camptothecin/fever

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Sequence of treatment is important in the modification of camptothecin induced cell killing by hyperthermia.

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We investigated the modification of camptothecin (CPT)-induced cell killing by hyperthermia in a radioresistant human melanoma (Sk-Mel-3) and a human normal (AG1522) cell line. CPT, a topoisomerase (topo) I inhibitor, was given as a 1 h exposure at variable doses up to 34 microM; hyperthermia was

Simultaneous analysis of DNA replication and apoptosis during treatment of HL-60 cells with camptothecin and hyperthermia and mitogen stimulation of human lymphocytes.

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A new method is described which combines the identification of DNA replicating and apoptotic cells in a single measurement by flow cytometry. The detection of DNA replicating cells is based on incorporation of 5-bromo-2'-deoxyuridine or 5-iodo-2'-deoxyuridine, followed by selective photolysis at the

Pre-irradiation 9-amino [20s] camptothecin (9-AC) in patients with newly diagnosed glioblastoma multiforme.

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OBJECTIVE To evaluate the efficacy of 9-amino [20s] camptothecin (9-AC) given before radiation therapy to patients with newly diagnosed glioblastoma multiforme (GBM). METHODS Eligible patients had newly diagnosed GBM who had residual measurable contrast-enhancing tumor. The trial was a phase 2 trial

Phase I and pharmacokinetic study of the camptothecin analog DX-8951f administered as a 30-minute infusion every 3 weeks in patients with advanced cancer.

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OBJECTIVE DX-8951f is a totally synthetic derivative of camptothecin with greater cytotoxicity and more potent topoisomerase I inhibition than SN-38, topotecan, and camptothecin in preclinical studies. This phase I study aimed to describe the toxicity and to determine the maximum-tolerated dose

DX-8951f, a hexacyclic camptothecin analog, on a daily-times-five schedule: a phase I and pharmacokinetic study in patients with advanced solid malignancies.

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OBJECTIVE 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

Combined effects of hyperthermia and CPT-11 on DNA strand breaks in mouse mammary carcinoma FM3A cells.

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The interaction between hyperthermia and a DNA topoisomerase I inhibitor, 7-ethyl-10-(4-(1-piperidyl)-1-piperidyl)-carbonyloxy- camptothecin (CPT-11), was studied in the mouse mammary carcinoma FM3A cells. When the cells were treated with CPT-11 at a concentration of 5 micrograms/ml and 44 degrees C

Alternative administration of camptothecin analogues.

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The binding of camptothecin (CPT) to the DNA-topoisomerase complex is reversible, but it needs to be maintained for maximal inhibitory activity. It is also dependent on the chemical structure of CPT. The lactone form is thought to be necessary for the activity. In human serum, the equilibrium

Preclinical studies of water-insoluble camptothecin congeners: cytotoxicity, development of resistance, and combination treatments.

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Water-insoluble camptothecin (CPT) congeners are rapidly establishing themselves as promising anticancer drugs. In vitro, they have exhibited: (a) insensitivity to elevated levels of P-glycoprotein that confers multidrug resistance; (b) selective killing of malignant cells traversing the S-phase of

Biomodulation by hyperthermia of topoisomerase II-targeting drugs in human colorectal cancer cells.

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We examined whether heat stress could enhance the sensitivity of human colon cancer WiDr cells to topoisomerase II-targeting anticancer agents, etoposide (VP-16) and teniposide (VM-26), and also determined the most effective timing for the drug administration after exposure to hyperthermia. Both

Production of camptothecin in cultures of Chonemorpha grandiflora.

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BACKGROUND Chonemorpha grandiflora (Syn. Chonemorpha fragrans (Apocynaceae) is an endangered medicinal plant. It is used in different preparations, such as sudarsanasavam and kumaryasavam used in Kerala Ayurvedic system. C. grandiflora is used for the treatment of fever and stomach disorders.

Phase I pharmacological and bioavailability study of oral diflomotecan (BN80915), a novel E-ring-modified camptothecin analogue in adults with solid tumors.

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OBJECTIVE Diflomotecan (BN80915) is an E-ring modified camptothecin analogue that possesses greater lactone stability in plasma compared with other topoisomerase I inhibitors, a potential advantage for antitumor activity. As with other camptothecins, oral administration has pharmacological and

Promotive effects of hyperthermia on the cytostatic activity to Ehrlich ascites tumor cells by diverse delta-alkyllactones.

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OBJECTIVE To evaluate promotive effects of hyperthermia on antitumor activity of new delta-alkyllactones (DALs) of low molecular weight (184-254 Da), chemically synthesized, which are different from natural macrocyclic lactones of high molecular weight (348-439 Da), such as camptothecin and

The combination of hyperthermia or chemotherapy with gimeracil for effective radiosensitization.

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OBJECTIVE 5-chloro-2,4-dihydroxypyridine (gimeracil) is a component of the oral fluoropyrimidine derivative S-1. Gimeracil was originally added to S-1 to yield prolonged 5-fluorouracil (5-FU) concentrations in serum and tumor tissues by inhibiting dihydropyrimidine dehydrogenase, which degrades

Camptothecin and 9-nitrocamptothecin (9NC) as anti-cancer, anti-HIV and cell-differentiation agents. Development of resistance, enhancement of 9NC-induced activities and combination treatments in cell and animal models.

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The anticancer drug, 9-nitrocamptothecin (9NC), has demonstrated an unprecedented activity against human caner cells grown in cultures and as xenografts in nude mice. 9NC-induced apoptosis of cancer cells is mediated by the nuclear enzyme, topoisomerase I, and executed by pathways that involve

Lineage-related susceptibility of human hemopoietic cell lines to apoptosis.

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Apoptosis plays a fundamental role in shaping normal hematopoiesis. We have investigated the relationship existing between susceptibility to apoptosis and lineage commitment in hemopoietic cells. The presence and degree of apoptosis were investigated in myeloid (HL-60 and K562), T (Jurkat and

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