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Title: Pharmacokinetics of cucurbitacin B from Trichosanthes cucumerina L. in rats
Authors: Natthaphon Hunsakunachai
Nitra Nuengchamnong
Weena Jiratchariyakul
Tanawan Kummalue
Phisit Khemawoot
Chulalongkorn University
Naresuan University
Mahidol University
Faculty of Medicine, Siriraj Hospital, Mahidol University
Keywords: Medicine
Issue Date: 4-Jul-2019
Citation: BMC Complementary and Alternative Medicine. Vol.19, No.1 (2019)
Abstract: © 2019 The Author(s). Background: Cucurbitacin B is the major bioactive constituent in Trichosanthes cucumerina L. fruits, which the pharmacological properties have been studied for decades particularly an anti-tumor activity. The pharmacokinetic profile of this compound is still limited and investigation is needed for further phytopharmaceutical product development. This study aimed to investigate the pharmacokinetic profile of cucurbitacin B after administering the compound at different doses and routes to rats. Methods: Male Wistar rats (n = 6) were treated by cucurbitacin B extracted from Trichosanthes cucumerina L. The cucurbitacin B was administered at 0.1 mg/kg intravenously or by oral gavage at 2-4 mg/kg. Blood samples and internal organs were collected serially within 24 h after administration. Urine and feces were collected from time 0 to 48 h. The level of cucurbitacin B in biological samples was determined by liquid chromatography-tandem mass spectrometry. Results: The absolute oral bioavailability of cucurbitacin B was approximately 10%. The maximum concentration in plasma after normalization by dose ranged from 4.85-7.81 μg/L and the time to reach maximum value was approximately within 30 min after oral dosing. The level of cucurbitacin B in plasma increased proportionally to the given dose. After intravenous administration, cucurbitacin B had a large volume of distribution of about 51.65 L/kg and exhibited a high tissue to plasma concentration ratio, approximately 60 to 280-fold in several organs. Negligible amount of unchanged cucurbitacin B could be detected in urine and feces and accounted less than 1% of administered dose. Conclusion: Cucurbitacin B had low oral bioavailability, but could be distributed extensively into internal organs with a high volume of distribution and tissue to plasma ratio. Only negligible amounts of unchanged cucurbitacin B were excreted via urine and feces suggesting that the compound might be biotransformed before undergoing an excretion. Further studies of the metabolic pathway and tissue uptake mechanism are required to strategize the future development of cucurbitacin B into clinical studies.
ISSN: 14726882
Appears in Collections:Scopus 2019

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