58523-30-1
58523-30-1 結(jié)構(gòu)式
基本信息
英文別名
PB-1pseurotin
NSC 348694
(5S,8S,9R)-8-Benzoyl-2-[(1S,2S,3Z)-1,2-dihydroxy-3-hexenyl]-9-hydroxy-8-methoxy-3-methyl-1-oxa-7-azaspiro[4.4]non-2-ene-4,6-dione
1-Oxa-7-azaspiro[4.4]non-2-ene-4,6-dione, 8-benzoyl-2-[(1S,2S,3Z)-1,2-dihydroxy-3-hexen-1-yl]-9-hydroxy-8-methoxy-3-methyl-, (5S,8S,9R)-
所屬類別
天然產(chǎn)物：生物堿物理化學(xué)性質(zhì)
熔點126.0-126.9℃
沸點751.5±60.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度溶于DMSO(10mg/ml)
酸度系數(shù)(pKa)14.76±0.20(Predicted)
形態(tài)白色至類白色粉末。
顏色白色
穩(wěn)定性可在-20°C下的DMSO中的溶液儲存長達(dá)3個月。
常見問題列表
生物活性
Pseurotin A，曲霉和其他真菌的次級代謝產(chǎn)物，是幾丁質(zhì)合成酶 (chitin synthase) 的競爭性抑制劑和神經(jīng)發(fā)生劑。Pseurotin A 抑制 IgE 的產(chǎn)生 (IC50=3.6 μM)。Pseurotin A 具有抗腫瘤活性。體外研究
Pseurotin A inhibits the expression of PCSK9 in HepG2 cells, with an IC
50
value of 1.2 μM. Pseurotin A (25-100 μM; 72 hours) significantly suppressed the PCSK9 level in a dose dependent manner in BT-474 and T47D BC cell lines. Pseurotin A (25-100 μM; 72 hours) significantly increases LDLR level in a dose dependent manner.
Pseurotin A (40-200 μM; 24-72 hours) shows anti-proliferative activity in the hormone-dependent BC cells.
Cell Viability Assay
| Cell Line: | BT-474 cells, T47D cells |
| Concentration: | 40-200 μM |
| Incubation Time: | 24-72 hours |
| Result: | Showed weak but time and dose-dependent inhibition of the growth of BT-474 and T47D BC cells, with gradual decrease of the IC 50 values over time (260.83-93.64 μM and 267.84-113.08 μM, respectively). |
體內(nèi)研究
Pseurotin A (10 mg/kg; p.o.; 7X/week, 30 days) shows anti-tumor activity.
| Animal Model: | HFD-fed orthotopic athymic mice (bearing BT-474 tumor cells xenograft mode) |
| Dosage: | 10 mg/kg |
| Administration: | P.o.; 7X/week, 30 days |
| Result: | Significantly suppressed the growth of BT474 tumors. |