生物活性
雷公藤甲素与人XPB共价结合，抑制其dna依赖的atp酶活性，从而抑制RNA聚合酶ii介导的转录和可能的核苷酸切除修复。PG490可抑制白细胞介素(IL)-2的表达，其作用机制为:用佛波12-肉芽氨酸13-乙酸酯(PMA)和CD3抗体刺激正常人外周血淋巴细胞(IC50为10 ng/ml)，用PMA和离子霉素刺激正常人外周血淋巴细胞(Iono, IC50为40 ng/ml)。PG490抑制活化t细胞(NF-AT)靶序列嘌呤盒/抗原受体反应元件(ARRE)/核因子(NF-AT) DNA结合活性的诱导，但不抑制NF-kappaB位点。PG490还抑制pma刺激的嵌合转录因子的激活，其中NF-kappaB p65的c端TA1反式激活域融合到GAL4的DNA结合域。在16HBE人支气管上皮细胞中，IL-8的表达主要受NF-kappaB的调控，PG490能完全抑制IL-8的表达，而环孢素A不能。PG490能有效抑制tnf -alpha诱导的NF-kappaB的激活。PG490还阻断了tnf -alpha介导的c-IAP2 (hiap-1)和c-IAP1 (hiap-2)的诱导，这是凋亡抑制剂(IAP)家族成员。有趣的是，PG490并没有阻断NF-kappaB的DNA结合，但它阻断了NF-kappaB的转录激活。
化学数据
| 分子量 | 360.40 |
| 分子式 | C20H24O6 |
| CAS号 | 38748-32-2 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 25 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | N2a and SKNSH cells |
| 方法 | Cell viability determination
Cells were seeded in serum-containing media onto 96-well plates at densities of 3 × 103cells per well for N2a and 5 × 103cells per well for SKNSH. Following overnight incubation, cells were treated with varying concentrations of triptolide in serum-free media and re-incubated for varying time courses at 37 °C. Controls were treated with serum-free media.Cell viability was determined using an MTT assay. Reagent was prepared by dissolving thiazolyl blue tetrazolium bromide (Sigma-Aldrich) in phosphate-buffered saline (Invitrogen) at a concentration of 2 mg/mL and filtering. After cells were incubated in 96-well plates and subsequently exposed to triptolide at varying doses and time durations, 20 μL MTT reagent were added to each well. Cells were re-incubated at 37°C for 4 hours, after which all liquid was aspirated from each well and absorbances were measured at 550 and 650 nm. These experiments were performed in triplicate and repeated 4 times. |
| 浓度 | 31.25 to 500 nM |
| 处理时间 | 24 and 48 h |
| 动物实验 |
|---|
| 动物模型 | Female A/J mice bearing Orthotopic neuroblastoma model |
| 配制 | DMSO |
| 剂量 | 0.4 mg/kg |
| 给药处理 | intraperitoneal injections |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7747 mL | 13.8735 mL | 27.7469 mL |
| 5 mM | 0.5549 mL | 2.7747 mL | 5.5494 mL |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7747 mL |
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