【產品名稱】 雷公藤甲素
【英文別稱】 triptolide
【CAS號】 38748-32-2
【檢測方式】高效液相色譜法HPLC≥98%
【規(guī)格】5mg 10mg 20mg 50mg 100mg 500mg 1g (可根據客戶需求包裝)
【鑒定方法】液相(HPLC)質譜(Mass) 核磁(NMR)
【作用與用途】本品用于含量測定、鑒別、藥理實驗、活性篩選等
【密度】 1.48g/cm3
【沸點】 601.7oC at 760mmHg
【閃點】 220.7oC
【熔點】 226-227oC
【用法】色譜條件:以甲醇:0.1%磷酸溶液=38:62為流動相,檢測波長為 215nm,柱溫:30oC(僅供參考)
【藥理藥效】 雷公藤甲素具有治療類風濕,抗腫瘤,抗炎,免疫抑制,抗病毒等作用
【注意事項】 本品應在低溫下保存,長時間在暴露在空氣中,含量會有所降低
【生產單位】 成都普菲德生物技術有限公司
【質量承諾】 非人為造成的產品質量問題,我司負責退貨或者換貨(非購買方人為造成)
【溫馨提醒】 我司提供一切產品僅供科研、實驗室使用,不得用于注射、食用或其他用途
Folate-modified triptolide liposomes target activated macrophages for safe rheumatoid arthritis therapy.DOI: 10.1039/D1BM01520F
TP was obtained from Pufei De Biotech Co., Ltd (Chengdu,China). Cholesterol and egg phosphatidylcholine (EPC) wereobtained from Avanti Polar Lipids, Inc. (Alabaster,AL,USA).DSPE-PEG2000 and 1,2-distearoyl-sn-glycero-3-phosphoethanol-amine-N-[amino (polyethylene glycol)-2000] (DSPE-PEG2000-NH2) were purchased from NOF Corp. (Tokyo, Japan). Chickentype II collagen, complete Freund adjuvant,and incompleteFreundadjuvant were obtained from Chondrex,Inc.(Redmond, WA,USA). RANKL was purchased from PeproTechInc. (Cranbury, NJ, USA). M-CSF and lipopolysaccharide (LPS)were provided by Meilun Co.,Ltd (Dalian,China). 4',6-Diamidino-2-phenylindole (DAPI) and 1,1-dioctadecyl-3,3,3,3-tetramethylindotricarbocyanine iodide (DiR) were obtainedfrom Kaiji Biological Technology Development Co.,Ltd(Nanjing,China).ELISA kits were purchased from SolarbioCo.,Ltd (Beijing, China). MMP-2 and MMP-9 antibodies werepurchased from Abcam Co.,Ltd (Cambridge,MA,USA). Allother reagents used were of analytical grade.
Rheumatoid arthritis (RA) is an autoimmune disease characterized by synovial joint hyperplasia, joint inflammation, cartilage erosion and bone destruction. Macrophages play an essential role in the pathogenesis of RA, and folate receptor β (FR-β) is highly expressed on the surface of activated synovial macrophages in RA patients. Triptolide (TP) has anti-inflammatory properties, and it can protect the cartilage matrix, but its clinical application has been limited due to poor solubility, low bioavailability and systemic toxicity. Therefore, we constructed folate-modified triptolide liposomes (FA-TP-Lips) to target macrophages, thereby treating RA in a safe and effective way. The experiments indicated that FA-TP-Lips had properties of small particle size, uniform particle size distribution, high drug encapsulation and long circulation. Furthermore, FA-TP-Lips showed reduced cytotoxicity, increased cellular uptake and significant anti-inflammatory effects in vitro. It also inhibited osteoclastogenesis. In vivo experiments revealed that liposomes could prolong the circulation of TP in the body, as well as exhibit significant cartilage-protective and anti-inflammatory effects with lower toxicity compared with the free TP group, thereby providing a promising new approach for the treatment of RA.
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[2]. Huang M, et al. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013 Feb;12(2):184-94.
[3]. Xu P, et al. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta25-35 via the Autophagy Pathway.PLoS One. 2015 Nov 10;10(11):e0142719.
[4]. Kong LL, et al. Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice.Sci Rep. 2015 Jul 2;5:11747.
[5]. Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.