Rosmarinic Acid–Human Pharmacokinetics and Health Benefits

Hitl, Maja; Kladar, Nebojša; Gavarić, Neda; Božin, Biljana

doi:10.1055/a-1301-8648

Cited by 92 publications

(71 citation statements)

References 69 publications

(115 reference statements)

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“…In addition, previous papers have reported a high metabolization of RA in the upper gastrointestinal tract. In this regard, in vitro digestion studies have described that RA is hydrolysed by different esterases and metabolised by the gut microbiota before its absorption, which could affect the functionality of this polyphenol as reviewed in [17]. The oral administration of appropriately formulated RA would improve its bioavailability and allow an adequate RA concentration to reach the inflamed colon.…”

Section: Introductionmentioning

confidence: 99%

Anti-Inflammatory Effects of Rosmarinic Acid-Loaded Nanovesicles in Acute Colitis through Modulation of NLRP3 Inflammasome

et al. 2021

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Ulcerative colitis (UC), one of the two main types of inflammatory bowel disease, has no effective treatment. Rosmarinic acid (RA) is a polyphenol that, when administered orally, is metabolised in the small intestine, compromising its beneficial effects. We used chitosan/nutriose-coated niosomes loaded with RA to protect RA from gastric degradation and target the colon and evaluated their effect on acute colitis induced by 4% dextran sodium sulphate (DSS) for seven days in mice. RA-loaded nanovesicles (5, 10 and 20 mg/kg) or free RA (20 mg/kg) were orally administered from three days prior to colitis induction and during days 1, 3, 5 and 7 of DSS administration. RA-loaded nanovesicles improved body weight loss and disease activity index as well as increased mucus production and decreased myeloperoxidase activity and TNF-α production. Moreover, RA-loaded nanovesicles downregulated protein expression of inflammasome components such as NLR family pyrin domain-containing 3 (NLRP3), adaptor protein (ASC) and caspase-1, and the consequent reduction of IL-1β levels. Furthermore, nuclear factor erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) protein expression increased after the RA-loaded nanovesicles treatment However, these mechanistic changes were not detected with the RA-free treatment. Our findings suggest that the use of chitosan/nutriose-coated niosomes to increase RA local bioavailability could be a promising nutraceutical strategy for oral colon-targeted UC therapy.

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Section: Introductionmentioning

confidence: 99%

Anti-Inflammatory Effects of Rosmarinic Acid-Loaded Nanovesicles in Acute Colitis through Modulation of NLRP3 Inflammasome

et al. 2021

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“…The fingerprints of the analyzed extracts were established using LC-PDA-MS method. The analysis revealed constituents comprising polyphenols as caffeic acid derivatives (14,24), flavonoids such as luteolin (7,8,16,20,22,23) and apigenin (10, 25) derivatives, respectively, and related compounds such as diterpenes (29,31,32). The LC-MS analysis is summarized in Table 2, Figure 2 and Figure 3.…”

Section: Qualitative and Quantitative Analysis Of Re And Lbementioning

confidence: 98%

“…An important component of rosemary extracts (RE) and lemon balm extract (LBE) that independently showed a wide range of pharmacological activities and therapeutic applications is rosmarinic acid (RA), an ester of caffeic acid and 3, 4-dihydroxyphenyl lactic acid (Figure 1). The characteristics of the RA have been discussed extensively in the reviews [6][7][8][9]. Based on the results of in vitro studies and clinical trials, it can be assumed that it brings many benefits in the treatment of disorders related to the nervous, cardiovascular, gastrointestinal, hepatic, endocrine, respiratory and reproductive systems, cancer diseases, osteoarthritis, allergic rhinitis, periodontal disease, acute pancreatitis, and metabolic syndrome.…”

Section: Introductionmentioning

confidence: 99%

“…Most (85-90%) patients experience qualitative or quantitative abnormalities of type I collagen, due to a mutation in one of two genes COL1A1/COL1A2 encoding this protein [24][25][26][27]. Currently, the classification The characteristics of the RA have been discussed extensively in the reviews [6][7][8][9]. Based on the results of in vitro studies and clinical trials, it can be assumed that it brings many benefits in the treatment of disorders related to the nervous, cardiovascular, gastrointestinal, hepatic, endocrine, respiratory and reproductive systems, cancer diseases, osteoarthritis, allergic rhinitis, periodontal disease, acute pancreatitis, and metabolic syndrome.…”

