RESEARCH ARTICLE Synergistic Anticancer Effects of Silibinin and ...
Chrysin và silibinin kháng T47D
Chrysin
From Wikipedia, the free encyclopedia
 | This article needs more medical references for verification or relies too heavily on primary sources. (September 2015) |  |
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| Names | |
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| IUPAC name
5,7-Dihydroxy-2-phenyl-4H-chromen-4-one
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| Other names
5,7-Dihydroxyflavone; NP-005901; Galangin flavanone
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| Identifiers | |
3D model (JSmol)
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| ChEBI | |
| ChemSpider | |
| ECHA InfoCard | 100.006.864 |
| KEGG | |
PubChem CID
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| UNII | |
| Properties | |
| C15H10O4 | |
| Molar mass | 254.24 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Chrysin is a naturally occurring flavone, a type of flavonoid. It is found in the passion flowers Passiflora caerulea and Passiflora incarnata, and in Oroxylum indicum. It is also found in chamomile, in the mushroom Pleurotus ostreatus,[1] and in honeycomb.
Aromatase inhibition[edit]
Studies performed in vivo show that orally administered chrysin does not have clinical activity as an aromataseinhibitor.[2][3]
Chrysin is available as a bodybuilding supplement and it is taken with the hope of raising testosterone levels or stimulating testosterone production; however, there is no clinical evidence for this effect.
Inflammation[edit]
Chrysin is under laboratory research for its potential effects on inflammation,[4] but there is no evidence it has anti-inflammatory activity in humans.
Bioavailability[edit]
Silibinin
From Wikipedia, the free encyclopedia
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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral and Intravenous |
| ATC code | |
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| UNII | |
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| ChEBI | |
| ChEMBL | |
| ECHA InfoCard | 100.041.168 |
| Chemical and physical data | |
| Formula | C25H22O10 |
| Molar mass | 482.44 g/mol |
| 3D model (Jmol) | |
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Silibinin (INN), also known as silybin (both from Silybum, the generic name of the plant from which it is extracted), is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin, and others. Silibinin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio.[1] The mixture exhibits a number of pharmacological effects, particularly in the liver, and there is some clinical evidence for the use of silibinin as a supportive element in alcoholic and child grade 'A' liver cirrhosis.[2]
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[hide]Pharmacology[edit]
Poor water solubility and bioavailability of silymarin led to the development of enhanced formulations. Silipide (trade name Siliphos), a complex of silymarin and phosphatidylcholine (lecithin), is about 10 times more bioavailable than silymarin.[3] An earlier study had concluded Siliphos to have 4.6 fold higher bioavailability.[4] It has been also reported that silymarin inclusion complex with β-cyclodextrin is much more soluble than silymarin itself.[5] There have also been prepared glycosides of silybin, which show better water solubility and even stronger hepatoprotective effect.[6]
Silymarin, as other flavonoids, has been shown to inhibit P-glycoprotein-mediated cellular efflux.[7] The modulation of P-glycoprotein activity may result in altered absorption and bioavailability of drugs that are P-glycoprotein substrates. It has been reported that silymarin inhibits cytochrome P450 enzymes and an interaction with drugs primarily cleared by P450s cannot be excluded.[8]
Toxicity[edit]
A phase I clinical trial in humans with prostate cancer designed to study the effects of high dose silibinin found 13 grams daily to be well tolerated in patients with advanced prostate cancer with asymptomatic liver toxicity (hyperbilirubinemiaand elevation of alanine aminotransferase) being the most commonly seen adverse event.[9]
Medical uses[edit]
Silibinin is available as drug (Legalon® SIL (Madaus) (D, CH, A) and Silimarit® (Bionorica), a Silymarin product) in some EU countries and used in the treatment of toxic liver damage (e.g. IV treatment in case of death cap poisoning); as adjunctive therapy in chronic hepatitis and cirrhosis. See also Silybum marianum#Medicinal use
For approved drug preparations and parenteral applications in the treatment of Amanita mushroom poisoning, the water-soluble silibinin-C-2’,3-dihyrogensuccinate disodium salt is used. In 2011, the same compound also received Orphan Medicinal Product Designation for the prevention of recurrent hepatitis C in liver transplant recipients by the European Commission.[12]
Potential medical uses[edit]
Silibinin is under investigation to see whether it may have a role in cancer treatment (e.g. due to its inhibition of STAT3 signalling).[13]
Silibinin also has a number of potential mechanisms that could benefit the skin. These include chemoprotective effects from environmental toxins, anti-inflammatory effects, protection from UV induced photocarcinogenesis, protection from sunburn, protection from UVB-induced epidermal hyperplasia, and DNA repair for UV induced DNA damage (double strand breaks).[14]
Biotechnology[edit]
Silymarin can be produced in callus and cells suspensions of Silybum marianum and substituted pyrazinecarboxamides can be used as abiotic elicitors of flavolignan production.[15]
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