Objective： To evaluate anti-melanoma effect of ethanol extract of Ilex hainanensis Merr. （IME） and elucidate its underlying mechanism. Methods： Thirty-six tumor-bearing mice were randomized into 6 groups （n=6） a...Objective： To evaluate anti-melanoma effect of ethanol extract of Ilex hainanensis Merr. （IME） and elucidate its underlying mechanism. Methods： Thirty-six tumor-bearing mice were randomized into 6 groups （n=6） as follows： model group, IME 25, 50, 100, and 200 mg/kg groups and dacarbazine （DTIC） 70 mg/kg group. The mice in the IME treatment groups were intragastrically administered with IME 25, 50, 100 or 200 mg/kg per day, respectively. The mice in the DTIC group were intraperitoneally injected with DTIC 70 mg/kg every 2 days. The drug administration was lasting for 14 days. The cell viability was evaluated by 3-（4,5-dime-thylthylthiazol-2-yl）-2, 5-diphenyl-tetrazolium bromide （MTT） assay. Flow cytometry was employed to detect cell cycle and apoptosis. The gene and protein expressions of nuclear factor κB-p65 （NF-κB-p65）, Bcl-2, B-cell lymphoma-extra large （Bcl-xL） and Bax were detected by quantitative real-time polymerase chain reaction and Western blot analyses. Caspases-3, -8, and -9 activities were detected using the colorimetric method. In addition, a B16-F10 melanoma xenograft mouse model was used to evaluate the anti-cancer activity of IME in vivo. Furthermore, a survival experiment of tumor-bearing mice was also performed to evaluate the possible toxicity of IME. Results： IME significantly inhibited the proliferation of B16-F10 cells （P〈0.01）. Flow cytometric analysis showed that IME induced G1/S cell cycle arrest and apoptosis （both P〈0.01）. IME inhibited activation of NF-κB, decreased the gene and protein expressions of Bcl-2, Bcl-xL, and increased the gene and protein expressions of Bax （all P〈0.01）. In addition, IME induced the activation of Caspases-3, -8, and -9 in B16-F10 cells. The study in vivo showed that IME significantly reduced tumor volume （P〈0.01）, and the inhibitory rate came up to 68.62%. IME also induced large areas of necrosis and intra-tumoral apoptosis that correlated with a reduction in tumor volume. Survival experiment showed that treatment with IME for 14 days significantly prolonged survival time and 20% of mice in the IME 200 mg/kg group were still alive until the 50th day. Notably, IME showed no apparent side-effects during the treatment period. Conclusion： IME exhibited significant anti-melanoma activity in vitro and in vivo, suggesting that IME might be a promising effective candidate with lower toxic for malignant melanoma therapy.展开更多
[Objectives] This study aimed to investigate the hypolipidemic effects of different processed products of Ilex hainanensis Merr to provide experimental basis for the research on the hypolipidemic mechanism of I. haina...[Objectives] This study aimed to investigate the hypolipidemic effects of different processed products of Ilex hainanensis Merr to provide experimental basis for the research on the hypolipidemic mechanism of I. hainanensis Merr. [Methods] SD rats were fed high-fat diet to establish hyperlipidemia rat models. The hyperlipidemia rats were administered with different processed products of I. hainanensis Merr by gavage to investigate the preventive and therapeutic effects of the medicinal material. [Results] The levels of total cholesterol(TC), triglyceride(TG), low density lipoprotein cholesterol(LDL-C) in the rats fed high-fat diet were significantly higher than those in of the control group(P<0.01), indicating successful modeling. Among different processing methods, the hypolipidemic effects were in the order as baking=traditional processing=frying=microwaving>drying in shade. Among different baking times, the hypolipidemic effects ranked as 180 ℃>200 ℃=220 ℃. Among different baking times, the hypolipidemic effects ranked as 20 min=40 min>30 min. The hypolipidemic effects of processed product of I. hainanensis Merr with different amounts of active ingredients were different. [Conclusions] The processed products of I. hainanensis Merr all had hypolipidemic effects, but the effects were different. This study will provide a scientific basis for expanding the resources of I. hainanensis Merr.展开更多
