蓝萼甲素的药理活性及其机制和毒理作用的研究进展
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摘要
蓝萼甲素(glaucocalyxin A,GLA)是一种具有对映15-氧-16贝壳杉烯(ent-15-oxo-16-kaurene)骨架结构的二萜类化合物。其具有心血管保护、内皮保护、抗凝血、抗乙肝病毒、抗肿瘤、抑菌、抗炎、耐缺氧、免疫抑制及调节钙离子浓度等多种药理作用,并且有很高的体内安全性。民间常用蓝萼香茶菜治疗肝炎、胃炎、乳腺炎、腹痛、关节痛等疾病,临床上蓝萼香茶菜主要用于治疗冠心病、心绞痛、脑供血不足等缺血、缺氧性心脑血管疾病。本研究将对蓝萼甲素的药理作用及其机制和毒理学作用做一总结。
Glaucocalyxin A(GLA)is a kind of diterpenoid enantiomers with organic chemical structure of en-15-oxo-16-kaurene.It has various pharmacological activities,such as cardiovascular and endothelium cellular protection,anti-blood coagulation,anti-Hepatitis B Virus(HBV),anti-tumor,anti-bacteria,anti-inflammation,hypoxic tolerance,immunomodulation and Ca2+concentration regulation effect,where as its in vivo safety is quite good.As a folk medicine,it is conventionally used to treat hepatitis,gastritis,mastitis,stomachache and arthralgia.It is also used for ischemic and/or hypoxic cardio-cerebrovascular diseases such as coronary heart diseases,stenocardia and chronic cerebral circulation insufficiency in clinic.This review gives a summary of the pharmacological effects,biological mechanism,and toxicity of Glaucocalyxin A.
Glaucocalyxin A(GLA)is a kind of diterpenoid enantiomers with organic chemical structure of en-15-oxo-16-kaurene.It has various pharmacological activities,such as cardiovascular and endothelium cellular protection,anti-blood coagulation,anti-Hepatitis B Virus(HBV),anti-tumor,anti-bacteria,anti-inflammation,hypoxic tolerance,immunomodulation and Ca2+concentration regulation effect,where as its in vivo safety is quite good.As a folk medicine,it is conventionally used to treat hepatitis,gastritis,mastitis,stomachache and arthralgia.It is also used for ischemic and/or hypoxic cardio-cerebrovascular diseases such as coronary heart diseases,stenocardia and chronic cerebral circulation insufficiency in clinic.This review gives a summary of the pharmacological effects,biological mechanism,and toxicity of Glaucocalyxin A.
引文
[1]余祖胤.对映贝壳杉烷类二萜化合物抗肿瘤作用及其分子机制研究[D].中国人民解放军军事医学科学院,2007.
[2]张冰月,郎轶咏,王强.蓝萼甲素抗血小板聚集的研究[J].中医药信息,2014,31(6):23-26.
[3]张雯,宋俊科,杜冠华.缺血再灌注损伤与细胞凋亡信号转导通路[J].中国药学杂志,2015,50(7):565-569.
[4]Duan X,Ji BY,Wang XH,et al.Expression of microRNA-1and microRNA-21in different protocols of ischemic conditioning in an isolatedrat heart model[J].Cardiology,2012,122(1):36-43.
[5]Kang S,Yang YJ,Wu YL,et al.Myocardium and microvessel endothelium,apoptosis at day 7following reperfused acute myocardial infarction[J].Microvasc Res,2010,79(1):70-79.
[6]刘明洁,孙旗,王强,等.蓝萼香茶菜总二萜预处理对兔心肌缺血/再灌注时心肌细胞凋亡的影响[J].中国实验方剂学杂志,2013,19(19):229-233.
[7]李上海,梁伟钧,孙炎华,等.缺血预处理对心肌缺血再灌注诱发凋亡的保护机制[J].国际心血管病杂志,2014,41(1):48-50.
[8]刘兰娣,叶丽卡,潘东军,等.蓝萼香茶菜对大鼠全心缺血-再灌注时心肌C-fos基因表达的影响[J].中国中药杂志,2003,28(4):358-361.
[9]谷洁,隋海静,李冬梅,等.内皮素与一氧化氮在2型糖尿病大鼠心肌缺血再灌注损伤中的变化及意义[J].国际免疫学杂志,2013,36(3):235-238.
[10]夏龙,褚纯隽,严彪,等.蓝萼甲素对血管内皮细胞的保护作用[J].中医药导报,2014,20(4):22-24.
[11]海广范,张慧,郭兰青.二萜类化合物药理学作用研究进展[J].新乡医学院学报,2015,32(1):77-80.
[12]王保强,丁兰,达文燕,等.蓝萼香茶菜叶与茎乙醇提取物的抑菌活性研究[J].安徽农业科学,2010,38(31):17526-17528.
