Antiplatelet activity of hesperetin, a bioflavonoid, is mainly mediated by inhibition of PLC-γ2 phosphorylation and cyclooxygenase-1 activity

Jin, Yong-Ri; Han, Xianghua; Zhang, Yonghe; Lee, Jung‐Jin; Lim, Yong; Chung, Jin‐Ho; Yun, Young Won

doi:10.1016/j.atherosclerosis.2006.10.011

Cited by 79 publications

(52 citation statements)

References 37 publications

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“…It has been demonstrated that collagen-and arachidonic-acid-induced platelet aggregation is potently inhibited by Hst via the inhibition of phospholipase C-γ2 (PLCγ2) phosphorylation and cyclooxygenase-1. 6 Serotonin is also effectively involved in platelet aggregation. Hst can also have antiplatelet effects via the inhibition of arachidonic acid-induced serotonin secretion.…”

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confidence: 99%

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Menezes

Frank

Lima

et al. 2017

IJN

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Chronic venous insufficiency is characterized by chronic reflux disorder of blood from the peripheral to the central vein, with subsequent venous hypertension and resulting changes in the skin. Traditionally, nonsurgical treatments relied on the use of compression therapy, and more recently a variety of flavonoids have been shown to have positive effects. There have also been developments of more effective drug delivery systems using various textiles and nanotechnology to provide new therapeutic options. Our objective was to use nanotechnology to develop a new formulation containing hesperetin (Hst), a substance not previously used in the treatment of chronic venous insufficiency, impregnated into textile fibers as a possible alternative treatment of venous diseases. We prepared the nanocapsules using the interfacial deposition of preformed polymer method with an Hst concentration of 0.5 mg/mL and then characterized the size and distribution of particles. To quantify the Hst in the samples, we developed an analytical method using high-performance liquid chromatography. Studies of encapsulation efficiency (98.81%±0.28%), microscopy, drug release (free-Hst: 104.96%±12.83%; lipid-core nanocapsule-Hst: 69.90%±1.33%), penetration/permeation, drug content (0.46±0.01 mg/mL) and the effect of washing the textile after drug impregnation were performed as part of the study. The results showed that nanoparticles of a suitable size and distribution with controlled release of the drug and penetration/permeation into the skin layers were achieved. Furthermore, it was established that polyamide was able to hold more of the drug, with a 2.54 times higher content than the cotton fiber; after one wash and after five washes, this relation was 2.80 times higher. In conclusion, this is a promising therapeutic alternative to be further studied in clinical trials.

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confidence: 99%

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Menezes

Frank

Lima

et al. 2017

IJN

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“…Hesperetin, an aglycone of hesperidin, had antiplatelet activity as described in the previous report. 5) Hesperetin showed no effect on erythrocyte aggregation and fibrinolysis as cited in Table 2. Since prunin was isolated for the first time from C. hassaku, we intended to confirm whether prunin is a genuine glycoside, and to determine the content of prunin in CH-ext by HPLC analysis.…”

Section: Resultsmentioning

confidence: 99%

“…4) Recently, it has been reported that hesperetin, an aglycone of hesperidin which is a constituent of Citrus fruits, inhibited rabbit platelet aggregation induced by collagen and arachidonic acid, and that the cellular mechanism for the antiplatelet activity of hesperetin was mainly mediated by the inhibition of phospholipase (PL)C-g2 phosphorylation and cyclooxygenase-1 activity. 5) A group of antioxidants of the flavonoid family has been reported to inhibit platelet aggregation in vitro and ex vivo, and human studies have also suggested that a diet high in flavonoids may inhibit platelet aggregation in vivo. 5) These reports prompted us to examine the antiplatelet activity of CH-ext, since there is no report on antiplatelet effects of C. hassaku.…”

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confidence: 99%

“…5) A group of antioxidants of the flavonoid family has been reported to inhibit platelet aggregation in vitro and ex vivo, and human studies have also suggested that a diet high in flavonoids may inhibit platelet aggregation in vivo. 5) These reports prompted us to examine the antiplatelet activity of CH-ext, since there is no report on antiplatelet effects of C. hassaku. First, we examined in vitro antiplatelet activity of CH-ext by an assay of the inhibitory effect on collagen-induced rabbit platelet aggregation.…”

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confidence: 99%

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Effects of Unripe Citrus hassaku Fruits Extract and Its Flavanone Glycosides on Blood Fluidity

