Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract
Eurycoma longifolia is one of the commonly consumed herbal preparations and its major chemical compound, eurycomanone, has been described to have antimalarial, antipyretic, aphrodisiac, and cytotoxic activities. Today, the consumption of E. longifolia is popular through the incorporation of its extr...
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| Format: | Article |
| Language: | English |
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MDPI AG
2018-07-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/10/3/90 |
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| author | Norzahirah Ahmad Dodheri Syed Samiulla Bee Ping Teh Murizal Zainol Nor Azlina Zolkifli Amirrudin Muhammad Emylyn Matom Azlina Zulkapli Noor Rain Abdullah Zakiah Ismail Ami Fazlin Syed Mohamed |
| author_facet | Norzahirah Ahmad Dodheri Syed Samiulla Bee Ping Teh Murizal Zainol Nor Azlina Zolkifli Amirrudin Muhammad Emylyn Matom Azlina Zulkapli Noor Rain Abdullah Zakiah Ismail Ami Fazlin Syed Mohamed |
| author_sort | Norzahirah Ahmad |
| collection | DOAJ |
| description | Eurycoma longifolia is one of the commonly consumed herbal preparations and its major chemical compound, eurycomanone, has been described to have antimalarial, antipyretic, aphrodisiac, and cytotoxic activities. Today, the consumption of E. longifolia is popular through the incorporation of its extract in food items, most frequently in drinks such as tea and coffee. In the current study, the characterisation of the physicochemical and pharmacokinetic (PK) attributes of eurycomanone were conducted via a series of in vitro and in vivo studies in rats and mice. The solubility and chemical stability of eurycomanone under the conditions of the gastrointestinal tract environment were determined. The permeability of eurycomanone was investigated by determining its distribution coefficient in aqueous and organic environments and its permeability using the parallel artificial membrane permeability assay system and Caco-2 cultured cells. Eurycomanone’s stability in plasma and its protein-binding ability were measured by using an equilibrium dialysis method. Its stability in liver microsomes across species (mice, rat, dog, monkey, and human) and rat liver hepatocytes was also investigated. Along with the PK evaluations of eurycomanone in mice and rats, the PK parameters for the Malaysian Standard (MS: 2409:201) standardised water extract of E. longifolia were also evaluated in rats. Both rodent models showed that eurycomanone in both the compound form and extract form had a half-life of 0.30 h. The differences in the bioavailability of eurycomanone in the compound form between the rats (11.8%) and mice (54.9%) suggests that the PK parameters cannot be directly extrapolated to humans. The results also suggest that eurycomanone is not readily absorbed across biological membranes. However, once absorbed, the compound is not easily metabolised (is stable), hence retaining its bioactive properties, which may be responsible for the various reported biological activities. |
| first_indexed | 2024-04-13T09:00:54Z |
| format | Article |
| id | doaj.art-3a789d7b36a24d3bb7febb82fbde8ab0 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T09:00:54Z |
| publishDate | 2018-07-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj.art-3a789d7b36a24d3bb7febb82fbde8ab02022-12-22T02:53:09ZengMDPI AGPharmaceutics1999-49232018-07-011039010.3390/pharmaceutics10030090pharmaceutics10030090Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water ExtractNorzahirah Ahmad0Dodheri Syed Samiulla1Bee Ping Teh2Murizal Zainol3Nor Azlina Zolkifli4Amirrudin Muhammad5Emylyn Matom6Azlina Zulkapli7Noor Rain Abdullah8Zakiah Ismail9Ami Fazlin Syed Mohamed10Herbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaAurigene Discovery Technologies Limited, Electronic City, Hosur Road, Bangalore 560100, Karmataka, IndiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaMedical Resource Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaHerbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, MalaysiaEurycoma longifolia is one of the commonly consumed herbal preparations and its major chemical compound, eurycomanone, has been described to have antimalarial, antipyretic, aphrodisiac, and cytotoxic activities. Today, the consumption of E. longifolia is popular through the incorporation of its extract in food items, most frequently in drinks such as tea and coffee. In the current study, the characterisation of the physicochemical and pharmacokinetic (PK) attributes of eurycomanone were conducted via a series of in vitro and in vivo studies in rats and mice. The solubility and chemical stability of eurycomanone under the conditions of the gastrointestinal tract environment were determined. The permeability of eurycomanone was investigated by determining its distribution coefficient in aqueous and organic environments and its permeability using the parallel artificial membrane permeability assay system and Caco-2 cultured cells. Eurycomanone’s stability in plasma and its protein-binding ability were measured by using an equilibrium dialysis method. Its stability in liver microsomes across species (mice, rat, dog, monkey, and human) and rat liver hepatocytes was also investigated. Along with the PK evaluations of eurycomanone in mice and rats, the PK parameters for the Malaysian Standard (MS: 2409:201) standardised water extract of E. longifolia were also evaluated in rats. Both rodent models showed that eurycomanone in both the compound form and extract form had a half-life of 0.30 h. The differences in the bioavailability of eurycomanone in the compound form between the rats (11.8%) and mice (54.9%) suggests that the PK parameters cannot be directly extrapolated to humans. The results also suggest that eurycomanone is not readily absorbed across biological membranes. However, once absorbed, the compound is not easily metabolised (is stable), hence retaining its bioactive properties, which may be responsible for the various reported biological activities.http://www.mdpi.com/1999-4923/10/3/90eurycomanoneEurycoma longifoliabioavailabilitypharmacokinetic |
| spellingShingle | Norzahirah Ahmad Dodheri Syed Samiulla Bee Ping Teh Murizal Zainol Nor Azlina Zolkifli Amirrudin Muhammad Emylyn Matom Azlina Zulkapli Noor Rain Abdullah Zakiah Ismail Ami Fazlin Syed Mohamed Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract Pharmaceutics eurycomanone Eurycoma longifolia bioavailability pharmacokinetic |
| title | Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract |
| title_full | Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract |
| title_fullStr | Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract |
| title_full_unstemmed | Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract |
| title_short | Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract |
| title_sort | bioavailability of eurycomanone in its pure form and in a standardised eurycoma longifolia water extract |
| topic | eurycomanone Eurycoma longifolia bioavailability pharmacokinetic |
| url | http://www.mdpi.com/1999-4923/10/3/90 |
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