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 is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

(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.

Aclacinomycin A hydrochloride (Aclarubicin HCl) is an anthracycline antibiotic and inhibitor of topoisomerase I II, interfering with DNA transcription and replication, inhibiting tumour invasion and angiogenesis, generating reactive oxygen species (ROS), and inhibiting the catalytic centre of the 20S proteasome. It is indicated for the treatment of relapsed leukaemia and advanced malignant lymphoma.

(±)-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.

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

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

Eupolauridine is a selective DNA topoisomerase II inhibitor, exhibiting an IC50 of 20 μM against fungal topoisomerase I and 33 μM for human topoisomerase I. By inhibiting the catalytic activity of topoisomerase II, Eupolauridine stabilizes the enzyme's cleavage complex with DNA, resulting in DNA damage and imparting antifungal activity. [Eupolauridine] holds potential for the study of fungal infectious diseases.

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.