Pharmacokinetic and oral bioavailability of andrographolide from Andrographis paniculata fixed combination Kan Jang in rats and human

Panossian, Alexander; Hovhannisyan, Areg; Mamikonyan, Grigor; Abrahamian, Heidemarie; Hambardzumyan, E.; Gabrielian, E.; Goukasova, G.I.; Wikman, G.; Wagner, Hildebert

doi:10.1016/s0944-7113(00)80054-9

Cited by 187 publications

(148 citation statements)

References 18 publications

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“…Antioxidative activities of A. paniculata and andrographolide and their other constituents have been described (Lin et al 2009;Chao & Lin 2010), and acetylcholinesterase inhibitory activities of AP and andrographolide in rat brain homogenates have recently been observed in our laboratories (results not shown). However, concentrations of andrographolide necessary for observing its effects in bioassays conducted in vitro were several folds higher than that of its maximal blood levels quantified after its oral intake in rats (Panossian et al 2000). Therefore, the presented study was conducted to verify in vivo relevance of these in vitro observations made in our laboratories and elsewhere.…”

Section: Discussionmentioning

confidence: 90%

“…Andrographolide and diverse other extractable secondary metabolites of A. paniculata possess bactericidal, fungicidal and antiviral activities (Sareer et al 2012), and oral bioavailability of andrographolide (as judged by its observed blood levels after oral intake) is low (Panossian et al 2000;Ye et al 2011). Andrographolide modulates physiological functions of diverse drug metabolising enzymes in liver and other peripheral organs as well (Pekthong et al 2008), and binds covalently with cellular metabolites and enzymes (Xia et al 2004).…”

Section: Discussionmentioning

confidence: 99%

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Beneficial effects of anAndrographis paniculataextract and andrographolide on cognitive functions in streptozotocin-induced diabetic rats

Thakur

Rai

Chatterjee³

et al. 2016

Pharmaceutical Biology

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Context Andrographolide containing Andrographis paniculata (Burm. F.) Wall. Ex Nees (Acanthaceae) extracts is often used for treatments of diabetes and other inflammatory disorders commonly accompanying cognitive and other psychiatric disorders.Objective To compare the efficacies of a standardised A. paniculata extract (AP) and pure andrographolide on cognitive functions, oxidative stress and cholinergic function in diabetic rats. Materials and methods Streptozotocin-induced diabetic Charles Foster albino rats treated orally with a hydro-methanolic A. paniculata leaf extract (50, 100 and 200 mg/kg/day), or with pure andrographolide (15, 30 and 60 mg/kg/day) for 10 consecutive days, were subjected to Morris water maze test. After the test, acetylcholinesterase, superoxide dismutase (SOD), and catalase (CAT) activities and lipid peroxidation (LPO) in brain tissues were assessed. Results Acetylcholinesterase activity in pre-frontal cortex and hippocampus of diabetic rats was 2.1 and 2.6 times higher compared to nondiabetic rats. LPO was 1.6 times higher and decreased SOD (56.3%) and CAT (44.9%) activities in pre-frontal cortex of diabetic rats compared to nondiabetic rats. AP or andrographolide treatments dose dependently attenuated cognitive deficits, reduced acetylcholinesterase activity, oxidative stress, improved diabetic hyperglycemia and insulin deficiency. All observed effects of AP were quantitatively almost equal to those expected from its analytically quantified andrographolide content. Discussion and conclusion Reported observations are the very first ones suggesting beneficial effects of andrographolide against diabetes associated cognitive deficits, increased acetylcholinesterase activity and deteriorated antioxidative status. Efforts to exploit A. paniculata extracts enriched in andrographolide as preventive measures against such disorders can be warranted. ARTICLE HISTORY

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Section: Discussionmentioning

confidence: 90%

Section: Discussionmentioning

confidence: 99%

Beneficial effects of anAndrographis paniculataextract and andrographolide on cognitive functions in streptozotocin-induced diabetic rats

Thakur

Rai

Chatterjee³

et al. 2016

Pharmaceutical Biology

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“…To address this issue, we have used a natural compound, AG (Andrographolide) that has anti-inflammatory and anti-tumor activity in this study. 5,6 Unlike other natural compounds, this bioactive constituent is readily absorbed in vivo 3,4 and have protective effects on liver and kidney. 18,19 We assessed the efficacy of AG on different PCa cell lines.…”

