Jineol (NSC-694081) is a quinoline alkaloid from Scolopendra subspinipes. Jineol shows cytotoxic activity against the growth of human tumor cell lines in vitro.
Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) shows human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity, with IC50 values of 0.83 +/- 0.04 microM and 4.20 +/- 0.19 microM, respectively.
SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.
6-Methoxydihydrosanguinarine is a natural product. 6-Methoxydihydrosanguinarine shows strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μM and 0.54 μM, respectively.It has antibacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) ranging from1.9 to 3.9 microg/ml
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.
Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.
1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I/R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho/ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.
1. Phellodendrine (Phallodendrin) has anti-nephritic activity, may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.
Dictamine (Dectamine) shows anticholinesterase, anti-inflammatory, mutagenic, and has antimicrobial activity against bacteria and fungi. It has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells.
Dihydroevocarpine (1-methyl-2-tridecylquinolin-4-one) induces AML cytotoxicity, apoptosis and G0/G1 blockade, and inhibits tumor growth by inhibiting mTORC1/2 activity and the mTOR pathway in an acute myeloid leukemia (AML) xenograft model.
Schinifoline is a quinolone derivative extracted from Zanthoxylum schinifolium Sieb with cytotoxic activity that promotes radiosensitization of cancer cells, affects the cell cycle and apoptosis.
Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35/CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.
Rubitecan (9-Nitrocamptothecin) is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner.Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties.
Quinine is a natural cinchona alkaloid that has been used for centuries in the prevention and therapy of malaria. Quinine is also used for idiopathic muscle cramps. Quinine therapy has been associated with rare instances of hypersensitivity reactions which can be accompanied by hepatitis and mild jaundice.
(±)-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.
1. Dihydrochelerythrine (12,13-Dihydrochelerythrine) is nontoxic up to 5μM concentration. 2. Dihydrochelerythrine has antifungal activity against pathogenic plant fungi. 3. Dihydrochelerythrine has potential application in the therapy of serious infection caused by I. multifiliis. 4. Dihydrochelerythrine affects cell cycle distribution, activates mitochondrial apoptotic pathway, and induces apoptosis and necrosis in HL-6 cells.