中文名 | 冬凌草甲素 |
英文名 | Oridonin |
别名 | 冬凌草 冬凌草素 东凌草素 冬草甲素 冬凌草甲素 冬凌草甲素(标准品) ORIDONIN 冬凌草甲素 冬凌草甲素(东凌草素,延命草宁,冬凌草) |
英文别名 | ,14r)- Oridonin ISODONAL Rubescensin rubescensin A Rabdosia rubescens (6beta,7beta)-1,6,7,14-tetrahydroxy-7,20-epoxykaur-16-en-15-one 20-epoxy-1-alpha,6-beta,7,14-tetrahydroxy-7-alph(14r)-kaur-16-en-15-on (14r)-7-alpha,20-epoxy-1-alpha,6-beta,7,14-tetrahydroxykaur-16-en-15-one kaur-16-en-15-one,7,20-epoxy-1,6,7,14-tetrahydroxy-,(1-alpha,6-beta,7-alpha (1-alpha,6-beta,7-alpha,14r)-7,20-epoxy-1,6,7,14-tetrahydroxykaur-16-en-15-o (1alpha,5beta,6beta,9beta,14S)-1,6,7,14-tetrahydroxy-7,20-epoxykaur-16-en-15-one (1alpha,5beta,6beta,7beta,9xi,10xi,14S)-1,6,7,14-tetrahydroxy-7,20-epoxykaur-16-en-15-one (1alpha,5beta,6beta,7beta,8alpha,9beta,10alpha,13alpha,14R)-1,6,7,14-tetrahydroxy-7,20-epoxykaur-16-en-15-one |
CAS | 28957-04-2 |
化学式 | C20H28O6 |
分子量 | 364.44 |
InChI | InChI=1/C20H28O6/c1-9-10-4-5-11-18-8-26-20(25,19(11,14(9)22)15(10)23)16(24)13(18)17(2,3)7-6-12(18)21/h10-13,15-16,21,23-25H,1,4-8H2,2-3H3/t10?,11?,12?,13?,15?,16-,18?,19?,20+/m0/s1 |
密度 | 1.42±0.1 g/cm3(Predicted) |
熔点 | 248-250°C |
沸点 | 599.8±50.0 °C(Predicted) |
比旋光度 | (c, 0.1 in EtOH)-47 |
闪点 | 215°C |
蒸汽压 | 6.9E-17mmHg at 25°C |
溶解度 | DMSO: >20 mg/mL |
折射率 | 1.635 |
酸度系数 | 10.96±0.70(Predicted) |
存储条件 | Sealed in dry,Room Temperature |
稳定性 | 从提供的购买之日起稳定2年。在DMSO或乙醇中的溶液可以在-20 ° 储存长达2个月。 |
外观 | 黄色固体 |
颜色 | White or off-white |
物化性质 | 来源于唇形科香茶菜属植物碎米亚桠(Rabdosia rubescens)的全草。 |
MDL号 | MFCD00221762 |
体外研究 | Oridonin有效抑制各种癌细胞的增殖,包括来自前列腺癌 (LNCaP, DU145, PC3),乳腺癌(MCF-7, MDA-MB231),非小细胞肺癌 (NSCL) (NCI-H520, NCI-H460, NCI-H1299),急性早幼粒细胞白血病(NB4),以及胶质母细胞瘤(U118, U138)的细胞增殖,ED50s的范围为1.8 to 7.5 μ克/毫升。 Oridonin的抗肿瘤活性可能是由于它对NF-κB和MAPKs信号通路的抑制作用。 |
体内研究 | LD50:小鼠35-40毫克/千克。 |
危险品标志 | Xn - 有害物品 |
风险术语 | 40 - 少数报道有致癌后果。 |
安全术语 | S36/37 - 穿戴适当的防护服和手套。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 2 |
RTECS | NZ8177000 |
海关编号 | 29389090 |
参考资料 展开查看 | 1. 汪伦记 许美秋 纠敏 等. 冬凌草提取物对金黄色葡萄球菌生物膜形成的抑制作用[J]. 天然产物研究与开发 2017 029(006):1000-1005. 2. 纠敏 孟媛媛 王倩 等. 冬凌草甲素/壳聚糖复合膜的性能和结构表征[J]. 食品与发酵工业 2019 045(024):119-123. 3. 肖香玲 何中维 黄秋月 季娟丽 张云飞 刘莹.冬凌草甲素下调EGFR/ERK/MMP-12和CIP2A/Akt信号通路抑制gefitinib耐受的非小细胞肺癌的转移[J].湖北医药学院学报 2016 35(06):536-542+629. 4. 田丽莉 朱国福 盛东来. 冬凌草甲素对人脐静脉内皮细胞的抑制作用[J]. 温州医学院学报 2017 047(012):880-883 887. 5. 纠敏 闫鹏 李晶晶 等. 冬凌草甲素对金黄色葡萄球菌生物膜的抑制机制[J]. 