粉防己鹼

粉防己鹼
臨床資料
商品名（英語：Drug nomenclature）	金艾康、漢力達等
其他名稱	漢防己甲素
法律規範狀態
法律規範	中：處方藥 ;
藥物動力學數據
藥物代謝	肝臟
生物半衰期	2–7.5小時（靜脈注射）、0–26小時（口服）
識別資訊
	IUPAC命名法 9,20,21,25-tetramethoxy-15,30-dimethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.2³,⁶.1⁸,¹².1¹⁴,¹⁸.0²⁷,³¹.0²²,³³]hexatriaconta-3,5,8(34),9,11,18,20,22(33),24(32),25,27(31),35-dodecaene; ;
CAS號	518-34-3
PubChem CID	73078;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID10178062 ;
ECHA InfoCard	100.208.615
化學資訊
化學式	C38H42N2O6
摩爾質量	622.74988 g/mol
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES CN1CCC2=CC(=C3C=C2C1CC4=CC=C(C=C4)OC5=C(C=CC(=C5)CC6C7=C(O3)C(=C(C=C7CCN6C)OC)OC)OC)OC;

粉防己鹼^[3]（tetrandrine，fanchinine，hanfangchin A）是一種雙苄基異喹啉類生物鹼，可從防己科植物粉防己根中和其他中草藥提取出來^[4]。具有抗炎、抗過敏、抗氧化、抗纖維化及免疫調節作用^[5]；其可抑制肥大細胞的脫粒，也有「類奎尼丁」的抗心律失常作用。另具有血管擴張特性，因此可以降低血壓^[6]。

粉防己鹼可能具有治療肝病^[7]和肝癌的潛在用途^[8]^[9]^[10]。具有預防小梁切除術後結膜炎或嚴重結膜炎症患者過度瘢痕/纖維化的潛在治療價值^[11]。粉防己鹼具有抗炎和抗纖維化作用，使得粉防己鹼和相關化合物可用於治療肺矽肺病，肝硬化和類風濕性關節炎。^[6]還表明粉防己鹼在體外抑制埃博拉病毒進入宿主細胞，並且在對小鼠的初步研究中顯示出對抗埃博拉病毒的治療功效。^[12]

生物合成

粉防己鹼是由S-N-甲基烏藥鹼的自由基偶聯二聚化生物合成的：^[13]

同義詞

其同義詞包括防己鹼、漢防己鹼A、NSC 77037、(S ,S )-(+)-粉防己鹼、青藤鹼A、TTD、四聯蛋白和d-粉防己鹼^[14] 。用作藥品時稱為漢防己甲素^[1]。

