Hesperidin-A short Review

 

Durgadevi Nardarajah

1st Year BDS, Saveetha Dental College and Hospital, Chennai India

*Corresponding Author E-mail: durgadevi1605@gmail.com

 

 

ABSTRACT:

Hesperidin, also known by other names, is derived from citrus fruits. It is classified as a flavonoid with anti-oxidant or antimicrobial properties. The drug is mainly considered as a herbal supplement that is used for medical purposes. Hesperidin is used in the treatment of breast cancer, lymphedema, cardiovascular, hemorrhoids, venous stasis, celebralvascular, and varicose veins. The side effects of the drug include gastrointestinal reactions including nausea and diarrhea. The precautions of using the drug include risk of bleeding, drowsiness, headaches, and allergic patients. Pregnant women are also required to use the drug under the prescription of a physician. The pharmacology and pharmacokinetics of hesperidin are not fully understood.

 

KEYWORDS: Hesperidin, anti-cancer agent.

 

 


INTRODUCTION:

Hesperidin is chemical that is mainly extracted from citrus fruits [1]. The plant’s chemical extract can be used alone, or combined with other plant chemicals for medicinal purposes. The drug is classified under the flavonoid group and may have antimicrobial or antioxidant properties. Because of these, it may have some effects on the human immune system. Apart from the effects on the immune system, when combined with other ingredients, hesperidin has been found to have medical benefits to the blood circulatory system [2-5].

 

Hesperidin:

Hesperidin is made up of anti-oxidants. Hesperidin has been known to treat various conditions including lymphedema, hemorrhoids, venous stasis, and varicose veins. It is also used in treatment of cardiovascular and celebralvascular diseases as well as some abortion cases [6-12]. Hesperidin is mainly applied during cancer surgeries. This implies that it can be effective at any stage of cancer treatment. Although toleration of hesperidin supplements is quite high, there are possible side effects. The adverse effects mainly involve gastrointestinal reactions. These include diarrhea and nausea among others [13-17].

 

The typical hesperidin is in the form of nutritional supplements like Vitamin C. However, they often contain other bioflavonoids. Hesperidin is also presented in other forms such as hesperidin-complex supplements, combinations with diosmin, different formulations with hesperidin, and orange juice with pulp [4]. Because of its forms, hesperidin is often considered as a non-prescription drug. Instead, it is considered as a supplement [13].

Clinical study tested the effect of the drug in treating various types of cancer including colon cancer, skin cancer esophageal cancer, and urinary bladder cancer among others. This research showed that hesperidin was more potent than other bioflavonoids and flavonoids. However, there is need for more clinical trials to ascertain the effects of hesperidin [14].

 

The drug is mainly used in the treatment of breast cancer. [7].

 

Other Names:

Hesperidin has other names that include Bioflavonoïdes d’Agrumes, Bioflavonoide, bioflavonoid Concentrate, Citrus Bioflavonoid, Bioflavonoid, Bioflavonoid Extract, Citrus Bioflavones, Bioflavonoid Complex, Bioflavonoïde d’Agrume, and Citrus Bioflavonoid Extract among others [7] [18-20].

 


 

Author

Year of Publication

Title

Fact(s)

Balakrishnan, A., and Menon, V.

2007

Antioxidant properties of hesperidin in nicotine-induced lung toxicity

Talks about hesperidin and its actions

Fathiazad, F., and Afshar, J.

2004

An investigation on methylation methods of hesperidin

Hesperidin has low solubility in water

Kar, A.

2003

Pharmacognosy and pharmacobiotechnology

Discusses the pharmacology and pharmacokinetics of hesperidin

Kingherbs

2007

Hesperidin

Drug monograph of hesperidin

Lee et al.,

2004

Antiallergic activity of hesperidin is activated by intestinal microflora

Presents a clinical test of hesperidin using animals

Natural Standard

2011

Hesperidin

Presents the drug monograph of hesperidin

Rizza et al.,

2011

Citrus polyphenol hesperidin stimulates production of nitric oxide in endothelial cells while improving endothelial function and reducing inflammatory markers in patients with metabolic syndrome

Talks about hesperidin and its properties

Shi et al.,

2012

Hesperidin prevents retinal and plasma abnormalities in streptozotocin-induced diabetic rats

Presents a clinical test of hesperidin using animals

WebMD

2013

Hesperidin

Discusses other names of hesperidin, properties and medical use

Westerink, B., and Cremers, T.