微生物学通报 2020 v.47(05):250-256. 6. 纠敏 闫鹏 闫国庆 等. 冬凌草甲素对金黄色葡萄球菌的抑菌作用机制[J]. 江苏农业科学 2019 47(07):202-206. 7. 田丽莉 盛东来 朱国福. 冬凌草甲素抑制血管生成活性及作用机制[J]. 中国实验方剂学杂志 2016 022(005):166-171. 8. 杜利月 郭留城 郝海军 等. 冬凌草甲素渗透泵片制备工艺研究及体外评价[J]. 中药材 2018 v.41;No.407(01):173-176. 9. 尚曙玉 张铁山 郝海军 等. 冬凌草甲素磷脂复合物不同制剂在SD大鼠体内生物利用度的比较[J]. 中药材 2019 v.42;No.422(04):170-173. 10. 何中维 肖香玲 蔡芬 张亮 黄秋月 段超 刘莹.冬凌草甲素逆转人胃癌细胞SGC 7901/DDP顺铂耐药的作用及机制研究[J].湖北医药学院学报 2016 35(03):261-265+226. 11. 李峥, 王强, 张晓莉. 蓝萼香茶菜提取溶剂的选择及其耐缺氧作用研究[J]. 中华中医药学刊, 2012, 030(006):1375-1377. 12. 王倩,纠敏,孟媛媛,孔铭杰,殷成芮,汪伦记.冬凌草甲素/壳聚糖复合膜对冰鲜鸡胸肉的保鲜效果[J].食品与机械,2021,37(03):125-130. 13. Cai, Mengru, et al. "Amino-functionalized Zn metal organic frameworks as antitumor drug curcumin carriers." New Journal of Chemistry 44.41 (2020): 17693-17704.DOIhttps://doi.org/10.1039/D0NJ03680C 14. Jushuang Li, Liping Bao, Dongqing Zha, Lian Zhang, Ping Gao, Juan Zhang, Xiaoyan Wu, Oridonin protects against the inflammatory response in diabetic nephropathy by inhibiting the TLR4/p38-MAPK and TLR4/NF-κB signaling pathways, International Immunopharmaco 15. Yang Sun, Xiubo Jiang, Ying Lu, Jianwei Zhu, Lisha Yu, Bo Ma, Qi Zhang, Oridonin prevents epithelial-mesenchymal transition and TGF-β1-induced epithelial-mesenchymal transition by inhibiting TGF-β1/Smad2/3 in osteosarcoma, Chemico-Biological Interactions, 16. Xiao, X., He, Z., Cao, W., Cai, F., Zhang, L., Huang, Q., Fan, C., Duan, C., Wang, X., Wang, J., Liu, Y."Oridonin inhibits gefitinib-resistant lung cancer cells by suppressing EGFR/ERK/MMP-12 and CIP2A/Akt signaling pathways". International Journal of Onco 17. Zhao G, Zhang T, Ma X, et al. Oridonin attenuates the release of pro-inflammatory cytokines in lipopolysaccharide-induced RAW264.7 cells and acute lung injury. Oncotarget. 2017;8(40):68153-68164. Published 2017 Jul 12. doi:10.18632/oncotarget.19249 18. Tian, L., Xie, K., Sheng, D. et al. Antiangiogenic effects of oridonin. BMC Complement Altern Med 17, 192 (2017). https://doi.org/10.1186/s12906-017-1706-3 19. [IF=5.959] Lu Ying et al."Oridonin exerts anticancer effect on osteosarcoma by activating PPAR-γ and inhibiting Nrf2 pathway."Cell Death Dis. 2018 Jan;9(1):1-16 20. [IF=5.722] Liu Qian-Qian et al."Oridonin inhibits pancreatic cancer cell migration and epithelial-mesenchymal transition by suppressing Wnt/β-catenin signaling pathway."Cancer Cell Int. 2016 Dec;16(1):1-8 21. [IF=3.723] Yang Sun et al."Oridonin prevents epithelial-mesenchymal transition and TGF-β1-induced epithelial-mesenchymal transition by inhibiting TGF-β1/Smad2/3 in osteosarcoma."Chem-Biol Interact. 