文摘Objective： To evaluate anti-melanoma effect of ethanol extract of Ilex hainanensis Merr. （IME） and elucidate its underlying mechanism. Methods： Thirty-six tumor-bearing mice were randomized into 6 groups （n=6） as follows： model group, IME 25, 50, 100, and 200 mg/kg groups and dacarbazine （DTIC） 70 mg/kg group. The mice in the IME treatment groups were intragastrically administered with IME 25, 50, 100 or 200 mg/kg per day, respectively. The mice in the DTIC group were intraperitoneally injected with DTIC 70 mg/kg every 2 days. The drug administration was lasting for 14 days. The cell viability was evaluated by 3-（4,5-dime-thylthylthiazol-2-yl）-2, 5-diphenyl-tetrazolium bromide （MTT） assay. Flow cytometry was employed to detect cell cycle and apoptosis. The gene and protein expressions of nuclear factor κB-p65 （NF-κB-p65）, Bcl-2, B-cell lymphoma-extra large （Bcl-xL） and Bax were detected by quantitative real-time polymerase chain reaction and Western blot analyses. Caspases-3, -8, and -9 activities were detected using the colorimetric method. In addition, a B16-F10 melanoma xenograft mouse model was used to evaluate the anti-cancer activity of IME in vivo. Furthermore, a survival experiment of tumor-bearing mice was also performed to evaluate the possible toxicity of IME. Results： IME significantly inhibited the proliferation of B16-F10 cells （P〈0.01）. Flow cytometric analysis showed that IME induced G1/S cell cycle arrest and apoptosis （both P〈0.01）. IME inhibited activation of NF-κB, decreased the gene and protein expressions of Bcl-2, Bcl-xL, and increased the gene and protein expressions of Bax （all P〈0.01）. In addition, IME induced the activation of Caspases-3, -8, and -9 in B16-F10 cells. The study in vivo showed that IME significantly reduced tumor volume （P〈0.01）, and the inhibitory rate came up to 68.62%. IME also induced large areas of necrosis and intra-tumoral apoptosis that correlated with a reduction in tumor volume. Survival experiment showed that treatment with IME for 14 days significantly prolonged survival time and 20% of mice in the IME 200 mg/kg group were still alive until the 50th day. Notably, IME showed no apparent side-effects during the treatment period. Conclusion： IME exhibited significant anti-melanoma activity in vitro and in vivo, suggesting that IME might be a promising effective candidate with lower toxic for malignant melanoma therapy.
基金Supported by National Natural Science Foundation of China(81060344,81660701)Guangxi Natural Science Foundation(2016GXNSFAA380148)+2 种基金Screening and Development of Medicinal Materials Containing Stepholidine(H14002)Guangxi Key Laboratory of Efficacy Study on Chinese Materia Medica(17-259-20)Laboratory of Chemical and Quality Analysis of Chinese(Zhuang) Medicine in the Research and Development Laboratory(Level 3) of the State Administration of Traditional Chinese Medicine(Guo Zhong Yi Yao Fa 2009[21])
文摘[Objectives] This study aimed to investigate the hypolipidemic effects of different processed products of Ilex hainanensis Merr to provide experimental basis for the research on the hypolipidemic mechanism of I. hainanensis Merr. [Methods] SD rats were fed high-fat diet to establish hyperlipidemia rat models. The hyperlipidemia rats were administered with different processed products of I. hainanensis Merr by gavage to investigate the preventive and therapeutic effects of the medicinal material. [Results] The levels of total cholesterol(TC), triglyceride(TG), low density lipoprotein cholesterol(LDL-C) in the rats fed high-fat diet were significantly higher than those in of the control group(P<0.01), indicating successful modeling. Among different processing methods, the hypolipidemic effects were in the order as baking=traditional processing=frying=microwaving>drying in shade. Among different baking times, the hypolipidemic effects ranked as 180 ℃>200 ℃=220 ℃. Among different baking times, the hypolipidemic effects ranked as 20 min=40 min>30 min. The hypolipidemic effects of processed product of I. hainanensis Merr with different amounts of active ingredients were different. [Conclusions] The processed products of I. hainanensis Merr all had hypolipidemic effects, but the effects were different. This study will provide a scientific basis for expanding the resources of I. hainanensis Merr.