2007

Handbook of microdialysis: Methods, applications and perspectives

Hesperidin anti-oxidant properties among others

Yanez et al.,

2008

Pharmacokinetics of selected chiral flavonoids: Hesperetin, naringenin and eriodictyol in rats and their content in fruit juices

Hesperidin has a short half-life

Sahelian, R.

n.d.

Hesperidin found in oranges and lemons

Hesperidin is a flavonoid found in citrus fruits

Wong, C.

2013

Hesperidin

Hesperidin is extracted from citrus fruits

Health Grades Inc.

2011

Hesperidin

Hesperidin has medical uses

WebMD.

2013

Hesperidin

Hesperidin has medical uses

Focus Technology Co., Ltd.

2013

Hesperidin

Hesperidin has medical uses

Dahl, D.

2010

What is hesperidin (Vitamin P)?

Hesperidin has medical uses

MedMelon

2010

Hesperidin

Hesperidin has medical uses

Plant Extract

n.d.

Hesperidin

Hesperidin has medical uses

Natural Standard

2011

Hesperidin

Hesperidin has medical uses

Milenkovic et al.,

n.d.

Hesperidin displays relevant role in the nutrigenomic effect of orange juice on blood leukocytes in human volunteers: A randomized controlled cross-over study.

Hesperidin has medical benefits and side effects

Truven Health Analytics

2013

Hesperidin

Hesperidin has side effects

Wood-Moen, R.

2010

Side effects of hesperidin

Hesperidin has side effects

RxList Inc.

2013

Hesperidin

Hesperidin has other names

Drugs.com

2013

Hesperidin

Hesperidin has other names

Hesperidin REACH

n.d.

Hesperidin substance description

Hesperidin has other names

MIMs

2013

Diosmin + hesperidin

Overdose is rare

 


Pharmacology/Pharmacokinetics:

Hesperidin has low solubility in water [21]. Despite this, it is has higher solubility in water than aglycone hesperidin. It also has a low solubility in alcohol, and is insoluble in chloroform, benzene, and ether [6]. Hesperidin may contain either of several actions that include vasoprotective, anti-allergic, anticarcinogenic, anti-inflammatory, hypolipemic, or of antioxidant actions [22]. With regard to its potential anti-inflammatory action, aglycone hesperidin may be responsible. This is because hesperidin has been linked to the interference in the process of arachidonic acid. Additionally, hesperidin has been associated with inhibiting the release of histamine from the mast cells. This is possibly the reason for hesperidin’s anti-allergic activity. Regarding the hypolipidemic action of hesperidin, it is probably the effect of hesperidin in reducing levels of plasma cholesterol through deterring enzymes that perform that opposite task [14]. Moreover, hesperidin reduces microvascular permeability, which is a possible explanation for its vasoprotective action. Other actions of hesperidin do not have clear explanations [23].

 

With regard to pharmacokinetics of hesperidin, it remains unclear whether the drug is absorbed from the intestines as glycoside. However, it is assumed that hesperidin’s glucuronidation could take place in the intestine wall and in the liver. Aglycone hesperidin is detected in urine after about three hours from the time of ingesting hesperidin [14]. Moreover, following ingestion of hesperidin, it is detected in serum. However, it remains unclear whether the hesperidin is formed before or after absorption [23]. Hesperidin has a relatively short half-life of about 3-7 hours [24].

 

Dosage:

The dosage of hesperidin varies depending on its different forms. The dosages may be 20mg for nutritional supplements, 500mg to 2g for hesperidin-complex supplements, and 1-3g for combination product. These are daily dosages. Reports of over-dosage are rare [23] [25].

 

CONCLUSION:

Hesperidin is mainly used as a supplement. Although the drug has been found to have some medical benefits, there is need for more clinical tests to ascertain its effects. Currently, there are gaps or grey areas regarding the clinical efficacy of hesperidin. Although the drug is considered to treat certain diseases including breast cancer, cardiovascular diseases, and celebralvasuclar diseases among others, the actions of the drug are still not fully understood. Therefore, the pharmacokinetics and pharmacology of the drug is filled with some assumptions to fill the grey areas. However, hesperidin continues to be used as a supplement drug because it has limited adverse affects [9].

 

REFERENCES:

1.       Sahelian, R. (n.d.). Hesperidin found in oranges and lemons. Retrieved from http://www.raysahelian.com/hesperidin.html

2.       Westerink, B., and Cremers, T. (2007). Handbook of microdialysis: Methods, applications and perspectives. Academic Press.

3.       Rizza, S., Muniyappam R., Iantorno, M., Kim, J., Chen, H., and …Quon, M. (2011). Citrus polyphenol hesperidin stimulates production of nitric oxide in endothelial cells while improving endothelial functions and reducing inflammatory markers in patients with metabolic syndrome. JCEM, 96(5), E782-E792.

