Sophoflavescenol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sophoflavescenol 是 PDE5 的混合抑制剂，K(i) 值为 0.005 microM。槐黄烯醇具有抗氧化、抗炎和细胞凋亡作用，这些作用可能有助于抗肿瘤活性，且没有严重的副作用。

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflavescenol exerts notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells.(In Vitro):Despite the small effect on human breast adenocarcinoma (MCF-7), Sophoflavescenol showed cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells. Interestingly, it also exerted potent in vivo antitumor activity by tumor growth inhibition in the LLC tumor model as well as apoptotic activity by caspase-3 activation in HL-60 cells. In addition, it exhibited potent antioxidant activities in 1,1-diphenyl-2-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radicals and lipid peroxidation assays. Sophoflavescenol exerted notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells.

Sophoflavescenol shows cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells. Sophoflavescenol exerts notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells. Sophoflavescenol exhibits remarkable inhibition of RLAR activity with an IC50 value of 0.30 μM, compared with 0.07 μM for epalrestat, a well known ARI. Sophoflavescenol also shows potent inhibitory activity with an IC50 value of 0.17 μM, comparable to epalrestat (0.15 μM) in the HRAR assay. In the AGE assay, sophoflavescenol (IC50 17.89 μg/mL) is a more potent inhibitor of AGE formation than aminoguanidine (IC50 81.05 μg/mL). Sophoflavescenol exerts both potent AChE and BChE inhibitory effects with respective IC50 values of 8.37 and 8.21 μM. Sophoflavescenol also exhibits good BACE1 inhibition in a dose-dependent manner with an IC50 value of 10.98 μM. Sophoflavescenol is a mixed inhibitor (Ki=0.005 μM) against cGMP PDE5. Sophoflavescenol shows greatest selectivity toward PDE5, 31.5- and 196.2-fold over PDE3 and PDE4, respectively.

Sophoflavescenol exerts potent in?vivo?antitumor?activity?by tumor growth inhibition in the LLC tumor model as well as apoptotic?activity?by caspase-3 activation in HL-60 cells.

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Others

Other Targets

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216450-65-6

368.385

C21H20O6

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (67.86 mM)

COc1cc(O)c(CC=C(C)C)c2oc(c(O)c(=O)c12)-c1ccc(O)cc1

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(-20℃)

With Ice Pack

≥ 2 years