clinical treatment of hepatocellular carcinoma.

The effect of small molecule anatagonists of XlAP(Embelin)on the multidrug resistance cells SGC7901 / 重庆医科大学学报

90% by MTT assay,in vivo experiment tumor weight inhibition rates were93.514 4,90.719 2,96.592 3respectivly. Conclusion:Embelin was good for cells SGC7901,especial for a low dose combination with VCR.