ChemInform Abstract: Studies on Rubia akane (RA) Derivatives. Part 11. Novel Water-Soluble Analogues (I) Retaining Potent Antitumor Activity of RA-VII, a Cyclic Hexapeptide from Rubia Plants

ChemInform ◽  
2010 ◽  
Vol 29 (17) ◽  
pp. no-no
Author(s):  
H. ITOKAWA ◽  
et al. et al.
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Cyclic Hexapeptide ◽  
Rubia Akane

Novel water-soluble analogues retaining potent antitumor activity of RA-VII, a cyclic hexapeptide from Rubia plants

1997 ◽  
Vol 7 (24) ◽  
pp. 3125-3128 ◽  
Author(s):  
Yukio Hitotsuyanagi ◽  
Yoshiaki Anazawa ◽  
Takehiro Yamagishi ◽  
Kazunori Samata ◽  
Tomoko Ichihara ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Cyclic Hexapeptide

Novel water soluble phosphate prodrugs of taxol® possessing in vivo antitumor activity

1993 ◽  
Vol 3 (8) ◽  
pp. 1761-1766 ◽  
Author(s):  
Yasutsugu Ueda ◽  
Amarendra B. Mikkilineni ◽  
Jay O. Knipe ◽  
William C. Rose ◽  
Anna Maria Casazza ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Soluble Phosphate ◽  
In Vivo Antitumor Activity

scholarly journals Epigallocatechin Gallate-Gold Nanoparticles Exhibit Superior Antitumor Activity Compared to Conventional Gold Nanoparticles: Potential Synergistic Interactions

Nanomaterials ◽  
2019 ◽  
Vol 9 (3) ◽  
pp. 396 ◽  
Author(s):  
Suhash Chavva ◽  
Sachin Deshmukh ◽  
Rajashekhar Kanchanapally ◽  
Nikhil Tyagi ◽  
Jason Coym ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Nuclear Translocation ◽  
Epigallocatechin Gallate ◽  
Drug Carriers ◽  
Water Soluble ◽  
Tetrazolium Salt ◽  
Uptake Studies

Epigallocatechin gallate (EGCG) possesses significant antitumor activity and binds to laminin receptors, overexpressed on cancer cells, with high affinity. Gold nanoparticles (GNPs) serve as excellent drug carriers and protect the conjugated drug from enzymatic metabolization. Citrate-gold nanoparticles (C-GNPs) and EGCG-gold nanoparticles (E-GNPs) were synthesized by reduction methods and characterized with UV-visible spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering (DLS). Cytotoxicity of citrate, EGCG, C-GNPs, and E-GNPs was evaluated by the water-soluble tetrazolium salt (WST-1) assay. Nanoparticle cellular uptake studies were performed by TEM and atomic absorption spectroscopy (AAS). Dialysis method was employed to assess drug release. Cell viability studies showed greater growth inhibition by E-GNPs compared to EGCG or C-GNPs. Cellular uptake studies revealed that, unlike C-GNPs, E-GNPs were taken up more efficiently by cancerous cells than noncancerous cells. We found that E-GNP nanoformulation releases EGCG in a sustained fashion. Furthermore, data showed that E-GNPs induced more apoptosis in cancer cells compared to EGCG and C-GNPs. From the mechanistic standpoint, we observed that E-GNPs inhibited the nuclear translocation and transcriptional activity of nuclear factor-kappaB (NF-κB) with greater potency than EGCG, whereas C-GNPs were only minimally effective. Altogether, our data suggest that E-GNPs can serve as potent tumor-selective chemotoxic agents.

DX-8951f, a Hexacyclic Camptothecin Analog, on a Daily-Times-Five Schedule: A Phase I and Pharmacokinetic Study in Patients With Advanced Solid Malignancies

2000 ◽  
Vol 18 (17) ◽  
pp. 3151-3163 ◽  
Author(s):  
Eric K. Rowinsky ◽  
Thomas R. Johnson ◽  
Charles E. Geyer ◽  
Lisa A. Hammond ◽  
S. Gail Eckhardt ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Dose Level ◽  
Compartment Model ◽  
Maximum Tolerated Dose ◽  
Preliminary Evidence ◽  
Water Soluble ◽  
Severe Thrombocytopenia ◽  
Phase Ii Studies ◽  
Solid Malignancies ◽  
Wide Range

PURPOSE: To assess the feasibility of administering DX-8951f (exatecan mesylate), a water-soluble, camptothecin analog, as a 30-minute intravenous infusion daily for 5 days every 3 weeks, determine the maximum-tolerated dose (MTD) and pharmacokinetic (PK) behavior of DX-8951f, and seek preliminary evidence of anticancer activity. PATIENTS AND METHODS: Patients with advanced solid malignancies were treated with escalating doses of DX-8951f. After three patients were treated at the first dose level, doses were to be escalated in increments of 100%, using a single patient at each dose level unless moderate toxicity was observed. The MTD, defined as the highest dose level at which the incidence of dose-limiting toxicity did not exceed 20%, was calculated separately for minimally pretreated (MP) and heavily pretreated (HP) patients. The PK and excretory profiles of DX-8951, the anhydrous form of DX-8951f, were also characterized. RESULTS: Thirty-six patients were treated with 130 courses of DX-8951f at six dose levels ranging from 0.1 to 0.6 mg/m2/d. Brief, noncumulative neutropenia was the most common toxicity observed. Severe myelosuppression (neutropenia that was protracted and/or associated with fever and/or severe thrombocytopenia) was consistently experienced by HP and MP patients at doses exceeding 0.3 and 0.5 mg/m2/d, respectively. Nonhematologic toxicities (nausea, vomiting, and diarrhea) were also observed, but these effects were rarely severe. Objective antitumor activity included partial responses in one patient each with platinum-resistant extrapulmonary small-cell and fluoropyrimidine- and irinotecan-resistant colorectal carcinoma, and minor responses in patients with prostate, hepatocellular, thymic, primary peritoneal, and irinotecan-resistant colorectal carcinomas. The PKs of total DX-8951 were linear and well fit by a three-compartment model. CONCLUSION: The recommended doses for phase II studies of DX-8951f as a 30-minute infusion daily for 5 days every 3 weeks are 0.5 and 0.3 mg/m2/d for MP and HP patients, respectively. The characteristics of the myelosuppressive effects of DX-8951f, paucity of severe nonhematologic toxicities, and antitumor activity against a wide range of malignancies warrant broad disease-directed evaluations of DX-8951f on this schedule.

Physicochemical Characterization and Antitumor Activity of Water-Soluble Polysaccharides from Bupleurum chinense

2015 ◽  
Vol 51 (5) ◽  
pp. 939-940
Author(s):  
Haibin Tong ◽  
Feng-e Li ◽  
Zhongmei He ◽  
Xiangfu Song ◽  
Shuwen Guan ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Physicochemical Characterization ◽  
Water Soluble

A Novel Water-Soluble Heptaplatin Analogue with Improved Antitumor Activity and Reduced Toxicity

2011 ◽  
Vol 50 (12) ◽  
pp. 5324-5326 ◽  
Author(s):  
Weiping Liu ◽  
Xizhu Chen ◽  
Qingsong Ye ◽  
Yongping Xu ◽  
Chengying Xie ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Reduced Toxicity
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