參考文獻

^ ^1.0 ^1.1 汉防己甲素片（北海阳光）. 丁香園·用藥助手.
^ Xin-Hui Jiang, Jun-Qing Yang, Na Li, Han Wang, Qi-Xin Zhou. The pharmacokinetical study of plant alkaloid tetrandrine with a simple HPLC method in rabbits. Fitoterapia. 2011-09, 82 (6): 878–882. doi:10.1016/j.fitote.2011.04.014.
^ 楊敬,朱安祥,胡軍,等. 粉防己鹼的作用機制研究進展[J]. 國際中醫中藥雜誌,2018,40:(3)：286-289. DOI:10.3760/cma.j.issn.1673-4246.2018.03.025
^ Zhang, Lijin; Geng, Yanling; Duan, Wenjuan. Ionic liquid-based ultrasound-assisted extraction of fangchinoline and tetrandrine from Stephaniae tetrandrae. Journal of Separation Science. 2009-10, 32 (20): 3550–3554 [2021-11-10]. ISSN 1615-9314. PMID 19764054. doi:10.1002/jssc.200900413. （原始內容存檔於2022-06-17）.
^ 謝林艷,陸嬌,柏芳芳,等. 粉防己鹼:一種治療支氣管哮喘的雙苄基異喹啉類生物鹼[J]. 國際呼吸雜誌,2015,35:(03)：210-214. DOI:10.3760/cma.j.issn.1673-436X.2015.03.013
^ ^6.0 ^6.1 Kwan, Chiu-Yin; Achike, F. I. Tetrandrine and related bis-benzylisoquinoline alkaloids from medicinal herbs: cardiovascular effects and mechanisms of action. Acta Pharmacologica Sinica. 2002-12, 23 (12): 1057–1068 [2021-11-10]. ISSN 1671-4083. PMID 12466042. （原始內容存檔於2022-07-04）.
^ Feng, Dechun; Mei, Yunhua; Wang, Ying; Zhang, Bianhong; Wang, Chen; Xu, Lingyun. Tetrandrine protects mice from concanavalin A-induced hepatitis through inhibiting NF-kappaB activation. Immunology Letters. 2008-12-22, 121 (2): 127–133 [2021-11-10]. ISSN 1879-0542. PMID 18992279. doi:10.1016/j.imlet.2008.10.001. （原始內容存檔於2021-11-10）.
^ Liu, Chaoyang; Gong, Ke; Mao, Xin; Li, Wenhua. Tetrandrine induces apoptosis by activating reactive oxygen species and repressing Akt activity in human hepatocellular carcinoma. International Journal of Cancer. 2011-09-15, 129 (6): 1519–1531 [2021-11-10]. ISSN 1097-0215. PMID 21128229. doi:10.1002/ijc.25817. （原始內容存檔於2021-11-10）.
^ Cheng, Zhixiang; Wang, Keming; Wei, Jia; Lu, Xiang; Liu, Baorui. Proteomic analysis of anti-tumor effects by tetrandrine treatment in HepG2 cells. Phytomedicine: International Journal of Phytotherapy and Phytopharmacology. 2010-11, 17 (13): 1000–1005 [2021-11-10]. ISSN 1618-095X. PMID 20554191. doi:10.1016/j.phymed.2010.03.018. （原始內容存檔於2021-11-10）.
^ Deng, Wen-Ying; Luo, Su-Xia; Zhou, Meng-Qiang; Li, Ning; Chen, Xiao-Bing; Han, Li-Li. [The study of anti-tumor effect of Tetrandrine combined with Nedaplatin on human liver cancer cell line 7402]. Zhong Yao Cai = Zhongyaocai = Journal of Chinese Medicinal Materials. 2008-10, 31 (10): 1522–1525 [2021-11-10]. ISSN 1001-4454. PMID 19230406. （原始內容存檔於2021-11-10）.
^ Kitano, Ai; Yamanaka, Osamu; Ikeda, Kazuo; Ishida-Nishikawa, Iku; Okada, Yuka; Shirai, Kumi; Saika, Shizuya. Tetrandrine suppresses activation of human subconjunctival fibroblasts in vitro. Current Eye Research. 2008-07, 33 (7): 559–565 [2021-11-10]. ISSN 1460-2202. PMID 18600488. doi:10.1080/02713680802220817. （原始內容存檔於2022-06-15）.
^ Sakurai, Yasuteru; Kolokoltsov, Andrey A.; Chen, Cheng-Chang; Tidwell, Michael W.; Bauta, William E.; Klugbauer, Norbert; Grimm, Christian; Wahl-Schott, Christian; Biel, Martin. Two pore channels control Ebolavirus host cell entry and are drug targets for disease treatment. Science (New York, N.Y.). 2015-02-27, 347 (6225): 995–998 [2021-11-10]. ISSN 0036-8075. PMC 4550587 . PMID 25722412. doi:10.1126/science.1258758. （原始內容存檔於2022-06-21）.
^ Bhakuni, Dewan S.; Jain, Sudha; Singh, Awadhesh N. Biosynthesis of the bisbenzylisoquinoline alkaloid, tetrandrine. Phytochemistry. 1980-01-01, 19 (11): 2347–2350. ISSN 0031-9422. doi:10.1016/S0031-9422(00)91024-0 （英語）.
^ Tetrandrine | ≥99%(HPLC) | TargetMol | Calcium Channel inhibitor. targetmol.com. [2021-11-10]. 原始內容存檔於2024-09-10.

[dxy-1] 1.0 ^1.1 汉防己甲素片（北海阳光）. 丁香園·用藥助手.

[2] Xin-Hui Jiang, Jun-Qing Yang, Na Li, Han Wang, Qi-Xin Zhou. The pharmacokinetical study of plant alkaloid tetrandrine with a simple HPLC method in rabbits. Fitoterapia. 2011-09, 82 (6): 878–882. doi:10.1016/j.fitote.2011.04.014.