2018 Dec;296:57 22. [IF=3.571] Xiangling Xiao et al."Oridonin inhibits gefitinib-resistant lung cancer cells by suppressing EGFR/ERK/MMP-12 and CIP2A/Akt signaling pathways."Int J Oncol. 2016 Jun;48(6):2608-2618 23. [IF=3.361] Jushuang Li et al."Oridonin protects against the inflammatory response in diabetic nephropathy by inhibiting the TLR4/p38-MAPK and TLR4/NF-κB signaling pathways."Int Immunopharmacol. 2018 Feb;55:9 24. [IF=2.833] Tian Lili et al."Antiangiogenic effects of oridonin."Bmc Complem Altern M. 2017 Dec;17(1):1-15 25. [IF=1.785] Tao Xu et al."Oridonin enhances in vitro anticancer effects of lentinan in SMMC‑7721 human hepatoma cells through apoptotic genes."Exp Ther Med. 2017 Nov;14(5):5129-5134 26. [IF=0] Gan Zhao et al."Oridonin attenuates the release of pro-inflammatory cytokines in lipopolysaccharide-induced RAW264.7 cells and acute lung injury."Oncotarget. 2017 Sep 15; 8(40): 68153–68164 27. [IF=6.543] Hong Mu-keng et al."Oridonin Alters Hepatic Urea Cycle via Gut Microbiota and Protects against Acetaminophen-Induced Liver Injury."Oxid Med Cell Longev. 2021;2021:3259238 28. [IF=3.591] Mengru Cai et al."Amino-functionalized Zn metal organic frameworks as antitumor drug curcumin carriers."New J Chem. 2020 Oct;44(41):17693-17704 29. [IF=3.503] Lili Tian et al."Preliminary safety assessment of oridonin in zebrafish."Pharm Biol. 2019;57(1):632-640 30. [IF=3.361] Mengru Cai et al."Functionalization of MOF-5 with mono-substituents: effects on drug delivery behavior."Rsc Adv. 2020 Oct;10(60):36862-36872 31. [IF=3] Qu Lala et al."Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay."N-S Arch Pharmacol. 2020 Jun;393(6):937-950 32. [IF=2.447] Yun Gui et al."Oridonin improves the therapeutic effect of lentinan on lung cancer."Exp Ther Med. 2021 Aug;22(2):1-9 33. [IF=2.248] Yang Huiyu et al."Selective synergistic anticancer effects of cisplatin and oridonin against human p53-mutant esophageal squamous carcinoma cells."Anti-Cancer Drug. 2022 Jan;33(1):e444-e452 34. [IF=5.811] |
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