(S)-10-Hydroxycamptothecin - CAS 19685-09-7
Catalog number: 19685-09-7
Category: Inhibitor
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10-Hydroxycamptothecin inhibits the growth of BT-20 and MDA-231 cell with IC50 of 34.3 nM and 7.27 nM, respectively, more potently than camptothecin (CPT) with IC50 of >500 nM.
10HCPT; 10OHCPT; Hydroxycamptothecin; 10hydroxycamptothecine; 10Hydroxy camptothecin; Hydroxycamptothecine; HCPT; 10HCPT; (S)10Hydroxycamptothecin; Camptothecin hydroxy10hydroxycamptothecin.
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1.Antitumor efficacy and intratumoral distribution of SN-38 from polymeric depots in brain tumor model.
Vejjasilpa K1, Nasongkla N2, Manaspon C1, Larbcharoensub N3, Boongird A4, Hongeng S5, Israsena N6. Exp Biol Med (Maywood). 2015 Dec;240(12):1640-7. doi: 10.1177/1535370215590819. Epub 2015 Jun 16.
We investigate antitumor efficacy and 2D and 3D intratumoral distribution of 7-ethyl-10-hydroxycamptothecin (SN-38) from polymeric depots inside U-87MG xenograft tumor model in nude mice. Results showed that polymeric depots could be used to administer and controlled release of a large amount of SN-38 directly to the brain tumor model. SN-38 released from depots suppressed tumor growth, where the extent of suppression greatly depended on doses and the number of depot injections. Tumor suppression of SN-38 from depots was three-fold higher in animals which received double injections of depots at high dose (9.7 mg of SN-38) compared to single injection (2.2 mg). H&E staining of tumor sections showed that the area of tumor cell death/survival of the former group was two-fold higher than those of the latter group. Fluorescence imaging based on self-fluorescent property of SN-38 was used to evaluate the intratumoral distribution of this drug compared to histological results.
2.Nanomicelle Based Peroral Delivery System for Enhanced Absorption and Sustained Release of 10-Hydrocamptothecin.
Tian Y, Shi C, Zhang X, Sun Y, Wang J, Zhang Y, Yang J, Wang L, Wang L, Mao S. J Biomed Nanotechnol. 2015 Feb;11(2):262-73.
An effective sustained-release peroral drug delivery system is needed for chemotherapy. Here, we show that such a system can be achieved by designing polymeric nanomicelles combining mucoadhesion, enhanced absorption and controlled release. Chitosan and glyceryl-monooleate have many desirable properties, so we synthesized a novel chitosan derivative, chitosan-conjugated glyceryl monooleate. We loaded 10-hydroxycamptothecin (HCPT) into the cores of nanomicelles by pH-coacervation, which significantly improved drug loading and stability. We studied the pharmacokinetics of these drug-loaded nanomicelles, and they demonstrated remarkably prolonged circulation time in vivo up to 72 h. Orally administered HCPT-loaded nanomicelles also showed comparable antitumor effects and smaller changes in body weight compared to HCPT administered by injection. Most importantly, by using in vivo pharmacokinetic and pharmacodynamic studies, we showed that comparable antitumor effects can be achieved by peroral administration of HCPT-loaded nanomicelles every three days, and that the nanomicelles had less severe side effects.
3.Amphiphilic drugs as surfactants to fabricate excipient-free stable nanodispersions of hydrophobic drugs for cancer chemotherapy.
Hu S1, Lee E2, Wang C3, Wang J1, Zhou Z1, Li Y2, Li X3, Tang J1, Lee DH2, Liu X1, Shen Y4. J Control Release. 2015 Dec 28;220(Pt A):175-9. doi: 10.1016/j.jconrel.2015.10.031. Epub 2015 Oct 19.
Nanoformulations have been extensively explored to deliver water-insoluble drugs, but they generally use exotic new materials, for instance, amphiphilic block copolymers, which must first go through extensively clinical trials and be approved as drug excipients before any clinical uses. We hypothesize that using clinical amphiphilic drugs as surfactants to self-assemble with and thus solubilize hydrophobic drugs will lead to readily translational nanoformulations as they contain no new excipients. Herein, we show the first example of such excipient-free nanodispersions using an amphiphilic anti-tumor drug, irinotecan hydrochloride (CPT11). CPT11 self-assembles with its insoluble active parent drug, 7-ethyl-10-hydroxy camptothecin (SN38), into stable and water-dispersible nanoparticles, increasing SN38's water solubility by thousands of times up to 25 mg/mL with a loading efficiency close to 100%. The versatility of this approach is also demonstrated by fabricating nanodispersions of CPT11 with other water-insoluble drugs including paclitaxel (PTX) and camptothecin (CPT).
4.Nanodrug Formed by Coassembly of Dual Anticancer Drugs to Inhibit Cancer Cell Drug Resistance.
Zhao Y1, Chen F1,2, Pan Y1, Li Z1, Xue X1,2, Okeke CI1,2, Wang Y1,2, Li C1, Peng L3, Wang PC4, Ma X1, Liang XJ1. ACS Appl Mater Interfaces. 2015 Sep 2;7(34):19295-305. doi: 10.1021/acsami.5b05347. Epub 2015 Aug 19.
Carrier-free pure nanodrugs (PNDs) that are composed entirely of pharmaceutically active molecules are regarded as promising candidates to be the next generation of drug formulations and are mainly formulated from supramolecular self-assembly of drug molecules. It benefits from the efficient use of drug compounds with poor aqueous solubility and takes advantage of nanoscale drug delivery systems. Here, a type of all-in-one nanoparticle consisting of multiple drugs with enhanced synergistic antiproliferation efficiency against drug-resistant cancer cells has been created. To nanoparticulate the anticancer drugs, 10-hydroxycamptothecin (HCPT) and doxorubicin (DOX) were chosen as a typical model. The resulting HD nanoparticles (HD NPs) were formulated by a "green" and convenient self-assembling method, and the water-solubility of 10-hydroxycamptothecin (HCPT) was improved 50-fold after nanosizing by coassembly with DOX. The formation process was studied by observing the morphological changes at various reaction times and molar ratios of DOX to HCPT.
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CAS 19685-09-7 (S)-10-Hydroxycamptothecin

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