dna topoisomerase i

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor used as a clinical therapeutic agent against hepatoma.

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.

(±)-10-Hydroxycamptothecin (Hydroxy Camptothecine) is an alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA topoisomerase, type I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.

Erythro-Austrobailignan-6, an orally active anti-cancer agent, inhibits DNA topoisomerase I and II activity, induces cell apoptosis, and enhances the phosphorylation of p38 and JNK.

Groenlandicine is a protoberberine alkaloid from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DN

Isodiospyrin is a novel human DNA topoisomerase I inhibitor, it exhibits cytotoxic activity to tumor cell lines. Isodiospyrin has antibacterial activity, the minimum inhibitory concentrations (MICs) against Gram-positive bacteria ranged from 0.78 to 50 mi

Podocarpusflavone A is a DNA topoisomerase I inhibitor with moderate anti-proliferative activity that induces cell apoptosis in MCF-7.