[3] 楊敬,朱安祥,胡軍,等. 粉防己鹼的作用機制研究進展[J]. 國際中醫中藥雜誌,2018,40:(3)：286-289. DOI:10.3760/cma.j.issn.1673-4246.2018.03.025

[4] Zhang, Lijin; Geng, Yanling; Duan, Wenjuan. Ionic liquid-based ultrasound-assisted extraction of fangchinoline and tetrandrine from Stephaniae tetrandrae. Journal of Separation Science. 2009-10, 32 (20): 3550–3554 [2021-11-10]. ISSN 1615-9314. PMID 19764054. doi:10.1002/jssc.200900413. （原始內容存檔於2022-06-17）.

[5] 謝林艷,陸嬌,柏芳芳,等. 粉防己鹼:一種治療支氣管哮喘的雙苄基異喹啉類生物鹼[J]. 國際呼吸雜誌,2015,35:(03)：210-214. DOI:10.3760/cma.j.issn.1673-436X.2015.03.013

[未命名-rHh0-1-6] 6.0 ^6.1 Kwan, Chiu-Yin; Achike, F. I. Tetrandrine and related bis-benzylisoquinoline alkaloids from medicinal herbs: cardiovascular effects and mechanisms of action. Acta Pharmacologica Sinica. 2002-12, 23 (12): 1057–1068 [2021-11-10]. ISSN 1671-4083. PMID 12466042. （原始內容存檔於2022-07-04）.

[7] Feng, Dechun; Mei, Yunhua; Wang, Ying; Zhang, Bianhong; Wang, Chen; Xu, Lingyun. Tetrandrine protects mice from concanavalin A-induced hepatitis through inhibiting NF-kappaB activation. Immunology Letters. 2008-12-22, 121 (2): 127–133 [2021-11-10]. ISSN 1879-0542. PMID 18992279. doi:10.1016/j.imlet.2008.10.001. （原始內容存檔於2021-11-10）.

[8] Liu, Chaoyang; Gong, Ke; Mao, Xin; Li, Wenhua. Tetrandrine induces apoptosis by activating reactive oxygen species and repressing Akt activity in human hepatocellular carcinoma. International Journal of Cancer. 2011-09-15, 129 (6): 1519–1531 [2021-11-10]. ISSN 1097-0215. PMID 21128229. doi:10.1002/ijc.25817. （原始內容存檔於2021-11-10）.

[9] Cheng, Zhixiang; Wang, Keming; Wei, Jia; Lu, Xiang; Liu, Baorui. Proteomic analysis of anti-tumor effects by tetrandrine treatment in HepG2 cells. Phytomedicine: International Journal of Phytotherapy and Phytopharmacology. 2010-11, 17 (13): 1000–1005 [2021-11-10]. ISSN 1618-095X. PMID 20554191. doi:10.1016/j.phymed.2010.03.018. （原始內容存檔於2021-11-10）.

[10] Deng, Wen-Ying; Luo, Su-Xia; Zhou, Meng-Qiang; Li, Ning; Chen, Xiao-Bing; Han, Li-Li. [The study of anti-tumor effect of Tetrandrine combined with Nedaplatin on human liver cancer cell line 7402]. Zhong Yao Cai = Zhongyaocai = Journal of Chinese Medicinal Materials. 2008-10, 31 (10): 1522–1525 [2021-11-10]. ISSN 1001-4454. PMID 19230406. （原始內容存檔於2021-11-10）.

[11] Kitano, Ai; Yamanaka, Osamu; Ikeda, Kazuo; Ishida-Nishikawa, Iku; Okada, Yuka; Shirai, Kumi; Saika, Shizuya. Tetrandrine suppresses activation of human subconjunctival fibroblasts in vitro. Current Eye Research. 2008-07, 33 (7): 559–565 [2021-11-10]. ISSN 1460-2202. PMID 18600488. doi:10.1080/02713680802220817. （原始內容存檔於2022-06-15）.

[12] Sakurai, Yasuteru; Kolokoltsov, Andrey A.; Chen, Cheng-Chang; Tidwell, Michael W.; Bauta, William E.; Klugbauer, Norbert; Grimm, Christian; Wahl-Schott, Christian; Biel, Martin. Two pore channels control Ebolavirus host cell entry and are drug targets for disease treatment. Science (New York, N.Y.). 2015-02-27, 347 (6225): 995–998 [2021-11-10]. ISSN 0036-8075. PMC 4550587 . PMID 25722412. doi:10.1126/science.1258758. （原始內容存檔於2022-06-21）.

[13] Bhakuni, Dewan S.; Jain, Sudha; Singh, Awadhesh N. Biosynthesis of the bisbenzylisoquinoline alkaloid, tetrandrine. Phytochemistry. 1980-01-01, 19 (11): 2347–2350. ISSN 0031-9422. doi:10.1016/S0031-9422(00)91024-0 （英語）.

