Ten new and four known clerodane diterpenoids were isolated from the vine and leaves of Tinospora crispa. The chemical structures and absolute stereochemical configurations of all the compounds were established by spectroscopic methods and single-crystal X-ray diffraction analysis combined with electronic circular dichroism (ECD) analysis. All these compounds possess a lactone ring system except compound 10 which has a rare bridge ring between C-2 and C-20. The lactone ring in these compounds is diversely constructed between C-1 and C-18, C-6 and C-18, C-6 and C-17, C-12 and C-17, or C-15 and C-16 in the clerodane diterpenoid skeleton. All the compounds were assayed for their anti-inflammatory activities on lipopolysaccharide (LPS)-activated microglial BV-2 cells. Compounds 5 and 7 exhibited nitric oxide (NO) release inhibitory activities with IC₅₀ values of 7.5 and 10.6 μM respectively. In particular, compound 7 exhibited better inhibitory activity and less cytotoxicity than the positive control minocycline. Moreover, compounds 9 and 14 were found to synergize with oxacillin (OXA) against methicillin-resistant Staphylococcus aureus (MRSA). This synergy was further confirmed by checkerboard and time-killing assays. Compounds 9 and 14 at the sub-MIC level significantly decreased the MIC of OXA from 32.0 to 1.0 μg mL⁻¹ and 0.5 μg mL⁻¹, respectively.

中文翻译：

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具有抗炎和协同抗菌活性的 Clerodane 二萜类化合物

十种新的和四种已知的克罗丹二萜类化合物是从卷曲黄孢的藤​​蔓和叶子中分离出来的。通过光谱法和单晶X射线衍射分析结合电子圆二色谱(ECD)分析确定了所有化合物的化学结构和绝对立体化学构型。所有这些化合物都具有内酯环系统，除了化合物10在 C-2 和 C-20 之间具有罕见的桥环。这些化合物中的内酯环在 C-1 和 C-18、C-6 和 C-18、C-6 和 C-17、C-12 和 C-17 或 C-15 和 C-16 之间构建不同在氯丹二萜骨架中。测定了所有化合物对脂多糖 (LPS) 激活的小胶质细胞 BV-2 细胞的抗炎活性。化合物图5和7显示出抑制一氧化氮(NO)释放的活性，IC ₅₀值分别为7.5和10.6μM。特别是，化合物7表现出比阳性对照米诺环素更好的抑制活性和更低的细胞毒性。此外，发现化合物9和14与苯唑西林 (OXA) 协同对抗耐甲氧西林金黄色葡萄球菌(MRSA)。这种协同作用通过棋盘格和时间杀伤分析得到进一步证实。亚 MIC 水平的化合物9和14使 OXA 的 MIC 从 32.0 显着降低至 1.0 μg mL ^-1和 0.5 μg mL ^-1， 分别。