[13]马占强,王敏,张健,等.蓝萼甲素抗凝血作用研究[J].云南中医学院学报,2011,34(3):26-29.
[14]朱晓红,张冰月,王莹莹,等.蓝萼香茶菜总二萜对小鼠抗凝血作用[J].中国公共卫生2013,29(1):86-87.
[15]汤晓蓉.蓝萼甲素对缺氧缺血性脑损伤保护作用的研究[D].苏州大学,2013.
[16]HasegawaY,Suzuki H,Sozen T,et al.Activation of sphingosine 1-phosphate receptor-1by FTY720is neuroprotective after ischemic stroke in rats[J].Stroke,2010,41(2):368-374.
[17]Zhou Y,Lekic T,Fathali N,et al.Isoflurane posttreatment reduces neonatal hypoxic-ischemic brain injury in rats by the sphingosine-1-phosphate/phosphatidylinositol-3-kinase/Akt pathway[J].Stroke,2010.41(7):1521-1527.
[18]刘洪川,项昭保,金永生,等.蓝萼香茶菜化学成分与结构修饰及抗肿瘤和抗乙肝病毒作用研究[C].2013中国药学大会暨第十三届中国药师周论文集,2014.
[19]王伟超.核仁蛋白EBP2反馈调控转录因子c-Myc影响rDNA转录、细胞增殖以及肿瘤形成[D].华东师范大学,2015.
[20]应娜,徐长亮,张健,等.蓝萼甲素对入肝癌细胞HepG2细胞株的作用[J].海峡药学,2012,24(1):235-238.
[21]李梦姣,顾振纶,董丽霞,等.蓝萼甲素对人肺癌A549细胞的作用及其机制[J].中国药理学通报,2013,29(6):882.
[22]Gao LW,Zhang J,Yang WH.Glaucocalyxin A induces apoptosis in human leukemia HL-60cells through mitochondriamediated death pathway[J].Toxicol in vitro,2011,25(1):51-63.
[23]刘学忠,薛彬,袁燕,等.乐果引起大鼠肝细胞凋亡的机理[J].中国兽医学报,2010,30(1):98-101.
[24]Xiong XX,Liu JM,Qiu XY,et al.Piperlongumine induces apoptotic and autophagic death of the primary myeloid leukemia cells from patients via activation of ROS-p38/JNK pathways[J].Acta Pharmacol Sin,2015,36(3):362-374.
[25]杨文华,张健,高立文,等.蓝萼甲素诱导K562细胞毒作用机制的初步研究[J].中国实验方剂学杂志,2011,17(19):181-184.
[26]黄敬敬,王修珍,蒋小岗,等.蓝萼甲素对宫颈HeLa细胞的作用及其相关机制研究[J].中国药理学通报,2012,28(3):421-424.
[27]夏维,王修珍,蒋小岗,等.蓝萼甲素对人宫颈鳞癌SiHa细胞株生长抑制作用[J].中国药理学通报,2011,27(7):1035-1036.
[28]陈子珺,李云森,周吉燕,等.蓝萼甲素对小鼠脾细胞Th1/Th2型5种细胞因子水平的影响[J].中国中药杂志,2006,31(15):1257-1260.
[29]陈子珺,李云森,周吉燕,等.蓝萼甲素对小鼠脾细胞内游离钙离子浓度的影响[J].中草药,2006,37(6):908-910.
[30]崔婷婷,赵丽娟,刘岩,等.蓝萼香茶菜的毒理学研究[J].中国医药指南,2010,08(19):246-249.
[31]沈晓丹,曹莉,董霞,等.蓝萼甲素体外细胞毒活性研究[J].中华中医药学刊,2011,29(6):1334-1335.
[2]张冰月,郎轶咏,王强.蓝萼甲素抗血小板聚集的研究[J].中医药信息,2014,31(6):23-26.
[3]张雯,宋俊科,杜冠华.缺血再灌注损伤与细胞凋亡信号转导通路[J].中国药学杂志,2015,50(7):565-569.
[4]Duan X,Ji BY,Wang XH,et al.Expression of microRNA-1and microRNA-21in different protocols of ischemic conditioning in an isolatedrat heart model[J].Cardiology,2012,122(1):36-43.
[5]Kang S,Yang YJ,Wu YL,et al.Myocardium and microvessel endothelium,apoptosis at day 7following reperfused acute myocardial infarction[J].Microvasc Res,2010,79(1):70-79.
[6]刘明洁,孙旗,王强,等.蓝萼香茶菜总二萜预处理对兔心肌缺血/再灌注时心肌细胞凋亡的影响[J].中国实验方剂学杂志,2013,19(19):229-233.
