Camptothecin prodrug
WebIntroduction. Camptothecin (CPT) is a naturally occurring alkaloid with potent antineoplastic activity against a broad spectrum of solid tumors (eg, primary and metastatic colon carcinoma, small cell lung carcinoma, and ovarian, breast, pancreatic, and stomach cancers), which inhibits DNA topoisomerase I. 1 SN38 (7-ethyl-10-hydroxyl … WebIt is well known that camptothecin (CPT), which inhibits topoisomerase Ⅰ activity, has significant anticancer activity against various solid tumors in vitro. 29, 30 However, the major problem encountered with CPT is its extremely low solubility and side effects, which lead to the failure of clinical treatment. 31 In order to overcome the problem, …
Camptothecin prodrug
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WebNov 14, 2003 · Abstract. 7-Ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (irinotecan, CPT-11) is a camptothecin prodrug that is metabolized by carboxylesterases (CE) to the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38), a topoisomerase I inhibitor. CPT-11 has shown encouraging antitumor activity against a broad spectrum of …
WebDec 15, 2024 · In this study, we report the synthesis and biological evaluation of the β-glucuronidase-reactive albumin-binding prodrug Mal-glu-CPTS0001 (Fig. 2 A) [40].The … WebFeb 16, 2024 · The aim of this study was to prepare small-molecule camptothecin (CPT) prodrugs and evaluate their effectiveness in colorectal carcinoma therapy. Prodrug nanoparticles (NPs) were physicochemically characterized and evaluated for their cytotoxicity in human colon cancer (HCT116) cell lines. The antitumor efficacy of the NPs …
WebCamptothecin and lactose act as the chemotherapy drug and targeting ligand in the drug delivery system, respectively. Since CPT-S-S-LA is an amphiphilic compound, it can self-assemble into nanoparticles with a diameter of around 110 nm. The CPT-S-S-LA nanoparticles displayed controllable drug release behavior in the physiological environment. 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 …
WebSep 20, 2024 · The construction of prodrug and glucose oxidase coloaded alginate (ALG) hydrogels for PDT-combined chemotherapy of melanoma will provide a promising injectable hydrogel platform for effective treatments of cancer. Biomimetic nanoprodrugs from fatty acid modified camptothecin and albumin for enhanced pharmacotherapy.
WebOct 15, 2006 · A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate … can motorcycles go in reverseWebJul 12, 2024 · Prodrug–prodrug activation Camptothecin 4 is a topoisomerase I inhibitor that induces S-phase specific cell death. Since its discovery in the 1960's, several camptothecin derivatives and prodrugs have been reported with the aim of overcoming the drawbacks associated with camptothecin such as solubility and the stability of the … can motorcycles go through drive throughsWebA novel amphiphilic camptothecin prodrug that spontaneously arranges into nanomicelles which preferentially release the cytotoxic drug under tumor-relevant reductive conditions is designed. You have access to this article fix hole in plastic bathtubWebCamptothecin (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 … can motorcycles helmet block bulletsWebFeb 4, 2024 · Conventional chemotherapy and targeted therapy promote the antitumor immune response by increasing the immunogenicity of tumor cells, improving CD8+ T cell infiltration, or inhibiting immunosuppressive cells in the tumor microenvironment. fix hole in plaster wallWebDec 5, 2024 · The highly toxic payloads, for instance, maytansine, camptothecin derivatives, auristatin, or doxorubicin are recommended to choose in the conjugates. 9 Finally, ... To create a TfR targeted prodrug of DM1, the TfR binding peptide B6 was designed to conjugate with DM1 through the side chain of cysteine at the C-terminus via … can motorcycles ride in hov laneWebOct 21, 2024 · A camptothecin prodrug induces mitochondria-mediated apoptosis in cancer cells with cascade activations. Mitochondria are crucial regulators of the … fix hole in plasterboard wall