Section: Introductionmentioning

confidence: 99%

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The Stimulating Effect of Rosmarinic Acid and Extracts from Rosemary and Lemon Balm on Collagen Type I Biosynthesis in Osteogenesis Imperfecta Type I Skin Fibroblasts

et al. 2021

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Rosemary extract (RE) and lemon balm extract (LBE) attract particular attention of pharmacists due to their high therapeutic potential. Osteogenesis imperfecta (OI) type I is a heritable disease caused by mutations in type I collagen and characterized by its reduced amount. The aim of the study was to evaluate the effect of the extracts and rosmarinic acid (RA) on collagen type I level in OI skin fibroblasts. Phytochemical analysis of RE and LBE was carried out by liquid chromatography–photodiode array detection–mass spectrometry. The expression of collagen type I at transcript and protein levels was analyzed by qPCR, ELISA, SDS-urea PAGE, and Western blot. In OI patient’s fibroblasts the exposure to the extracts (0.1–100 µg/mL) and RA (0.1–100 µM) significantly increased collagen type I and the best results were obtained with 0.1–10 µM RA and 0.1–10 µg/mL of the extracts. LBE showed a greater stimulating effect than RE, likely due to a higher RA content. Moreover, collagen type III expression and matrix metalloproteinase (MMP-1, -2, -9) activity remained unchanged or decreased. The obtained data support the clinical potential of RA-rich extracts and RA itself in modulating the quantitative defect of type I collagen in type I OI.

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“…Rosmarinic acid is considered to be metabolized by gut microbiota, thus providing phenolic elements that may be absorbed more easily. In the human organism, molecules of rosmarinic acid alter their structure, undergo conjugation reactions, and are removed with excrements (Hitl et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

Hematological parameters and protein metabolism in the blood of pregnant rats under the effect of vanadium citrate

Klymets

Iskra

Svarchevska

2021

Regul. Mech. Biosyst.

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Dose-dependent changes in protein metabolism in the blood and hematological parameters of pregnant rats under the effect of vanadium citrate are presented in the article. The animals were divided into five groups: group I – non-pregnant females, II – pregnant females consuming pure water without additives, III, IV, V – females which during the mating and pregnancy period received the solution of vanadium citrate at concentrations of 0.03, 0.125 and 0.50 μg V/mL water. The research findings show that in pregnant animals of group II, the level of urea and alkaline phosphatase activity increased, meanwhile aspartate aminotransferase activity decreased, as compared to the non-pregnant females of group І. The levels of total protein and albumin decreased; however, the content of β-globulins increased in the pregnant animals of group II, as compared with that in group I. Also, in the rats of group II, there was a decrease in hemolysis time, total content of erythrocytes and hemoglobin, the content of old and mature erythrocytes, while the content of young erythrocytes increased, as compared to group I. The platelet content and thrombocrit in rats of group II increased in comparison with group I. The content of leukocytes and lymphocytes in pregnant animals of group II decreased, while the content of granulocytes increased, in contrast to non-pregnant rats. Under the effect of vanadium citrate at concentrations of 0.03–0.50 μg V/mL, there was a significant increase in the maximum number of prohemolized erythrocytes, the time of maximum hemolysis was delayed by 0.4–0.6 min, as compared with the pregnant rats of group II. This did not affect the time of total hemolysis in rats of groups III and V, as compared with the pregnant animals in group II. Under the effect of vanadium citrate, an increase in the content of young erythrocytes was observed, as compared with group II. The hemoglobin content decreased at the concentration of 0.125 μg V/mL, while at the concentration of 0.50 μg V/mL it increased, as compared to the pregnant animals of group II. Also, under the effect of vanadium citrate there was a decrease in the mean hemoglobin concentration in the erythrocyte. In pregnant animals fed with vanadium citrate solutions, the platelet content and thrombocrit, the relative width of platelet distribution by volume decreased, as compared with the pregnant rats of group II. The content of leukocytes, lymphocytes and granulocytes under the effect of vanadium citrate increased, as compared with the pregnant animals in group II. Under the effect of vanadium citrate at the concentration of 0.03 μg V/mL, the level of albumin, creatinine and aspartate aminotransferase activity increased in blood plasma in comparison with group II. Meanwhile, at the concentration of 0.125 μg V/mL, the relative content of γ-globulins and aspartate aminotransferase activity increased, alkaline phosphatase activity and urea level decreased in comparison with group II. However at the concentration of 0.50 μg V/mL, the relative α- and γ-globulins content and aspartate aminotransferase activity increased, at the same time, the relative β-globulins content and urea level decreased in comparison with group II. Therefore, vanadium citrate normalizes the indicators of protein metabolism during pregnancy, thus it can be considered as a potential dietary drug for the pregnant.

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Rosmarinic Acid–Human Pharmacokinetics and Health Benefits

Cited by 92 publications

References 69 publications

Anti-Inflammatory Effects of Rosmarinic Acid-Loaded Nanovesicles in Acute Colitis through Modulation of NLRP3 Inflammasome

Anti-Inflammatory Effects of Rosmarinic Acid-Loaded Nanovesicles in Acute Colitis through Modulation of NLRP3 Inflammasome

The Stimulating Effect of Rosmarinic Acid and Extracts from Rosemary and Lemon Balm on Collagen Type I Biosynthesis in Osteogenesis Imperfecta Type I Skin Fibroblasts

Hematological parameters and protein metabolism in the blood of pregnant rats under the effect of vanadium citrate

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