Section: Discussionmentioning

confidence: 99%

“…Independent pharmacokinetic studies showed that 90% of orally administered AG is absorbed in the blood and 40% in tissues and cells. 3,4 AG functions mainly by manipulating cell cycle and cytokine signaling. Studies have shown that it inhibits NF-kB and reduces pro-inflammatory cytokines IL-2, IL-6, TNF-a and IFN-g in PCa.…”

Section: Introductionmentioning

confidence: 99%

Andrographolide inhibits prostate cancer by targeting cell cycle regulators, CXCR3 and CXCR7 chemokine receptors

et al. 2016

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Despite state of the art cancer diagnostics and therapies offered in clinic, prostate cancer (PCa) remains the second leading cause of cancer-related deaths. Hence, more robust therapeutic/preventive regimes are required to combat this lethal disease. In the current study, we have tested the efficacy of Andrographolide (AG), a bioactive diterpenoid isolated from Andrographis paniculata, against PCa. This natural agent selectively affects PCa cell viability in a dose and time-dependent manner, without affecting primary prostate epithelial cells. Furthermore, AG showed differential effect on cell cycle phases in LNCaP, C4-2b and PC3 cells compared to retinoblastoma protein (RB ¡/¡ ) and CDKN2A lacking DU-145 cells. G2/M transition was blocked in LNCaP, C4-2b and PC3 after AG treatment whereas DU-145 cells failed to transit G1/S phase. This difference was primarily due to differential activation of cell cycle regulators in these cell lines. Levels of cyclin A2 after AG treatment increased in all PCa cells line. Cyclin B1 levels increased in LNCaP and PC3, decreased in C4-2b and showed no difference in DU-145 cells after AG treatment. AG decreased cyclin E2 levels only in PC3 and DU-145 cells. It also altered Rb, H3, Wee1 and CDC2 phosphorylation in PCa cells. Intriguingly, AG reduced cell viability and the ability of PCa cells to migrate via modulating CXCL11 and CXCR3 and CXCR7 expression. The significant impact of AG on cellular and molecular processes involved in PCa progression suggests its potential use as a therapeutic and/or preventive agent for PCa.

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“…Many experiments have been done, but much still remains to be clarified about andrographolide. Some results about the pharmacokinetics of this product have been reported after oral administration of andrographolide (Zhu and Kang, 1981;Panossian et al, 2000). However, there have been no reports on its metabolism, either in humans or animals, to our knowledge.…”

mentioning

confidence: 98%

Identification of a Rare Sulfonic Acid Metabolite of Andrographolide in Rats

Li²,

Gao³

et al. 2003

Drug Metab Dispos

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This article is available online at http://dmd.aspetjournals.org ABSTRACT:Andrographolide is widely used in clinic as an anti-inflammatory and antibiotic drug. In this paper, the metabolites of andrographolide in rats after single oral doses of 120 mg/kg were investigated. The structures of the metabolites were elucidated by high-resolution mass spectra, NMR spectroscopy including 1 H NMR, 13 C NMR, and two-dimensional NMR, through comparison to a synthetic standard. The main metabolite of andrographolide in rats was 14-deoxy-12(R)-sulfo andrographolide. In the proposed mechanism, the ␤-carbon of ␣, ␤-unsaturated carbonyl was attacked by sulfonic acid, to form the sulfonate compound. This was a rare metabolic reaction. It may be the main metabolic pathway of andrographolide in rats. The polarity of the sulfonate metabolite increased greatly and could be easily eliminated from body.

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Pharmacokinetic and oral bioavailability of andrographolide from Andrographis paniculata fixed combination Kan Jang in rats and human

Cited by 187 publications

References 18 publications

Beneficial effects of anAndrographis paniculataextract and andrographolide on cognitive functions in streptozotocin-induced diabetic rats

Beneficial effects of anAndrographis paniculataextract and andrographolide on cognitive functions in streptozotocin-induced diabetic rats

Andrographolide inhibits prostate cancer by targeting cell cycle regulators, CXCR3 and CXCR7 chemokine receptors

Identification of a Rare Sulfonic Acid Metabolite of Andrographolide in Rats

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