Camptothecin metabolism

Author: wesd

August undefined, 2024

WebPurpose: Camptothecin (CPT) is a potent topoisomerase I inhibitor that has recently been undergoing phase I clinical trials.Though CPT shows high activity against various tumor cells, its biotransformation is still unknown. To investigate the metabolism and biliary excretion of CPT, an isolated perfused rat liver system was used. WebJun 10, 2024 · On the basis of annotated metabolites and enzymes identified 11, the camptothecin biosynthetic pathway in C. acuminata is similar to that of some other MIAs, such as vinblastine and vincristine...

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WebCamptothecin (CPT, 1) is a plant alkaloid from the Camptotheca acuminata tree. 83 In in vitro assay, camptothecin exhibited excellent topoisomerase I inhibitory activity but poor … WebOct 10, 2024 · Nanomaterials have broad application prospects in the biomedical field because of their unique characteristics. Drug delivery based on nanoparticles has been extensively studied to maximize the therapeutic efficacy of drugs [].Among the diverse nanomaterials that have been found, graphene and its derivatives have been … cycloplegics and mydriatics

Camptothecin Cell Signaling Technology

WebJun 13, 2024 · Camptothecin is a potent anticancer drug which inhibits the enzyme, deoxyribonucleic acid topoisomerase I, during the S-phase of cell cycle (Zunino et al. 2002 ). Deoxyribonucleic acid topoisomerase I is an enzyme which is essential for replication and transcription of deoxyribonucleic acid. WebSep 11, 2007 · Camptothecin 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. Type Small Molecule Groups Experimental Structure Similar … WebA recent study confirmed that Camptothecin could downregulate SLC25A6 and induce apoptosis in a mitochondria-dependent pathway . SLC25A6 isoforms are expressed in all tissues and in cultured fibroblasts at levels that depend on the state of oxidative metabolism [ … cyclopithecus

Metabolism of camptothecin, a potent topoisomerase I

The impact of camptothecin-encapsulated poly (lactic-

WebMay 16, 2014 · Specialties: Bioinformatics, R, Linux, Gene Sequencing, Biomarker discovery, Environmental Health Sciences, Toxicology, Radiation Oncology Learn more about Karan B.'s work experience, education ... cyclopinclopanWebMar 2, 2001 · The camptothecins are a new class of chemotherapeutic radiation sensitizers. Clinical trials with camptothecins alone show higher toxicity than predicted by preclinical models, which has created the challenge of finding new ABSTRACT: The camptothecins are a new class of chemotherapeutic radiationsensitizers. cycloplegic eye refraction

"WebPharmacodynamics. Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. DNA topoisomerases are enzymes in the cell nucleus that regulate DNA topology (3-dimensional conformation) and facilitate … " - Camptothecin metabolism

Camptothecin metabolism

Frontiers Microbiota-Host-Irinotecan Axis: A New Insight Toward ...

WebJul 1, 2005 · 7-Ethyl-10-hydroxy-camptothecin (SN-38), the active metabolite of the anti-cancer agent irinotecan, contains a lactone ring that equilibrates with a carboxylate form. Since SN-38 lactone is the active and toxic form, it is prudent to examine whether the more soluble carboxylate is a surrogate for SN-38 lactone conjugation. Therefore, relative … WebMar 1, 1990 · A new water-soluble derivative of camptothecin, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11), did not exhibit potent antitumor activity …

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WebDec 1, 1999 · Camptothecin Resistance: Role of the ATP-binding Cassette (ABC), Mitoxantrone-resistance Half-Transporter (MXR), and Potential for Glucuronidation in MXR-expressing Cells. ... Although the importance of glucuronidation in hepatic drug metabolism is well known, it has received little attention as a possible mechanism of resistance in … WebThe hairy roots (HR) of Ophiorrhiza pumila produce camptothecin (CPT), a monoterpenoid indole alkaloid used as a precursor in the synthesis of chemotherapeutic drugs. O. pumila HR culture is considered as a promising alternative source of CPT,

WebOct 1, 2006 · a Camptothecin is a 5-ring heterocyclic alkaloid that contains an a-hydroxylactone within its E-ring that is unstable at physiological pH. For all camptothecin derivatives, the carboxylate... WebOct 14, 2024 · The active metabolite ethyl-10-hydroxy-camptothecin (SN38) has been shown to significantly increase expression of p53 protein and pro-apoptosis proteins Bax, caspase-3, and caspase-9 in human hepatocellular carcinoma cell lines, and meanwhile decrease expression of the anti-apoptosis protein B-cell lymphoma (Bcl)-xL ( Takeba et …

WebMay 1, 2024 · The camptothecin-derived agents exert their antitumor activities by specifically stabilizing the Top1–DNA covalent complexes (Top1cc) and blocking the DNA religation step. When exposed to these DNA damage agents, tumor cells quickly activate DNA damage response. WebCamptothecin is a cytotoxic plant alkaloid originally isolated from C. acuminate that inhibits DNA and RNA synthesis in mammalian cells and is an effective anti-tumor agent (1). Research studies indicate that camptothecin inhibits topoisomerase I with an IC 50 of 679 nM (2). Camptothecin binds and stabilizes topoisomerase I–DNA cleavage ...

WebOct 15, 2024 · Camptothecin is a planar pentacyclic quinoline alkaloid with a molecular formula of C 20 H 16 N 2 O 4, and is insoluble in water. Ring A and B are quinoline rings, ring C is pyrrole ring, ring D is pyridone ring, and ring E is α-hydroxy lactone ring.

WebDec 31, 2013 · Camptothecin (CPT) is a water-insoluble tryptophan-derived quinolone alkaloid and is a lead compound for two FDA (Food and Drug Administration) approved antineoplastic drugs, irinotecan and... cycloplegic mechanism of actionWebAug 1, 2001 · Of the currently available camptothecin analogues, CPT-11 has an extremely complex pharmacological profile, which is dependent on a host of enzymes involved in … cyclophyllidean tapewormsWebMar 24, 2024 · Untargeted analyses revealed that treatments with MeJa, AgNO 3, and PEG significantly inhibited the photosynthetic pathway and promoted carbon metabolism and secondary metabolic pathways. The CPT levels increased by 78.6, 73.3, and 50.0% in the MeJa, AgNO 3, and PEG treatment groups, respectively. cycloplegic refraction slideshareWeb5μM Camptothecin作用于HCT116细胞，诱导蛋白酶体调节的混合系白血病5(MLL5)蛋白降解，导致p53在Ser392位点磷酸化。由于Camptothecin的溶解性低及具有一定副作用，所以已经研发了多种Camptothecin类似物，其中两种如Topotecan和Irinotecan,已经获得FDA准核，用于癌症化学疗法中。 cyclophyllum coprosmoidesWebCamptothecin. Camptothecin is a naturally occurring alkaloid derived from the plant Camptotheca acuminata that was identified in an anticancer drug discovery screen in the … cyclopiteWebMar 22, 2024 · Antibody–drug conjugate (ADC) is typically composed of a monoclonal antibody (mAbs) covalently attached to a cytotoxic drug via a chemical linker. It combines both the advantages of highly ... cyclop junctionsWebCamptothecin (CPT) is a pentacyclic alkaloid that was first isolated from stem wood of Camptotheca acuminata by botanists working in the USDA’s Plant Introduction Division in the mid-1950s ( Wall et al., 1966 ). cycloplegic mydriatics