Favourable drug-lead pharmacokinetic features for designing gallic acid-standardized Syzygium polyanthum aqueous extract-based product
Keywords:
Gallic acid, Syzygium polyanthum, aqueous extract, pharmacokinetic
Abstract
In this study, Syzygium polyanthum was standardized against gallic acid (GA), and a complete pharmacokinetic test was conducted using in vitro and in vivo models against this phytochemical. High-performance liquid chromatography showed that GA is a major phytochemical in aqueous extract of S. polyanthum. It exhibited a low equilibrium solubility and physiochemical stability at pH 2.0 and 7.4, but it deteriorated rapidly at pH 9.2. It showed low permeability toward Caco-2 intestinal absorption with eight times slower absorption in oral than intravenous administration. GA was unstable in mouse, rat, and dog plasma sera with in vitro half-lives (t1/2) of 60, 53, and 56 min, respectively, but was relatively stable in human plasma serum (t1/2 = 185 min). Approximately 5.6% of GA (10 µM) bound to the human plasma proteins. GA was stable in mouse, rat, dog, and human microsomal extracts with in vitro microsomal intrinsic clearance values of 72, 68, 6, and 22 µL/min/mg, respectively. GA selectively inhibited or stimulated the activity of the tested CYP450 enzymes. The in vivo oral bioavailability of GA was 54%, with short elimination half-life and a high volume of distribution. Thus, the mention pharmacokinetic features of GA must be considered during the development of GA-based products to yield the optimum dosage and pharmacological effect.
References
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Grosvenor, P. W., Gothard, P. K., McWilliam, N. C., Supriono, A., & Gray, D. O. (1995). Medicinal plants from riau province, sumatra, Indonesia. Part 1: uses. Journal of ethnopharmacology, 45(2), 75-95.
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Hefti, F. F. (2008). Requirements for a lead compound to become a clinical candidate. BMC neuroscience, 9(3), 1-7.
Hidayati, M. D., Ersam, T., Shimizu, K., & Fatmawati, S. (2017). Antioxidant activity of Syzygium polyanthum extracts. Indonesian Journal of Chemistry, 17(1), 49-53.
Honda, S., Ishida, R., Hidaka, K., & Masuda, T. (2019). Stability of polyphenols under alkaline conditions and the formation of a xanthine oxidase inhibitor from gallic acid in a solution at pH 7.4. Food Science and Technology Research, 25(1), 123-129.
Ismail, A., & Ahmad, W. A. N. W. (2017). Autonomic receptors and nitric-oxide involvements in mediating vasorelaxation effect induced by Syzygium polyanthum leaves extract. Pharmacognosy research, 9(Suppl 1), S9.
Ismail, A., & Ahmad, W. A. N. W. (2019). Syzygium polyanthum (Wight) Walp: a potential phytomedicine. Pharmacognosy Journal, 11(2).
Ismail, A., Mohamed, M., Sulaiman, S. A., & Wan Ahmad, W. A. N. (2013). Autonomic nervous system mediates the hypotensive effects of aqueous and residual methanolic extracts of Syzygium polyanthum (Wight) Walp. var. polyanthum leaves in anaesthetized rats. Evidence-Based Complementary and Alternative Medicine, 2013.
Ismail, A., Rahim, E. N. A. A., Omar, M. N., & Ahmad, W. A. N. W. (2020). Antihypertensive Assay-Guided Fractionation of Syzygium polyanthum Leaves and Phenolics Profile Analysis Using LCQTOF/MS. Pharmacognosy Journal, 12(6s).
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Jing, X., Hou, Y., Hallett, W., Sahajwalla, C. G., & Ji, P. (2019). Key physicochemical characteristics influencing adme properties of therapeutic proteins. Therapeutic Enzymes: Function and Clinical Implications, 115-129.
Karimi-Khouzani, O., Heidarian, E., & Amini, S. A. (2017). Anti-inflammatory and ameliorative effects of gallic acid on fluoxetine-induced oxidative stress and liver damage in rats. Pharmacological reports, 69(4), 830-835.
Kato, E., Nakagomi, R., Gunawan-Puteri, M. D., & Kawabata, J. (2013). Identification of hydroxychavicol and its dimers, the lipase inhibitors contained in the Indonesian spice, Eugenia polyantha. Food chemistry, 136(3-4), 1239-1242.
Khorsandi, K., Kianmehr, Z., & Hosseinzadeh, R. (2020). Anti-cancer effect of gallic acid in presence of low level laser irradiation: ROS production and induction of apoptosis and ferroptosis. Cancer cell international, 20(1), 1-14.
Kok-Yong, S., Lawrence, L. (2015). Drug distribution and drug elimination. Basic pharmacokinetic concepts and some clinical applications, 99-116.
Konishi, Y., Kobayashi, S., & Shimizu, M. (2003). Transepithelial transport of p-coumaric acid and gallic acid in Caco-2 cell monolayers. Bioscience, biotechnology, and biochemistry, 67(11), 2317-2324.
Konsoula, R., & Jung, M. (2008). In vitro plasma stability, permeability and solubility of mercaptoacetamide histone deacetylase inhibitors. International journal of pharmaceutics, 361(1-2), 19-25.
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Lelono, R. A., Tachibana, S., & Itoh, K. (2009). In vitro antioxidative activities and polyphenol content of Eugenia polyantha Wight grown in Indonesia. Pakistan journal of biological sciences: PJBS, 12(24), 1564-1570.
Malik, A. (2013). Antidiarrheal Acitivity of Ethanolik Extract of Bay Leaves (Syzygium polianthum (Weight.) Walp.). International Research Journal of Pharmacy (IRJP), 4(4).
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Published
2022-12-20
How to Cite
Hassan Fahmi Ismail, Fadhlina, A., Siti Nurazwa Zainol, Archan Kumar Mamillapalli, Vijayabalaji Venkatesan, Rajesh Eswarappa, Renuka Pillai, & Fadzilah Adibah Abdul Majid. (2022). Favourable drug-lead pharmacokinetic features for designing gallic acid-standardized Syzygium polyanthum aqueous extract-based product. Indonesian Journal of Pharmacy, 33(4), 666–679. https://doi.org/10.22146/ijp.3639
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Section
Research Article
