小白菊內(nèi)酯性質(zhì)、用途與生產(chǎn)工藝
小白菊內(nèi)酯是一種倍半萜烯內(nèi)酯類(lèi)天然產(chǎn)物，分離自艾菊、觀光木等藥用植物，這些植物廣泛應(yīng)用于發(fā)熱、驅(qū)蟲(chóng)和抗炎等。近年來(lái)的研究證實(shí)小白菊內(nèi)酯具有多種重要的藥理活性，如抗腫瘤、抗病毒、抗炎和抗動(dòng)脈粥樣硬化等，小白菊內(nèi)酯傳統(tǒng)上主要用來(lái)治療偏頭痛、發(fā)熱和類(lèi)風(fēng)濕性關(guān)節(jié)炎等。
倍半萜內(nèi)酯類(lèi)化合物小白菊內(nèi)酯是從小白菊中提取的化合物，最初被用來(lái)治療皮膚感染、風(fēng)濕病以及偏頭痛。近期研究表明，小白菊內(nèi)酯可抑制前列腺癌、乳腺癌、胃癌、白血病癌、腎癌、肺癌、結(jié)腸腺癌、成神經(jīng)管細(xì)胞瘤等癌細(xì)胞的生長(zhǎng)，在動(dòng)物模型上小白菊內(nèi)酯還能治療紫外線引起的皮膚癌。
(-)-Parthenolide, Nuclear Factor-κB抑制劑，可特異性地耗盡HDAC1蛋白，而不影響其他I/II類(lèi) HDACs。促進(jìn)MDM2的泛素化并激活p53的細(xì)胞功能。
| Target | Value |
|
HDAC1
|
|
NF-κB
|
|
MDM2 ubiquitination
|
p53
()
|
Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells, indicating that apoptosis is trigged after Parthenolide exposure. In addition to induction of apoptosis, Parthenolide also induces G
0
/G
1
cell cycle arrest in a concentration-dependent manner in A549 cells and G
2
/M cell cycle arrest in H1792 cells.
Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect in
Phb1
KO hepatocytes. Indeed, TSA and Parthenolide-treated hepatocytes showed increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a results of specific HDAC inhibition, resulting in the attenuation of the
Phb1
KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL in
Phb1
KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to control
Phb1
KO mice.
小白菊內(nèi)酯
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品