| 名稱(chēng) | Astragaloside IV |
| 描述 | Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts. |
| 細(xì)胞實(shí)驗(yàn) | CCK-8 assay is adopted to determine cell viability. cultured NSCLC cells are seeded into 96-well plates at the density of 4×104 (cells/well). Then 10 μL?well CCK8 solution is added and incubated in dark at 37°C for another 2 h. The absorbance is determined with the wavelength of 490 nm. |
| 激酶實(shí)驗(yàn) | MDA-MB-231 cells treated as indicated or tumor tissues are harvested and lysed in Mg2+ lysis buffer containing 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.5 M NaCl, and protease inhibitor cocktail. Equal amounts of lysates are incubated with PAK-PBD beads at 4°C for 1 h. PAK-PBD beads are pelleted by centrifugation and washed with ish buffer containing 25 mM Tris (pH 7.5), 30 mM MgCl2, 40 mM NaCl. Active Rac1 is detected by western blotting. |
| 動(dòng)物實(shí)驗(yàn) | Transient cerebral ischemia and reperfusion is prepared by BCCAO. Mice are randomly divided into the Sham, Model, Astragaloside IV (10 mg/kg) and Astragaloside IV (20 mg/kg) treatment groups. The Astragaloside IV treatment groups are intragastrically administered 7 days before the surgery and terminated on the day of sacrifice. On the day of the surgery, Astragaloside IV is administrated 2 h prior to ischemia. The Sham-operated and Model groups are treated with distilled water. After the mice are anesthetized with an intraperitoneal injection of chloral hydrate (350 mg/kg), the bilateral common carotid arteries are exposed and carefully separated with a small ventral neck incision and occluded twice (20 min each) with ligated surgical silk as described previously with minor modifications. There is a 10 min reperfusion period between the two occlusion periods (ischemia 20 min ? reperfusion 10 min ? ischemia 20 min). Sham-operated mice are subjected to the same surgical operation without the surgical silk ligation. Mouse body temperature is maintained at 37±0.5°C during the surgery with heating equipment until recovery from the anesthesia. |
| 體外活性 | Astragaloside IV對(duì)MDA-MB-231乳腺癌細(xì)胞的活性和侵襲性產(chǎn)生抑制作用，能夠壓抑絲裂原活化蛋白激酶（MAPK）家族成員ERK1/2和JNK的激活，并下調(diào)金屬蛋白酶（MMP）-2和-9的表達(dá)。在NSCLC細(xì)胞生長(zhǎng)抑制方面，Astragaloside IV（10、20、40 ng/mL）顯示出明顯的作用，而低濃度Astragaloside IV（1、2.5、5 ng/mL）對(duì)細(xì)胞活性無(wú)明顯細(xì)胞毒性。此外，Astragaloside IV與化療化合物順鉑聯(lián)合治療顯著提高了NSCLC細(xì)胞對(duì)化療化合物的敏感性。在分子水平上，Astragaloside IV與順鉑聯(lián)合使用顯著抑制了B7-H3的mRNA和蛋白水平的表達(dá)。 |
| 體內(nèi)活性 | 在小鼠模型中，高劑量的Astragaloside IV組在48小時(shí)存活率上顯示出顯著增加[60%(9/15)對(duì)比13.3%(2/15), P<0.05]，血清ALT和AST水平顯著降低(P<0.01)，肝臟組織病理學(xué)指數(shù)及肝細(xì)胞凋亡程度顯著降低(P<0.01)，以及肝勻漿中MDA含量顯著減少(P<0.01)，SOD活性顯著增加。Astragaloside IV（10, 20 mg/kg, p.o.）顯著地預(yù)防了短暫腦缺血及再灌注所誘導(dǎo)的認(rèn)知缺陷。與模型組相比，Astragaloside IV（10 mg/kg）和Astragaloside IV（20 mg/kg）能顯著降低這些細(xì)胞因子的水平。Astragaloside IV明顯抑制了TLR4及其下游蛋白的水平，表明MyD88依賴(lài)性和非依賴(lài)性途徑在Astragaloside IV的抗炎作用中發(fā)揮了重要作用。此外，Astragaloside IV減少了NLRP3和活化的caspase-1的表達(dá)，同時(shí)也降低了Iba1蛋白的表達(dá)。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (63.7 mM), Sonication is recommended.
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| 關(guān)鍵字 | JNK | Extracellular signal regulated kinases | Inhibitor | MMP | inhibit | Astragaloside IV | ERK | Matrix metalloproteinases |
| 相關(guān)產(chǎn)品 | Lidocaine hydrochloride | Lidocaine | Melatonin | Mifepristone | Doxycycline | Glucosamine | Tauroursodeoxycholate | Ethisterone | Tamoxifen | Kaempferol | TBHQ | Edaravone |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 植物來(lái)源化合物庫(kù) | 抗衰老化合物庫(kù) | 天然產(chǎn)物庫(kù) | 抗病毒中藥單體化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 中藥抗炎分子庫(kù) |