Oral bioavailability of curcumin in rat and the herbal analysis from Curcuma longa by LC–MS/MS

Yang, Kuo Yi; Lin, Lei Chwen; Tseng, Ting Yu; Wang, Shau Chun; Tsai, Tung Hu

doi:10.1016/j.jchromb.2007.03.010

Cited by 524 publications

(344 citation statements)

References 23 publications

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“…However, CUR has very low bioavailability owing to its poor water solubility and structural stability, which is contradictory to the diversity of its pharmacological activities [4][5][6]. Based on this, a hypothesis was raised that the degradation or biotransformation products of CUR may make important contributions to its diverse bioactivities [5,7,8].…”

Section: Introductionmentioning

confidence: 99%

Biotransformation of food spice curcumin by gut bacterium Bacillus megaterium DCMB-002 and its pharmacological implications

Sun

Shen

et al. 2017

Food & Nutrition Research

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The food additive curcumin shows many benefits for human health but has low solubility and stability, which leads to its low bioavailability. After oral administration, curcumin undergoes biotransformation by gut microbiota in digestive tracts, and thus it is interesting to characterize the biotransformation products of curcumin and assess their bioactivities to help us understand the pharmacology. Herein a bacterial strain of Bacillus megaterium DCMB-002 isolated from mice feces, showed the capability of transforming curcumin to its various derivatives. The tracing high performance liquid chromatogram coupled with quadrupole time-of-flight tandem mass spectra (HPLC-Q-TOF MS n ) led to the identification of seven hydrogenation transformation metabolites through reduction, hydroxylation, demethylation and demethoxylation etc, six of which were reported for the first time. The metabolites exhibited moderate antioxidant activity. The findings provided insights into the microbial biotransformation of curcumin and roles of gut microbiota in its pharmacological effects. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Biotransformation of food spice curcumin by gut bacterium Bacillus megaterium DCMB-002 and its pharmacological implications

Sun

Shen

et al. 2017

Food & Nutrition Research

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“…6) Curcumin was found to be poorly soluble in water, the maximum solubility of which in aqueous buffer (pH 5.0) was reported to be as low as 11 ng/ml. 7) The limited solubility of curcumin, as well as extensive systemic metabolism, could be responsible for the low bioavailability of curcumin after oral delivery.…”

mentioning

confidence: 99%

Innovative Preparation of Curcumin for Improved Oral Bioavailability

Sasaki¹,

Sunagawa

Takahashi³

et al. 2011

Biological & Pharmaceutical Bulletin

392

305

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Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] is the active ingredient of turmeric, which has a long history of being consumed as a dietary spice.1) In addition, turmeric is widely used in traditional Indian medicine to treat biliary disorders, anorexia, cough, diabetic complications, hepatic disorders, rheumatism, and sinusitis.2) Extensive investigation over the past five decades has indicated that curcumin reduces blood cholesterol, prevents low-density lipoprotein oxidation, inhibits platelet aggregation, suppresses thrombosis and myocardial infarction, suppresses symptoms associated with type 2 diabetes, rheumatoid arthritis, multiple sclerosis, and Alzheimer's disease, inhibits human immunodeficiency virus (HIV) replication, enhances wound healing, protects against liver injury, increases bile secretion, protects from cataract formation, and protects against pulmonary toxicity and fibrosis.3-5) Evidence indicates that the divergent effects of curcumin are dependent on its pleiotropic molecular effects.In spite of these attractive properties of curcumin, information on the therapeutic efficiency of curcumin has been limited, partly due to its poor oral bioavailability. 6) Curcumin was found to be poorly soluble in water, the maximum solubility of which in aqueous buffer (pH 5.0) was reported to be as low as 11 ng/ml.7) The limited solubility of curcumin, as well as extensive systemic metabolism, could be responsible for the low bioavailability of curcumin after oral delivery. [8][9][10] In addition, curcumin in solution may be sensitive to UV light, and so marked photochemical degradation could occur under UV exposure, 11) leading to difficulty in its handling for clinical use.A number of efforts have been made to design a soluble formulation of curcumin, but no suitable delivery options have been found so far. We have developed an effective preparation of curcumin, a nano-particle colloidal dispersion, with improved oral bioavailability, and named it THER-ACURMIN. It has the following unique properties: 1) it is an effective preparation for new health care products (beverages, food, and supplements) which may be taken at a much lower dosage; 2) it is soluble in water, which is a must for an effective beverage product; 3) the preparation is highly stable in light (UV), and, therefore, can be put into transparent PET bottles; 4) it is heat-stable, including high temperature sterilization conditions; 5) the preparation has no unpleasant odor or taste.The main purpose of this study was to provide evidence to support the improved bioavailability and alcohol-toxicity-reducing effect of THERACURMIN through oral delivery. We evaluated the plasma pharmacokinetics of this new curcumin preparation and compared the results with curcumin powder after oral administration in rats and healthy human subjects. We also investigated the effect of THERACURMIN on the toxicity of alcohol following drinking. MATERIALS AND METHODS Preparation of Curcumin Powder and THERACUR-MINCurcumin powder was extracted...

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“…and p.o. dose administration to each group illustrated in Fig.1 [5] has reported oral bioavailability of curcumin was about 1%, 15 times higher bioavailability than curcumin might indicated better medical potential of DMC. …”

Section: Pharmacokinetic Studymentioning

confidence: 96%

Absorption and Elimination of Dimethoxycurcumin, An Active Analogue of Curcumin

Zhang¹,

Yang²,

Wang³

et al. 2017

dtbh

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Abstract. Dimethoxycurcumin (DMC) is an active analogue of curcumin with superior efficacy in various disease models. However, pharmacokinetic research on DMC is limited.The present study was designed to investigate oral absorption and excretion of DMC, as well as making a thorough examination on in vivo metabolism. DMC in rat plasma, bile, urine and feces was quantitated by High performance liquid chromatography(HPLC), and liquid chromatography-mass spectra(LC-MS) detection was performed for metabolites identification. The results showed that the oral bioavailability of DMC was 15 times higher than curcumin. DMC was metabolized in vivo via a similar pathway to curcumin. However, accumulated excretion of DMC was 13.21%±1.83%in bile, and the metabolic degree was less extensive than curcumin. Excretion of DMC was less than 1% in urine, and about 65% in feces. All the findings indicated similar in vivo disposition characteristics of curcuminoid.

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Oral bioavailability of curcumin in rat and the herbal analysis from Curcuma longa by LC–MS/MS

Cited by 524 publications

References 23 publications

Biotransformation of food spice curcumin by gut bacterium Bacillus megaterium DCMB-002 and its pharmacological implications

Biotransformation of food spice curcumin by gut bacterium Bacillus megaterium DCMB-002 and its pharmacological implications

Innovative Preparation of Curcumin for Improved Oral Bioavailability

Absorption and Elimination of Dimethoxycurcumin, An Active Analogue of Curcumin

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