Itoh

Masuda

Naruto

et al. 2010

Biological & Pharmaceutical Bulletin

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Citrus fruits are widely consumed in Asian countries, especially in Japan. Some Citrus species, such as Citrus unshiu MARKOVICH and Citrus hassaku HORT ex T. TANAKA originate in Japan. Both species have been shown to possess various biological activities such as anti-allergy, tyrosinase inhibitory and anti-melanogenesis activities through recent extensive research. 1,2) Our previous reports 1,2) described that the 50% ethanolic extract (CH-ext) obtained from C. hassaku unripe fruits collected in July possessed significant anti-melanogenesis activity with potent tyrosinase inhibitory activity. In addition, CH-ext inhibited the allergic symptoms in vivo and degranulation of mast cells obtained from rat peritoneal showing its potent anti-allergic activity. Thus, CH-ext is expected to be a functional material possessing both skinwhitening and anti-allergy effects and a useful ingredient for cosmetics and/or supplements.The brightness of skin may be influenced by infraorbital dark circles around the eyes and skin darkness. From an antiaging point of view, these factors are recognized as unfavorable for many women. Thus, many cosmetic products to reduce these symptoms have been launched by Japanese cosmetic-related companies. One of the ways to improve infraorbital dark circles around the eyes and skin darkness is the enhancement of blood fluidity, since the murkiness is said to be due to the blood stasis ("Oketsu" in Japanese, a term in oriental medicine) in specific areas of the body. The treatment of Oketsu can be achieved by invigorating blood circulation and eliminating blood stasis. The enhancement of blood fluidity may lead to the improvement of skin problems resulting from unsmooth circulation or stagnation of blood. From the study of blood fluidity, it is known that blood platelet hyperactivity results in platelet adhesion to the vessel wall. Thus platelet hyperactivity is one of the most essential factors responsible for thrombosis, and the incidence of Oketsu, and for cardiovascular, cerebrovascular, and peripheral vascular diseases. 3) Many investigations for antiplatelet agents from natural resources have therefore been carried out to prevent platelet dysfunction. 4) Recently, it has been reported that hesperetin, an aglycone of hesperidin which is a constituent of Citrus fruits, inhibited rabbit platelet aggregation induced by collagen and arachidonic acid, and that the cellular mechanism for the antiplatelet activity of hesperetin was mainly mediated by the inhibition of phospholipase (PL)C-g2 phosphorylation and cyclooxygenase-1 activity. 5) A group of antioxidants of the flavonoid family has been reported to inhibit platelet aggregation in vitro and ex vivo, and human studies have also suggested that a diet high in flavonoids may inhibit platelet aggregation in vivo. 5) These reports prompted us to examine the antiplatelet activity of CH-ext, since there is no report on antiplatelet effects of C. hassaku. First, we examined in vitro antiplatelet activity of CH-ext by an assay of the inhibitory effect ...

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“…Hesperetin (5, 7, 3 -trihydroxy-4 -methoxy-flavanone, Figure 1), a bioflavonoid compound with glycosidic hesperidin as its natural existing form which is abundant in citrus fruits including lemon, lime (Citrus aurantifolia), and mandarin (Citrusreticulata) [1], possesses a wide spectrum of biological activities such as antiplatelet, anti-inflammatory, antioxidant and neuroprotective activities [2][3][4][5]. Since reported on the clinical application in attenuating capillary permeability in 1945 [6], there has been a growing interest in the pharmacological studies of hesperetin [7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Determination of Hesperetin in Pericarpium Citri Reticulatae and Human Serum Using Flow Injection Chemiluminescence

Wang

Tan

et al. 2012

ISRN Analytical Chemistry

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A sensitive chemiluminescence (CL) method for the determination of hesperetin at nanogram levels was first presented. It was based on the inhibitory effect of hesperetin on luminol-dissolved oxygen CL reaction in a flow injection system. The decrements of CL intensity were logarithm over the concentrations of hesperetin in a range of 0.5 to 1000 ng mL −1 , with a detection limit of 0.2 ng mL −1 (3σ) and the relative standard deviations lower than 2.1%. At a flow rate of 2.0 mL min −1 , the whole determining performance including sampling and washing could be accomplished in 30 s, giving a sampling efficiency of 120 h −1 . The proposed method was applied successfully to the direct hesperetin determination in human serum with recoveries from 97.0 to 106.6%, and indirect hesperidin quantification in 2.5 g pericarpium citri reticulatae showing that the content is 8.1 ± 0.2%. The possible CL mechanism of luminol-dissolved oxygen-hesperetin reaction was also discussed in detail.

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Antiplatelet activity of hesperetin, a bioflavonoid, is mainly mediated by inhibition of PLC-γ2 phosphorylation and cyclooxygenase-1 activity

Cited by 79 publications

References 37 publications

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Effects of Unripe Citrus hassaku Fruits Extract and Its Flavanone Glycosides on Blood Fluidity

Determination of Hesperetin in Pericarpium Citri Reticulatae and Human Serum Using Flow Injection Chemiluminescence

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