biotransformation

Naringinase 是一种在自然界中广泛存在的水解酶复合物，具有 α-L-鼠李糖苷酶和 β-D-葡萄糖苷酶的活性，主要用于糖苷的水解。

Isonicotinic acid 是 Isoniazid 的代谢产物。Isoniazid 通过肼解转化为 Isonicotinic acid。 Isoniazid 向 Isonicotinic acid 的生物转化可以通过细胞色素 P450 酶催化。

(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO

Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix , clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascular ischemic events for patients without deficiencies in CYP2C19-related metabolism.

rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1 Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1 Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)

Vaccarin 是从王不留行中提取的一种黄酮糖苷，可显著促进伤口愈合以及伤口部位的内皮和成纤维细胞增殖。它通过激活 AMPK 信号通路改善胰岛素抵抗和脂肪变性。

Aurantio-obtusin 是从决明子中分离出的蒽醌类化合物，具有抗炎、抗凝血、抗氧化、抗高血压的活性。它能抑制 IgE 介导的肥大细胞和过敏模型中的过敏反应，具有研究过敏相关疾病的潜力。在大鼠中，它通过内皮细胞 PI3K AKT eNOS 依赖信号通路放松全身动脉，是潜在的新型血管扩张剂。

Diaphorase 能从厌氧污泥生物中获得。Diaphorase 通过脱硝作用，催化六氢-1,3,5-三硝基-1,3,5-三嗪 (RDX) 的生物转化。

7-Hydroxy-TSU-68为TSU-68的衍生物，该化合物为TSU-68在人类肝微粒体内经生物转化途径形成的代谢产物，其含量标识了TSU-68自身诱导的羟基化程度。

4'-Demethylpodophyllotoxone为链格孢（Alternaria alternata）S-f6的生物转化中间产物，经4-(2,3,5,6-tetramethylpyrazine-1) (4-TMP)修饰后形成的新化合物，可有效抑制人胃癌细胞系（BGC-823）的生长。

(±)-Lavandulol为一不对称的单萜醇，能由米根霉(Rhizopus oryzae)真菌转化为其对应氧化代谢产物。

8-Chloroadenosine-5’-triphosphate（8-chloro ATP）是抗癌剂8-chloro cAMP的活性代谢物，也是核苷酸腺苷5’-三磷酸（ATP）的衍生物。它通过8-chloro cAMP、8-chloroadenosine以及一磷酸和二磷酸中间体形成。应用8-chloro cAMP或8-chloroadenosine后，8-chloro ATP可累积长达12小时，与细胞生长抑制、内源性ATP水平下降以及患者源多发性骨髓瘤细胞中RNA合成减少（但DNA合成不受影响）相关。在1.5至8 mM浓度范围内，它抑制topoisomerase II-α依赖的超螺旋pUC19 DNA放松，同时在1 mM时减少了K562人髓性白血病细胞中topoisomerase II-α催化的ATP水解50%。

10,11-Dihydro-10,11-dihydroxy Carbamazepine, a metabolite of the anticonvulsant carbamazepine and the antiepileptic prodrug oxcarbazepine, is produced through the biotransformation of carbamazepine via a carbamazepine 10,11-epoxide intermediate by epoxide hydrolase, and from oxcarbazepine via a 10,11-dihydro-10-hydroxy carbamazepine intermediate. This compound has been detected in wastewater effluent, highlighting its environmental presence following pharmaceutical use.

3-epi-Resibufogenin (compound 2),通过Actinomucor elegans AS 3.2778的生物转化,从Resibufogenin派生而来,具有抗癌活性.该化合物在对抗癌细胞时展现出明显的细胞毒性,其IC50值为42.5 μM(A549)和48.4 μM(H1299).