[14] Tetrandrine | ≥99%(HPLC) | TargetMol | Calcium Channel inhibitor. targetmol.com. [2021-11-10]. 原始內容存檔於2024-09-10.

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閱論編通道阻滯劑（英語：Channel blocker）
鈣 (Ca²⁺)	氨氯地平氨力農大麻素阿尼帕米阿雷地平阿折地平阿齊利特巴尼地平苄環烷貝尼地平苄普地爾小檗胺貝凡洛爾氫化小檗鹼羧胺三唑卡羅維林西尼地平桂利嗪克侖硫䓬氯維地平芋螺毒素達羅地平蝙蝠葛鹼待華帕米地爾硫䓬 Dimeditiapramine（英語：Dimeditiapramine）多他利嗪決奈達隆依福地平依莫帕米橋派酷乙哌立松乙琥胺法利帕米泛托法隆法舒地爾非洛地平芬那酸苯乙二苯丙胺氟桂利嗪福司地爾加洛帕米伊拉地平拉西地平拉莫三嗪樂卡地平利多氟嗪硫酸鎂馬尼地平 Manoalide（英語：Manoalide） Mepirodipine（英語：Mepirodipine）甲琥胺米貝拉地爾莫那匹爾萘哌地爾尼卡地平硝苯地平尼古地平 Niludipin（英語：Niludipin）尼伐地平尼莫地平尼索地平尼群地平去甲維拉帕米赭曲毒素A 蛇床子素奧替溴銨奧索地平哌克昔林苯琥胺匹維溴銨哌啶普拉地平普尼拉明利塞膦酸 Ryodipine（英語：Ryodipine）司莫地爾丙戊酸鈉光千金藤定鹼 TROX-1（英語：TROX-1）特羅地林延胡索乙素粉防己鹼防己諾林鹼托芬那酸曲尼司特戊諾酰胺戊哌醇丙戊匹酯丙戊酸半鈉丙戊酸丙戊酰胺維拉帕米齊考諾肽選擇性VDCC配體: 4-甲基普瑞巴林 Atagabalin（英語：Atagabalin）加巴噴丁加巴噴丁緩釋片 Imagabalin（英語：Imagabalin） PD-200,347 PD-217,014 PD-299,685 普瑞巴林
鉀 (K⁺)	3,4-二氨基吡啶 4-氨基吡啶胺碘酮溴苄胺丁萘夫汀蠍毒素芋螺毒素多非利特決奈達隆 E-4031（英語：E-4031）伊布利特利諾吡啶 Maurotoxin（英語：Maurotoxin）尼非卡蘭鈣激活鉀通道阻斷劑索他洛爾替地沙米四乙胺維納卡蘭
鈉 (Na⁺)	抗心律失常藥: 阿義馬林阿普林定丙吡胺決奈達隆英卡胺氟卡尼利多卡因勞拉義明勞卡尼美西律莫雷西嗪苯妥英吡西卡尼普拉馬林普魯卡因胺普羅帕酮奎尼丁司巴丁妥卡尼抗痙攣藥: 卡馬西平艾司利卡西平醋酸鹽乙苯妥英磷苯妥英利卡西平美芬妥因奧卡西平奧昔替林苯妥英盧非酰胺托吡酯丙戊酸鈉戊諾酰胺丙戊匹酯丙戊酸半鈉丙戊酸丙戊酰胺利尿劑: 阿米洛利 Benzamil（英語：Benzamil）氨苯蝶啶局部麻醉劑: 3-(p-Fluorobenzoyloxy)tropane（英語：3-(p-Fluorobenzoyloxy)tropane）阿米卡因阿替卡因苯佐卡因布比卡因 (左布比卡因, 羅哌卡因) 布大卡因氨苯丁酯氯普魯卡因辛可卡因可卡因環美卡因二甲卡因衣鐵卡因海克卡因 Iontocaine（英語：Iontocaine）利多卡因甲哌卡因美普卡因美布卡因奧索卡因哌羅卡因丙胺卡因普魯卡因丙氧卡因丙美卡因利索卡因丁卡因三甲卡因毒素: 芋螺毒素新岩蛤毒素蛤蚌毒素河魨毒素其他: 薄荷醇
其他	未分類: 依沙雙酮乙甲雙酮苯乙酰脲苯丁酰脲三甲雙酮