Reductase

Poliumoside is a natural compound which exhibits significant inhibition of advanced glycation end product formation with IC50 value of 4.6-25.7 μM, it also exhibits great inhibitory effects on rat lens aldose reductase with IC50 values of 0.85 μM.Poliumos

5α-Reductase is the enzyme responsible for converting testosterone into 5-α dihydrotestosterone (DHT), a potent androgen involved in male sexual differentiation. The 5α-reductase family comprises three subfamilies and five isozyme members: 5αR1, 5αR2, 5αR3, GPSN2, and GPSN2L.

Isoliquiritigenin (ISL) is a flavonoid natural product that inhibits influenza virus replication (EC50=24.7 μM) and aldose reductase activity (IC50=320 nM). Isoliquiritigenin has antitumor activity.

Alpha-Estradiol (Epiestradiol) is an estrogen that inhibits 5alpha-reductase and has potential in the study of androgenetic alopecia.

DL-Glyceraldehyde (Glyceric aldehyde) is produced from the action of the enzyme glyceraldehyde dehydrogenase, which converts glycerol to glyceraldehyde using NADP as a cofactor. When present at sufficiently high levels, DL-Glyceraldehyde can be a cytotoxin and a mutagen. A cytotoxin is a compound that kills cells. A mutagen is a compound that causes mutations in DNA. DL-Glyceraldehyde is a highly reactive compound that can modify and cross-link proteins. DL-Glyceraldehyde modified proteins appear to be cytotoxic, depress intracellular glutathione levels, and induce reactive oxygen species (ROS) production (PMID: 14981296 ). DL-Glyceraldehyde has been shown to cause chromosome damage to human cells in culture and is mutagenic in the Ames bacterial test.

6-Methoxytricin, a flavonoid isolated from Centella asiatica, is an inhibitor of aldose reductase (AR) and advanced glycosylation end-products (AGE), and inhibits T-cell proliferation and activation in biologic cells.

Tectoridin (Shekanin) possesses an estrogenic and thyroid hormone-like agent by activating estrogen and thyroid hormone receptors. Tectoridin has anti-oxidant, anti-inflammatory and hypoglycemic activities; Tectoridin and its five metabolites inhibits the activities of lens aldose reductase in rat (IC : 1.4-15.5 μM).

2'-Acetylacteoside has antioxidative activity. It can significantly attenuate glutamate-induced neurotoxicity at concentrations ranging from 0.1 to 10 μM. 2'-Acetylacteoside shows antiproliferative effects on aortic smooth muscle, indicates that it may ha

Quercitrin hydrate is a natural flavonoid glycoside with multiple activities, including anti-inflammatory, antioxidant, anticancer, neuroprotective, and cardiovascular protective effects, and inhibits aldose reductase.

Ganoderic acid C2 has anti-inflammatory,and anti-tumor-promoting activities. Ganoderic acid C2 can inhibit histamine release, it also has inhibitory effects on the induction of Epstein-Barr Virus early antigen.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.

Triptocalline A, a compound from Salacia chinensis, inhibits rat lens aldose reductase.

1. Engeletin (Dihydrokaempferol 3-rhamnoside) may serve as a potential anti-inflammatory agent. 2. Engeletin possesses potent inhibition of PGE2 release with IC5 values of 19.6 μg ml. 3. Engeletin inhibits a recombinant human aldose reductase (IC5 value=1.16 microM).

beta-Glucogallin (beta-Glucogallin) is a selective aldose reductase (AKR1B1) inhibitor with antioxidant, anti-glycation, and anti-inflammatory properties. beta-Glucogallin is a naturally occurring compound derived from Emblica officinalis and is used in diabetes research. Vitamin B3-d4

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

BYAKANGELICIN,a main furanocoumarin constituent isolated and characterized as an aldose reductase inhibitor,and is effective for the treatment of sugar cataracts and diabetic neuropathy and hence might be useful as a lead compound for the development of new type drugs for clinical use.

1. Isocurcumenol inhibits 5α-reductase which converts testosterone to dihydrotestosterone (DHT).

Quercetin 3-gentiobioside (Quercetin-3-gentiobioside) is an inhibitor of AR and AGE formation and can be extracted from A. iwayomogi.Quercetin 3-gentiobioside inhibits the biological activity of aldose reductase (AR) and the formation of advanced glycosylation end products (AGEs).

12-O-Methylcarnosic acid is a diterpene carnosic acid isolated from Salvia microphylla, is an active constituent of 5α-Reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid has Antioxidant activity, it is effective preventing gastric lesions. 12-O-Methylcarnosic acid can suppress melanin production with downregulation of Tyrosinase expression in HMV-II melanoma cells. 12-O-Methylcarnosic acid may have anti-diabetic activity, it is able to significantly activate peroxisome proliferator-activated receptor (PPAR)γ.

8-Lavandulylkaempferol exhibits significant inhibitory effects with IC(50) values of 7.10 and 8.11 microM for butyrylcholinesterase and acetylcholinesterase, respectively. It shows inhibitory activities against aldose reductase, with the the IC50 of 0.79 microM.

Cornoside is a natural phenolic glycoside that inhibits rat lens aldose reductase (AR) activity, reducing oxidative stress and inflammation in diabetic complications.

Danshenol A has strong aldose reductase (AR) inhibitory activity, has IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Danshenol A also has antitumor activity in T-24, QGY, K562, Me180 and BIU87 cell lines, shows inhibited growth of K562 (IC50 = 0.53 μg mL), T-24 (IC50 = 7.94 μg mL), QGY (IC50 = 4.65 μg mL) and Me180 (IC50 = 6.89 μg mL) cell lines.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that acts as a selective and potent inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting antimicrobial activity by blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.