Pharmacokinetics of Tiqueside (β‐Tigogenin Cellobioside) in Dogs, Rats, Rabbits, and Monkeys†

Inskeep, Philip B.; Connolly, Ann G.; Cole, Mark J.; Luther, Elbridge W.; Biehl, Michael; Marzetta, Carol A.; Savoy, Yvette E.; Silber, B. Michael

doi:10.1002/jps.2600840105

Cited by 2 publications

(5 citation statements)

References 6 publications

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“…These data indicate that pamaqueside also inhibits the absorption of biliary or endogenous cholesterol as well as dietary cholesterol. Rabbits had relatively higher plasma levels of CAI after oral administration than did hamsters or dogs (26,31). Thus, it is conceivable, and perhaps more likely in rabbits than in other species, that systemic mechanisms could contribute to TPC lowering.…”

Section: Discussionmentioning

confidence: 99%

“…Upper and lower limits of quantitation for the assay were 15 mg/ml and 100 ng/ml, respectively. Plasma tiqueside concentrations were determined using a reverse phase HPLC system with detection on a Sciex API III mass spectrometer as previously described (31).…”

Section: Methodsmentioning

confidence: 99%

“…Although both synthetic saponins are poorly absorbed, high doses of pamaqueside and tiqueside yield measurable plasma levels (26,31). To examine potential systemic actions of these agents, rabbits were administered a choles-Fig.…”

Section: Administrationmentioning

confidence: 99%

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Comparison of synthetic saponin cholesterol absorption inhibitors in rabbits: evidence for a non-stoichiometric, intestinal mechanism of action

Morehouse

Bangerter

DeNinno

et al. 1999

Journal of Lipid Research

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The hypocholesterolemic activities of pamaqueside and tiqueside, two structurally similar saponins, were evaluated in cholesterol-fed rabbits. The pharmacological profiles of the saponins were virtually identical: both dosedependently decreased the intestinal absorption of labeled cholesterol 25-75%, increased fecal neutral sterol excretion up to 2.5-fold, and decreased hepatic cholesterol content 10-55%. High doses of pamaqueside ( Ͼ 5 mg/kg) or tiqueside ( Ͼ 125 mg/kg) completely prevented hypercholesterolemia. Decreases in plasma and hepatic cholesterol levels were strongly correlated with increased neutral sterol excretion. Ratios of neutral sterol excreted to pamaqueside administered were greater than 1:1 at all doses, in opposition to the formation of a stoichiometric complex previously suggested for tiqueside and other saponins. Ratios in tiqueside-treated rabbits were less than unity, a reflection of its lower potency. Pamaqueside-treated rabbits exhibited a more rapid decline in plasma cholesterol concentrations than control animals fed a cholesterol-free diet, indicating that the compound also inhibited the absorption of biliary cholesterol. Intravenous administration of pamaqueside had no effect on plasma cholesterol levels despite plasma levels twice those observed in rabbits given pamaqueside orally. These data indicate that pamaqueside and tiqueside induce hypocholesterolemia by blocking lumenal cholesterol absorption via a mechanism that apparently differs from the stoichiometric complexation of cholesterol hypothesized for other saponins. -Morehouse, L.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Comparison of synthetic saponin cholesterol absorption inhibitors in rabbits: evidence for a non-stoichiometric, intestinal mechanism of action

Morehouse

Bangerter

DeNinno

et al. 1999

Journal of Lipid Research

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“…These effects were associated with a decrease in fractional cholesterol absorption and increased excretion of fecal neutral sterols. The bioavailability of 2 in dogs was low (1.7%), but not insignificant …”

mentioning

confidence: 83%

“…The bioavailability of 2 in dogs was low (1.7%), but not insignificant. 10 Although these results were encouraging, 2 appeared limited by its weak potency and its higher than necessary bioavailability.…”

mentioning

confidence: 99%

11-Ketotigogenin Cellobioside (Pamaqueside): A Potent Cholesterol Absorption Inhibitor in the Hamster

et al. 1996

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Pharmacokinetics of Tiqueside (β‐Tigogenin Cellobioside) in Dogs, Rats, Rabbits, and Monkeys†

Cited by 2 publications

References 6 publications

Comparison of synthetic saponin cholesterol absorption inhibitors in rabbits: evidence for a non-stoichiometric, intestinal mechanism of action

Comparison of synthetic saponin cholesterol absorption inhibitors in rabbits: evidence for a non-stoichiometric, intestinal mechanism of action

11-Ketotigogenin Cellobioside (Pamaqueside): A Potent Cholesterol Absorption Inhibitor in the Hamster

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