10-Hydroxycamptothecin/1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 4-ethyl-4,9-dihydroxy-, (4S)-/hydroxycamtothecine/Camptothecin, 10-hydroxy/9-hydroxy-20(S)-camptothecin/10-hydroxy-Camptothecin/9-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g] chromene-5,10-dione/(4S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione/3,4-dihydro-9-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10
Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
820.7±65.0 °C at 760 mmHg
HS Code Reference
Personal Projective Equipment
For Reference Standard and R&D, Not for Human Use Directly.
provides coniferyl ferulate(CAS#:67656-30-8) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Natural bioactive derivatives of camptothecin (CPT), 10-methoxycamptothecin (MCPT) and 10-hydroxycamptothecin (HCPT) have been confirmed to possess high antitumor activities. MCPT could be metabolized to HCPT in vivo. The HPLC method for the quantification of MCPT and HCPT was established and validated, and the pharmacokinetics and the tissue distribution of MCPT in rats after i.v. administration have been well carried out in our previous studies. To improve the further understanding of the in vivo behavior of MCPT, a rapid and sensitive UPLC-MS/MS method was developed and validated for the quantification of MCPT and HCPT in plasma and tissue samples, and the pharmacokinetics and tissue distribution as well as the bioavailability of MCPT after i.g. were also illustrated. The results showed that MCPT could be highly converted to its active metabolite HCPT in plasma with the AUC0-∞ value of (185.28±61.73) ngh/mL and (717.25±165.67) ngh/mL for MCPT and HCPT, respectively. Meanwhile, MCPT and HCPT were rapidly absorbed and diffused into all the tested tissues (heart, liver, spleen, lung, kidney and brain) after i.g. administration. Similar with the results after i.v. administration of MCPT, MCPT concentration in lung tissue was also extremely higher than in other tested tissues, which implied that MCPT might have a great potential for the treatment of lung cancer.
10-hydroxycamptothecin; 10-methoxycamptothecin; Oral bioavailability; UPLC-MS/MS.
Pharmacokinetics and Tissue Distribution Study of 10-methoxycamptothecin in Rats Following Intragastric Administration
Jian Zheng 1, Yong Ji 1, Changmin Shao 1, Lijia Jing 1, Yang Wang 2
2018 Feb 5;
Nanoparticles based on hybrid block copolymers had been expected as effective nanocarriers for hydrophobic drug delivery. Herein, the novel dendritic-linear molecules from OEG dendron conjugated with octadecylamine (G2-C18) was designed, synthesized, and further applied as nanocarrier to prepare 10-hydroxycamptothecin (HCPT) nanoparticles via antisolvent precipitation method. It seemed that the feed weight ratio of HCPT vs G2-C18 not only affected the drug-loading content of nanoparticles but also influenced the morphology of HCPT nanoparticles; the morphology of HCPT nanoparticles was changed from nanosphere (NSs) to nanorod (NRs) with increasing the feed weight ratio. Both of HCPT nanoparticles presented good stability and similar drug release profiles, but different anticancer efficacy and cellular uptake mechanism. The cytotoxicity of HCPT NRs was enhanced significant comparing with HCPT NSs, the IC50 value was 2-fold lower than HCPT NSs ( p < 0.05). More importantly, HCPT NRs showed apparently higher antitumor activity in vivo, the inhibition rate of HCPT NRs was 1.3-fold higher than HCPT NSs. Based on these results, it suggested that the antitumor activity could be influenced significantly by particle morphology, which should be considered and optimized during the nanocarrier design.
antitumor efficacy; dendritic linear molecules; self-assembly mechanism; shape-dependent property.
Amphiphilic Hybrid Dendritic-Linear Molecules as Nanocarriers for Shape-Dependent Antitumor Drug Delivery
Yifei Guo 1, Ting Wang 1 2, Shuang Zhao 1, Meihua Han 1, Zhengqi Dong 1, Xiangtao Wang 1, Yanhong Wang 2
2018 Jul 2
The medicinal plant Camptotheca acuminata accumulates camptothecin, 10-hydroxycamptothecin, and 10-methoxycamptothecin as its major bioactive monoterpene indole alkaloids. Here, we describe identification and functional characterization of 10-hydroxycamptothecin O-methyltransferase (Ca10OMT), a member of the Diverse subclade of class II OMTs. Ca10OMT is highly active toward both its alkaloid substrate and a wide range of flavonoids in vitro and in this way contrasts with other alkaloid OMTs in the subclade that only utilize alkaloid substrates. Ca10OMT shows a strong preference for the A-ring 7-OH of flavonoids, which is structurally equivalent to the 10-OH of 10-hydroxycamptothecin. The substrates of other alkaloid OMTs in the subclade bear little similarity to flavonoids, but the 3-D positioning of the 7-OH, A- and C-rings of flavonoids is nearly identical to the 10-OH, A- and B-rings of 10-hydroxycamptothecin. This structural similarity likely explains the retention of flavonoid OMT activity by Ca10OMT and also why kaempferol and quercetin aglycones are potent inhibitors of its 10-hydroxycamptothecin activity. The catalytic promiscuity and strong inhibition of Ca10OMT by flavonoid aglycones in vitro prompted us to investigate the potential physiological roles of the enzyme in vivo. Based on its regioselectivity, kinetic parameters and absence of 7-OMT flavonoids in vivo, we conclude that the major and likely only substrate of Ca10OMTin vivo is 10-hydroxycamptothecin. This is likely accomplished by Ca10OMT being kept spatially separated at the tissue levels from potentially inhibitory flavonoid aglycones, and flavonoid aglycones being rapidly glycosylated to non-inhibitory flavonoid glycosides.
Camptotheca acuminata; O-methyltransferase; alkaloid; camptothecin; flavonoids; medicinal plant; specialized metabolism.
Camptotheca Acuminata 10-hydroxycamptothecin O-methyltransferase: An Alkaloid Biosynthetic Enzyme Co-Opted From Flavonoid Metabolism
Vonny Salim 1, A Daniel Jones 1 2, Dean DellaPenna 1