In vivo Effect of Didemnin B on Two Tumors of the Rat

Fimiani, Vincenzo

doi:10.1159/000226441

Cited by 21 publications

(14 citation statements)

References 4 publications

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“…The compound also exhibited antiviral and antitumor activities more active than didemnin A. Some antitumor tests were also evaluated against human tumor stem cell assay [153] and Yoshida ascites tumor through in vivo analysis [154]. Some antitumor tests were also evaluated against human tumor stem cell assay [153] and Yoshida ascites tumor through in vivo analysis [154].…”

Section: Biological Activitymentioning

confidence: 99%

Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides

Maharani

Sleebs

Hughes³

2015

Studies in Natural Products Chemistry

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Section: Biological Activitymentioning

confidence: 99%

Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides

Maharani

Sleebs

Hughes³

2015

Studies in Natural Products Chemistry

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“…Three mice each were randomly assigned to high-and low-dose groups given didemnin B at 1280 mg/kg or 320 mg/kg, or a control group given 0.8 ml of vehicle. Each lowand high-dose mouse was given 272 mg/kg of their total didemnin B dose as [ 3 H]didemnin B. Urine and feces were collected at 3,6,9,12,15,18,21,24,30,36,42,48,60,72,84,96,108,120,132,144,156 and 168 h after administration of [ 3 H]didemnin B. At 168 h, mice were anesthetized with xylazine and ketamine hydrochloride and exsanguinated via cardiac puncture.…”

Section: Animals Dosing and Specimen Collectionmentioning

confidence: 99%

“…Didemnin B (NSC 325319) and related compounds are in preclinical and clinical trials as anticancer, antiviral and immunosuppressive drugs [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17]. In mice, didemnin B protected against intraperitoneally (i.p.)…”

Section: Introductionmentioning

confidence: 99%

Fate of tritiated didemnin B in mice: excretion and tissue concentrations after an intraperitoneal dose

Beasley

Bruno

Burner

et al. 2005

Biopharm. Drug Dispos.

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Didemnin B has undergone trials in cancer patients, and has antiviral and immunosuppressive properties. [(3)H]didemnin B was administered intraperitoneally (i.p.) to mice at 320 or 1280 microg/kg. Urine and feces were collected until 168 h, at which time the mice were killed and tissues collected. Additionally, [(3)H]didemnin B was given i.p. at 320 microg/kg, and mice were killed at 1-120 h post-dosing. Radiolabel increased rapidly in blood then rapidly declined. Most radiolabel in urine, feces and tissues represented parent compound. Concentrations of [(3)H]didemnin B were greatest in the liver > gallbladder > lower digestive tract congruent with pancreas > spleen > kidney congruent with adipose tissue congruent with urinary bladder with urine. The pancreas had the longest terminal half-life of the tissues and the highest radioactivity at 7 days. Intermediate concentrations were in the duodenum congruent with jejunum > lung > iliopsoas > stomach congruent with testes congruent with skin > heart. Low concentrations were in the humerus congruent with femur congruent with quadriceps congruent with triceps >> brain. Fecal excretion accounted for 45.9%-58.3% of the dose and declined after 24 h, followed by an increase, suggesting possible enterohepatic recycling or an impact of circadian rhythms. Urinary excretion accounted for 18.4%-25.2% of the dose, but was minimal after 24 h. The concentrations were highest in organs previously found to be sensitive in animals and humans. Didemnin B should be evaluated in animal models for treatment of pancreatic cancer.

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“…Fimiani 36 reported that doses of 0.06 mg/kg were non-toxic but highly effective against Yoshida ascites tumors in rats. The report also noted, however, that intraperitoneal injection was required, since drug delivery by other routes was ineffective.…”

Section: Antitumor Activitymentioning

confidence: 99%

Natural products as probes of cell biology: 20 years of didemnin research

Vera

Joullié

2002

Medicinal Research Reviews

143

109

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The discovery of the didemnin family of marine depsipeptides launched an exciting and intriguing chapter in natural product chemistry. The unusual structure of the didemnin congeners has led to several total syntheses by research groups from around the world. The impressive in vitro and in vivo biological activities of the didemnins resulted in the first human clinical trials in the U.S. of a marine natural product against cancer, and additional clinical trials of a second-generation didemnin, dehydrodidemnin B (aplidine), are underway. As we mark the 20-year anniversary of the discovery of the didemnins, this class of natural products continues to stimulate active research in fields ranging from synthetic and medicinal chemistry to clinical oncology and cell biology. While some progress was made in dissecting the molecular mechanism of action and in establishing structure-activity relationships, there are still more questions than answers. This review covers the recent didemnin literature, highlighting the work directed towards understanding how this group of natural products interact with fundamental processes such as cell proliferation, protein biosynthesis, and apoptosis. The didemnin field illustrates how natural product chemistry may be used as a critical tool for the study of cell biology.

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In vivo Effect of Didemnin B on Two Tumors of the Rat

Cited by 21 publications

References 4 publications

Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides

Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides

Fate of tritiated didemnin B in mice: excretion and tissue concentrations after an intraperitoneal dose

Natural products as probes of cell biology: 20 years of didemnin research

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