Reductase

Epristeride (ONO-9302) is an orally active, selective and non-competitive steroidal 5-α-reductase isoform 2 inhibitor that inhibits SR isoform 2.Episteride reduces prostate size and improves symptoms in men with BPH.Episteride induces atrophy and apoptosis of the ventral prostate in rats.

Auranofin (SKF-39162) is an antirheumatic agent, is used to treat rheumatoid arthritis, improves arthritis symptoms including painful or tender and swollen joints and morning stiffness.

Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

1. Soyasaponin Bb (Soyasaponin I) can suppress Eca-976 cell growth, reverse effects on over expression of c-met, VEGF, and induce cell apoptosis through inhibiting HDAC1-NF-kappaB and activating PETEN and caspase-3 signaling pathways.

Ranirestat (AS-3201) is an orally active and potent aldose reductase (AR) inhibitor with neuroprotective properties that ameliorates peripheral nerve dysfunction in rats with advanced diabetic polyneuropathy.Ranirestat inhibits the inflammatory response of high glucose-exposed endothelial cells and may be useful for the study of diabetic sensory-motor polyneuropathy.

Alconil (Al 1567) is an aldose reductase inhibitor that may be used to study chronic obstructive pulmonary disease (COPD) and diabetes.

Soyasaponin Ba may represent viable candidates for effective vaccine adjuvants due to their higher and lower or non-haemolytic effects.Soyasaponins Ab and Bb prevent scopolamine-induced memory impairment in mice without the inhibition of acetylcholinester

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

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.

Risarestat (CT-112) is a potent aldose reductase inhibitor and thyroid hormone receptor (TR) antagonist for the treatment of hypoglycemia.

IDD388 is a selective and potent aldose reductase (ALR2) inhibitor with antitumor activity that inhibits the ALR1 receptor.

Sorbinil is an Aldose reductase inhibitor. Sorbinil plays a therapeutic role in treating diabetes and diabetic complications decreases AR activity and inhibit the polyol pathway.

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

Finasteride (MK-906) is an oral inhibitor of active testosterone 5-alpha-reductase and Ki value is 10 nM.

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

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.

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

Dutasteride (GI 198745) is a 5-alpha-reductase inhibitor that inhibits both type-1 and type2 isoforms of the enzyme and is used to treat benign prostatic hyperplasia.

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).

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.

Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.

TrxR1-IN-B19 (TrxR1 IN B19), a TrxR1 inhibitor, selectively kills gastric cancer cells by a small molecule via targeting TrxR1 and ROS-mediated ER stress activation.

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

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.