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Clinical Studies
References
Hesperidin is a bioflavonoid compound found in plants, mainly in citrus fruit peel, known as a citrus bioflavonoid. It is closely related to other citrus bioflavonoids such as quercetin, rutin and diosmin. Hesperidin alone, or in combination with other citrus bioflavonoids, is most often used for vascular conditions such as hemorrhoids and varicose veins. It has an anti-inflammatory and pain relieving effect in these conditions.
Hesperidin may also reduce the generation of free radicals and inhibit tumor growth as well as chronic venous insufficiency, pain and night leg cramps.
Published Clinical Studiesclin
1
Hesperidin, a citrus flavonoid, inhibits bone loss and decreases serum and hepatic lipids in ovariectomized mice.
Chiba H, Uehara M, Wu J, Wang X, Masuyama R, Suzuki K, Kanazawa K, Ishimi Y.
Division of Food Science, National Institute of Health and Nutrition, Tokyo, Japan.
The purpose of this study was to examine whether hesperidin inhibits bone loss in ovariectomized mice (OVX), an animal model of postmenopausal osteoporosis. Forty 8-wk-old female ddY mice were assigned to five groups: a sham-operated group fed the control diet (AIN-93G), an OVX group fed the control diet, an OVX+HesA group fed the control diet containing 0.5 g/100 g hesperidin, and an OVX+HesB group fed the control diet containing 0.7 g/100 g alpha-glucosylhesperidin and an OVX+17beta-estradiol (E(2)) group fed the control diet and administered 0.03 micro g E(2)/d with a mini-osmotic pump. After 4 wk, the mice were killed and blood, femoral, uterine and liver were sampled immediately. Hesperidin administration did not affect the uterine weight. In OVX mice, the bone mineral density of the femur was lower than in the sham group (P < 0.05) and this bone loss was significantly prevented by dietary hesperidin or alpha-glucosylhesperidin. The Ca, P and Zn concentrations in the femur were significantly higher in the hesperidin-fed and E(2) groups than in the OVX group. Histomorphometric analyses showed that the trabecular bone volume and trabecular thickness in the femoral distal metaphysis were markedly decreased (P < 0.05) by OVX, and alpha-glucosylhesperidin significantly prevented this bone loss. Furthermore, hesperidin decreased the osteoclast number of the femoral metaphysis in OVX mice, as did E(2). Serum and hepatic lipids were lower in mice that consumed the hesperidin-containing diets (P < 0.05) than in the OVX group fed the control diet. These results suggest a possible role for citrus flavonoids in the prevention of lifestyle-related diseases because of their beneficial effects on bone and lipids.
PMID: 12771335 [PubMed - indexed for MEDLINE]
6-methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS.2
Marder M, Viola H, Wasowski C, Fernandez S, Medina JH, Paladini AC.
Facultad de Farmacia y Bioquimica, Instituto de Quimica y Fisicoquimica Biologicas, Junin 956 (1113), Buenos Aires, Argentina.
Valerian is an ancient tranquillizing drug obtained from the underground organs of several Valeriana species. Its active principles were assumed to be terpenoids in the form of valepotriates and/or as components of the essential oil. However, unknown active compounds were not discarded and synergic effects were suspected.We have recently isolated 6-methylapigenin (MA) from Valeriana wallichii and proved that it is a benzodiazepine binding site (BDZ-bs) ligand [Planta Med. 68 (2002) 934].The present paper is the first report of the presence of 2S(-)-hesperidin in valeriana and describes that it has sedative and sleep-enhancing properties. MA, in turn, was found to have anxiolytic properties and was able to potentiate the sleep-enhancing properties of hesperidin (HN).MA and HN are new members of the growing family of natural flavonoids with activity on the CNS, and their properties suggest that they are promising drug leads in the field.
PMID: 12895671 [PubMed - in process]
Hot flashes--a review of the literature on alternative and complementary treatment approaches.3
Philp HA.
Hot flashes are a common experience for menopausal women, with an 85-percent incidence in the West. With the increased knowledge of side effects attributable to conventional treatment options, more women are exploring natural alternatives. Although more definitive research is necessary, several natural therapies show promise in treating hot flashes without the risks associated with conventional therapies. Soy and other phytoestrogens, black cohosh, evening primrose oil, vitamin E, the bioflavonoid hesperidin with vitamin C, ferulic acid, acupuncture treatment, and regular aerobic exercise have been shown effective in treating hot flashes in menopausal women.
Publication Types:
PMID: 12946239 [PubMed - indexed for MEDLINE]
Comparative study of flavonoids in experimental models of inflammation.4
Rotelli AE, Guardia T, Juarez AO, de la Rocha NE, Pelzer LE.
Catedra de Farmacologia, Facultad de Quimica, Bioquimica y Farmacia, Universidad Nacional de San Luis, Chacabuco y Pedernera, 5700 San Luis, Argentina. arotelli@unsl.edu.ar
The anti-inflammatory activities of flavonols (quercetin, rutin and morin) and flavanones (hesperetin and hesperidin) were investigated in animal models of acute and chronic inflammation. Rutin was only effective in the chronic process, principally in adjuvant arthritis. On neurogenic inflammation induced by xylene, only the flavanones were effective; besides, these compounds were the most effective on subchronic process. The most important compound in reducing paw oedema induced by carrageenan was quercetin.