4.       Wong, C. (2013). Hesperidin. Retrieved from http://altmedicine.about.com/od/herbsupplementguide/a/Hesperidin.htm

5.       Health Grades Inc. (2011). Hesperidin. Retrieved from http://www.rightdiagnosis.com/vitamin/hesperidin.htm

6.       Kar, A. (2003). Pharmacognosy and pharmacobiotechnology. New Age International.

7.       WebMD. (2013). Hesperidin. Retrieved from http://www.webmd.com/vitamins-supplements/ingredientmono-1033-HESPERIDIN.aspx?activeIngredientId=1033andactiveIngredientName=HESPERIDIN

8.       Focus Technology Co., Ltd. (2013). Hesperidin. Retrieved from http://china-cac1.en.made-in-china.com/product/volmBLkPhaRX/China-Hesperidin.html

9.       Dahl, D. (2010). What is hesperidin (Vitamin P)? Retrieved from http://www.livestrong.com/article/342775-what-is-hesperidin-vitamin-p/

10.     MedMelon (2010). Hesperidin. Retrieved from http://www.medmelon.gr/frontend/new.php?aid=291andcid=111

11.     Plant Extract (n.d.). Hesperidin. Retrieved from http://www.naturalplantextract.com/active-ingredients/hesperidin.html

12.     Natural Standard (2011). Hesperidin. Retrieved from http://www.weiserx.com/ns/DisplayMonograph.asp?storeID=D5014D8206A24FA7A9B57A43F807BE7EandDocID=hesperidin

13.     Milenkovic, D., Deval, C., Dubray, C., Mazur, A., and Morand, C. (n.d.). Hesperidin displays relevant role in the nutrigenomic effect of orange juice on blood leukocytes in human volunteers: A randomized controlled cross-over study. Retrieved from http://www.plosone.org/article/info:doi/10.1371/journal.pone.0026669

14.     Lee, N., Choi, S., Park, S., Park, E., and Kim, D. (2004). Antiallergic activity of hesperidin is activated by intestinal microflora. Pharmacology, 71(4), 174-80.

15.     Shi, X., Liao, S., Mi, H., Guo, C., Qi, D., Li, F., and ... Yang, Z. (2012). Hesperidin prevents retinal and plasma abnormalities in streptozotocin-induced diabetic rats. Molecules (Basel, Switzerland), 17(11), 12868-12881. doi:10.3390/molecules171112868

16.     Truven Health Analytics (2013). Hesperidin. Retrieved from http://loyolauniversity.adam.com/content.aspx?productId=48andpid=48andgid=10459

17.     Wood-Moen, R. (2010). Side effects of hesperidin. Retrieved from http://www.livestrong.com/article/215299-side-effects-of-hesperidin/

18.     RxList Inc. (2013). Hesperidin. Retrieved from http://www.rxlist.com/hesperidin/supplements.htm

19.     Drugs.com (2013). Hesperidin. Retrieved from http://www.drugs.com/international/hesperidin.html

20.     Hesperidin REACH (n.d.). Hesperidin substance description. Retrieved from http://www.hesperidin-sief.com/hespiridin-substance-description

21.     Fathiazad, F., and Afshar, J. (2004). An investigation on methylation methods of hesperidin. Daru, 12(2), 67-70.

22.     Balakrishnan, A., and Menon, V. (2007). Antioxidant properties of hesperidin in nicotine-induced lung toxicity. Fundamental and Clinical Pharmacology, 21(5), 535-546.

23.     Kingherbs (2007). Hesperidin. Retrieved from http://www.kingherbs.com.cn/english.asp?id=40

24.     Yanez, J. A., Remsberg, C. M., Miranda, N. D., Vega-Villa, K. R., Andrews, P. K., and Davies, N. M. (2008). Pharmacokinetics of selected chiral flavonoids: Hesperetin, naringenin and eriodictyol in rats and their content in fruit juices. Biopharmaceuticals and Drug Disposition, 29(2), 63-82

25.     MIMS (2013). Diosmin + hesperidin. Retrieved from http://www.mims.com/USA/drug/info/diosmin%20+%20hesperidin/diosmin%20+%20hesperidin?type=full

 

 

 

 

Received on 30.07.2013       Modified on 05.09.2013

Accepted on 14.09.2013      © RJPT All right reserved

Research J. Pharm. and Tech. 7(1): Jan. 2014; Page   78-80