[7]李上海,梁伟钧,孙炎华,等.缺血预处理对心肌缺血再灌注诱发凋亡的保护机制[J].国际心血管病杂志,2014,41(1):48-50.
[8]刘兰娣,叶丽卡,潘东军,等.蓝萼香茶菜对大鼠全心缺血-再灌注时心肌C-fos基因表达的影响[J].中国中药杂志,2003,28(4):358-361.
[9]谷洁,隋海静,李冬梅,等.内皮素与一氧化氮在2型糖尿病大鼠心肌缺血再灌注损伤中的变化及意义[J].国际免疫学杂志,2013,36(3):235-238.
[10]夏龙,褚纯隽,严彪,等.蓝萼甲素对血管内皮细胞的保护作用[J].中医药导报,2014,20(4):22-24.
[11]海广范,张慧,郭兰青.二萜类化合物药理学作用研究进展[J].新乡医学院学报,2015,32(1):77-80.
[12]王保强,丁兰,达文燕,等.蓝萼香茶菜叶与茎乙醇提取物的抑菌活性研究[J].安徽农业科学,2010,38(31):17526-17528.
[13]马占强,王敏,张健,等.蓝萼甲素抗凝血作用研究[J].云南中医学院学报,2011,34(3):26-29.
[14]朱晓红,张冰月,王莹莹,等.蓝萼香茶菜总二萜对小鼠抗凝血作用[J].中国公共卫生2013,29(1):86-87.
[15]汤晓蓉.蓝萼甲素对缺氧缺血性脑损伤保护作用的研究[D].苏州大学,2013.
[16]HasegawaY,Suzuki H,Sozen T,et al.Activation of sphingosine 1-phosphate receptor-1by FTY720is neuroprotective after ischemic stroke in rats[J].Stroke,2010,41(2):368-374.
[17]Zhou Y,Lekic T,Fathali N,et al.Isoflurane posttreatment reduces neonatal hypoxic-ischemic brain injury in rats by the sphingosine-1-phosphate/phosphatidylinositol-3-kinase/Akt pathway[J].Stroke,2010.41(7):1521-1527.
[18]刘洪川,项昭保,金永生,等.蓝萼香茶菜化学成分与结构修饰及抗肿瘤和抗乙肝病毒作用研究[C].2013中国药学大会暨第十三届中国药师周论文集,2014.
[19]王伟超.核仁蛋白EBP2反馈调控转录因子c-Myc影响rDNA转录、细胞增殖以及肿瘤形成[D].华东师范大学,2015.
[20]应娜,徐长亮,张健,等.蓝萼甲素对入肝癌细胞HepG2细胞株的作用[J].海峡药学,2012,24(1):235-238.
[21]李梦姣,顾振纶,董丽霞,等.蓝萼甲素对人肺癌A549细胞的作用及其机制[J].中国药理学通报,2013,29(6):882.
[22]Gao LW,Zhang J,Yang WH.Glaucocalyxin A induces apoptosis in human leukemia HL-60cells through mitochondriamediated death pathway[J].Toxicol in vitro,2011,25(1):51-63.
[23]刘学忠,薛彬,袁燕,等.乐果引起大鼠肝细胞凋亡的机理[J].中国兽医学报,2010,30(1):98-101.
[24]Xiong XX,Liu JM,Qiu XY,et al.Piperlongumine induces apoptotic and autophagic death of the primary myeloid leukemia cells from patients via activation of ROS-p38/JNK pathways[J].Acta Pharmacol Sin,2015,36(3):362-374.
[25]杨文华,张健,高立文,等.蓝萼甲素诱导K562细胞毒作用机制的初步研究[J].中国实验方剂学杂志,2011,17(19):181-184.
[26]黄敬敬,王修珍,蒋小岗,等.蓝萼甲素对宫颈HeLa细胞的作用及其相关机制研究[J].中国药理学通报,2012,28(3):421-424.
[27]夏维,王修珍,蒋小岗,等.蓝萼甲素对人宫颈鳞癌SiHa细胞株生长抑制作用[J].中国药理学通报,2011,27(7):1035-1036.
[28]陈子珺,李云森,周吉燕,等.蓝萼甲素对小鼠脾细胞Th1/Th2型5种细胞因子水平的影响[J].中国中药杂志,2006,31(15):1257-1260.
[29]陈子珺,李云森,周吉燕,等.蓝萼甲素对小鼠脾细胞内游离钙离子浓度的影响[J].中草药,2006,37(6):908-910.
[30]崔婷婷,赵丽娟,刘岩,等.蓝萼香茶菜的毒理学研究[J].中国医药指南,2010,08(19):246-249.
[31]沈晓丹,曹莉,董霞,等.蓝萼甲素体外细胞毒活性研究[J].中华中医药学刊,2011,29(6):1334-1335.