PMID: 14527825 [PubMed - in process]
5
The compositional characterisation and antioxidant activity of fresh juices from sicilian sweet orange (Citrus sinensis L. Osbeck) varieties.
Proteggente AR, Saija A, De Pasquale A, Rice-Evans CA.
Antioxidant Research Group, Wolfson Centre for Age-Related Diseases, GKT School of Biomedical Sciences, King's College London, London SE1 9RT, UK.
Epidemiological evidence has suggested that consumption of fruit and vegetables reduces the risk of both cancer and cardiovascular diseases, potentially through the biological actions of components such as vitamin C, vitamin E, flavonoids and carotenoids. Citrus species are extremely rich sources in vitamin C and flavanones, a class of compounds which belongs to the flavonoids family. A comparison of the phenolic compositions, the ascorbic acid contents and the antioxidant activities of fresh Sicilian orange juices from pigmented (Moro, Tarocco and Sanguinello) and non-pigmented (Ovale, Valencia and Navel) varieties of orange (Citrus sinensis L. Osbeck), was undertaken. The simultaneous characterisation and quantification of the major flavanone, anthocyanin and hydroxycinnamate components were attained by HPLC with diode array detection. Differences between varieties in terms of the flavanone glycoside content, particularly hesperidin, were observed, with the Tarocco juices reporting the highest content. Furthermore, cyanidin-3-glucoside and cyanidin-3-(6"-malonyl)-glucoside were predominant in all the pigmented varieties, but their concentration was higher in the juices of the Moro variety. Quantitatively, the major antioxidant component of all juices was ascorbic acid and its concentration was significantly correlated (r = 0.74, P < 0.001) with the total antioxidant activity of the juices, determined in vitro using the ABTS radical cation decolorization assay. Similarly, hydroxycinnamates (r = 0.73, P < 0.01) and anthocyanins (r = 0.98, P < 0.001) content showed a good correlation with the determined antioxidant capacity. Therefore orange juices, particularly those rich in anthocyanins, may represent a significant dietary source of flavonoids.
PMID: 12868495 [PubMed - indexed for MEDLINE]
6
Effects of baicalein, berberine, curcumin and hesperidin on mucin release from airway goblet cells.
Lee CJ, Lee JH, Seok JH, Hur GM, Park YC, Seol IC, Kim YH.
Department of Pharmacology, College of Medicine, Chungnam National University, Daejeon, Korea. LCJ123@cnu.ac.kr
Baicalein, berberine, curcumin and hesperidin are the major components derived from Scutellaria baicalensis, Coptis japonica, Curcuma longa and Poncirus trifoliata, respectively. These plants have been used for the treatment of diverse chronic inflammatory diseases including respiratory disease in oriental medicine and their respective major components were reported to have various biological effects including anti-inflammatory activity. In the present study, we investigated whether these four natural products affect mucin release from airway goblet cells and compared the possible activities of these agents with the inhibitory action on mucin release by PLL and the stimulatory action by ATP. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled using 3H-glucosamine for 24 h and chased for 30 min in the presence of varying concentrations of each agent to assess the effects on 3H-mucin release. The results were as follows: (i) baicalein did not affect mucin release significantly; (ii) berberine, curcumin and hesperidin increased mucin release at the highest concentration (10 - 4 M); (iii) PLL inhibited and ATP increased mucin release. We conclude that berberine, curcumin and hesperidin can increase mucin release by directly acting on airway mucin-secreting cells and suggest that these agents be further studied for possible use as mild expectorants during the treatment of chronic airway diseases. Abbreviations. PLL:poly- L-lysine ATP:adenosine triphosphate HTSE:hamster tracheal surface epithelial DMSO:dimethylsulfoxide IL-12:interleukin-12 PBS:phosphate-buffered saline
PMID: 12865970 [PubMed - indexed for MEDLINE]
7
Inhibition of inducible isoforms of cyclooxygenase and nitric oxide synthase by flavonoid hesperidin in mouse macrophage cell line.
Sakata K, Hirose Y, Qiao Z, Tanaka T, Mori H.
Department of Tumor Pathology, Gifu University School of Medicine, 40 Tsukasa-machi, Gifu 500-8705, Japan. f2101002@guedu.cc.gifu-u.ac.jp
Previous data have shown that a citrus flavanone, hesperidin possesses chemopreventive efficacies. We designed to investigate the inhibitory effect of hesperidin on lipopolysaccharide (LPS)-induced over-expression of cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) proteins, over-production of prostaglandin E2 (PGE2) and nitric oxide (NO) using mouse macrophage cells. Treatment with hesperidin suppressed production of PGE2, nitrogen dioxide (NO2), and expression of iNOS protein. In the case of COX-2, hesperidin did not affect the protein level. Our data indicate hesperidin as a COX-2 and iNOS inhibitor, which might be related to the anti-inflammatory and anti-tumorigenic efficacies.
PMID: 12969786 [PubMed - indexed for MEDLINE]
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