sterol biosynthesis

Fenhexamid (Elevate) 是一种甾醇生物合成抑制剂，对植物病原真菌具有抗真菌活性。 Fenhexamid 用于农业，并在水果和蔬菜中以可测量的量存在。

Diallyl disulfide 能够抑制人角鲨烯单加氧酶，抑制角鲨烯环氧化的 IC50为 400 μM。它也具有抗肿瘤作用，同miR-200b 和miR-22联合使用可增强该作用。

AY 9944 是特异性的胆固醇生物合成抑制剂。它抑制 7- 脱氢胆固醇 Δ7- 还原酶 (IC50:13 nM)，导致胆固醇不足和 7DHC 积累。在高剂量下，它可在培养的胚胎中抑制固醇 Δ7-Δ8 异构酶，造成胆固醇 8-en-3β-ol 的积累。

Naftifine hydrochloride (Naftifine HCl) 是一种抗生素。它具有抗真菌活性，对皮肤真菌、曲霉、Sporothrix schenckii、假丝酵母属的酵母有抑制作用。

Uniconazole 是植物生长调节剂，能够抑制细胞色素 P450 707As (Ki=68 nM)。他是分解脱落酸的酶家族成员，能够抑制赤霉素和甾醇的生物合成。

Clotrimazole (FB 5097) 是咪唑衍生物，有抗真菌和抗菌活性，是 P450抑制剂。

25-Hydroxycholesterol 是胆固醇的代谢产物，由巨噬细胞响应 Toll 样受体激活而分泌。它有效抑制 B 细胞产生 IgA，EC50约为 65 nM。

Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which is accompanied by an increase in the plasma level of 25-hydroxyvitamin D3. Treatment with peraclopone dramatically alters membrane sterol content in many membranes including the microvillus membrane of both the jejunum and ileum. In the jejunal microvillus membrane a major change in chemical composition occurred, presumably in response to the alteration in membrane sterol. The net result was a significant decline in both the static and dynamic component of membrane fluidity.

Dimethomorph 是一种吗啉类杀菌剂，属于甾醇生物合成抑制剂类杀菌剂，可抑制真菌细胞壁的形成。Dimethomorph 抑制了oomycete fungi，P. citrophthora，P. parasitica，P. capsici，和P. infestans 的菌丝生长 (EC50=0.14 μg/mL，0.38 μg/mL，<0.1 μg/mL 和 0.16-0.3 μg/mL)，但是对绿藻物种C. vulgaris 和S. obliquus 的活性较低 (EC50=47.46 μg/mL 和 44.87 μg/mL)。在 MDA-kb2 人乳腺癌细胞的报告基因分析中，Dimethomorph 抑制雄激素受体 (AR) 的活性，而在酵母抗雄激素筛选中不起作用 (IC20=0.263 μM 和 38.5 μM)。

(Z)-Lanoconazole 是 Lanoconazole 的 Z 构型，用于研究皮肤癣菌病和甲癣。Lanoconazole 抑制甾醇 14-α脱甲基酶并阻断真菌膜上的麦角甾醇生物合成，从而干扰麦角甾醇的生物合成。Lanoconazole 是具有口服活性的咪唑类抗真菌剂，在体外和体内均具有广谱的抗真菌活性。

Steryl glucosides are neutral glycolipids commonly found in plant cell membranes and vegetable oils that contain a glucose moiety conjugated to a sterol lipid. They function as glucose donors in the biosynthesis of glucocerebrosides in plant microsomes and are metabolic precursors to acylated esterified steryl glucosides. Steryl glucosides are the major component of filter- and engine-damaging precipitates formed during biodiesel production from transesterification of vegetable oils. This product contains a mixture of steryl glucosides.

Penconazole 是一种典型的三唑类杀菌剂 (fungicide)，主要用于苹果、葡萄、蔬菜等的白粉病防治。Penconazole 抑制真菌甾醇生物合成。Penconazole 降低大鼠大脑和小脑AChE 活性。

The compound binds and blocks farnesyl diphosphate synthase in the HMG-CoA pathway (IC50 = 460 nM for recombinant human FPPS). It causes macrophage apoptosis and inhibits prenylation and sterol biosynthesis in purified osteoclasts.

Pregnanetriol is a metabolite of 17α-hydroxyprogesterone .1,2It is formed from 17α-hydroxyprogesterone by reduction of the C-20 ketone.2Urinary levels of pregnanetriol are elevated in patients with 21-hydroxylase deficiency and congenital adrenal hyperplasia.3,4 1.Kamrath, C., Hartmann, M.F., Boettcher, C., et al.Diagnosis of 21-hydroxylase deficiency by urinary metabolite ratios using gas chromatography-mass spectrometry analysis: Reference values for neonates and infantsJ. Steroid Biochem. Mol. Biol.15610-16(2016) 2.Schiffer, L., Barnard, L., Baranowski, E.S., et al.Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: A comprehensive reviewJ. Steroid Biochem. Mol. Biol.194105439(2019) 3.Disorders of steroidogenesis guide to steroid profiling and biochemical diagnosis1(2019) 4.Shackleton, C.H.L.Role of a disordered steroid metabolome in the elucidation of sterol and steroid biosynthesisLipids47(1)1-12(2012)

Fenpropidin (Ro-12-3049) 是甾醇类生物合成的抑制剂，具有杀菌的活性。