Milk Thistle

Publication Title: 
Journal of Alternative and Complementary Medicine (New York, N.Y.)

OBJECTIVES: To determine the potential toxicity and safety of the Chinese herbal medicine NPI-028 in rats following subchronic (3-month) exposure via daily oral consumption. DESIGN: Subchronic toxicity was evaluated in four groups of rats (n = 10 per group) receiving NPI-028 orally at a dose of either 0.0 (normal diet control), 0.5, 1.0, or 2.0 g/kg, ingested as part of their daily diet for 3 months. NPI-028 was incorporated into powdered rat chow diet as a specific percent of the total diet provided each day.

Author(s): 
Keyler, Daniel E.
Baker, John I.
Lee, David Y. W.
Overstreet, David H.
Boucher, Tacey A.
Lenz, Scott K.
Publication Title: 
Clinical Cancer Research: An Official Journal of the American Association for Cancer Research

PURPOSE: Milk thistle (Silybum marianum) is one of the most commonly used herbal therapies, and its principal constituent silybin significantly inhibits cytochrome P450 isoform 3A4 (CYP3A4) and UDP glucuronosyltransferase isoform 1A1 (UGT1A1) in vitro. Here, we investigated whether milk thistle affects the pharmacokinetics of irinotecan, a substrate for CYP3A4 and UGT1A1, in humans. EXPERIMENTAL DESIGN: Six cancer patients were treated with irinotecan (dose, 125 mg/m(2)) given as a 90-minute infusion once every week.

Author(s): 
van Erp, Nielka P. H.
Baker, Sharyn D.
Zhao, Ming
Rudek, Michelle A.
Guchelaar, Henk-Jan
Nortier, Johan W. R.
Sparreboom, Alex
Gelderblom, Hans
Publication Title: 
Cancer Epidemiology, Biomarkers & Prevention: A Publication of the American Association for Cancer Research, Cosponsored by the American Society of Preventive Oncology

Naturopathic physicians commonly make dietary and/or dietary supplement recommendations for breast cancer prevention. This placebo-controlled, parallel-arm, pilot study tested the effects of two naturopathic interventions over five menstrual cycles on sex steroid hormones and metabolic markers in 40 healthy premenopausal women.

Author(s): 
Greenlee, Heather
Atkinson, Charlotte
Stanczyk, Frank Z.
Lampe, Johanna W.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

Silymarin, a mixture of polyphenolic flavonoids extracted from milk thistle (Silybum marianum), is composed mainly of silychristin, silydianin, silybin A, silybin B (SB(B)), isosilybin A (ISB(A)), and isosilybin B. In this study, the plasma concentrations of free (unconjugated), conjugated (sulfated and glucuronidated), and total (free and conjugated) silymarin flavonolignans were measured using liquid chromatography-electrospray ionization-mass spectrometry, after a single oral dose of 600 mg of standardized milk thistle extracts to three healthy volunteers.

Author(s): 
Wen, Zhiming
Dumas, Todd E.
Schrieber, Sarah J.
Hawke, Roy L.
Fried, Michael W.
Smith, Philip C.
Publication Title: 
Journal of Natural Products

Isosilybin A (1) is one of the major flavonolignans that constitute silymarin, an extract of the fruits (achenes) of milk thistle (Silybum marianum). The chemistry of the Silybum flavonolignans has been studied for over four decades, and the absolute configuration of 1 has been determined previously by electronic circular dichroism and X-ray crystallography via correlating the relative configuration of the phenylpropanoid moiety to the established absolute configuration of the 3-hydroxyflavanone portion of the molecule.

Author(s): 
Sy-Cordero, Arlene A.
Day, Cynthia S.
Oberlies, Nicholas H.
Publication Title: 
Bioorganic & Medicinal Chemistry

Silymarin, an extract of the seeds of milk thistle (Silybum marianum), is used as an herbal remedy, particularly for hepatoprotection. The main chemical constituents in silymarin are seven flavonolignans. Recent studies explored the non-selective methylation of one flavonolignan, silybin B, and then tested those analogues for cytotoxicity and inhibition of both cytochrome P450 (CYP) 2C9 activity in human liver microsomes and hepatitis C virus infection in a human hepatoma (Huh7.5.1) cell line. In general, enhanced bioactivity was observed with the analogues.

Author(s): 
Althagafy, Hanan S.
Graf, Tyler N.
Sy-Cordero, Arlene A.
Gufford, Brandon T.
Paine, Mary F.
Wagoner, Jessica
Polyak, Stephen J.
Croatt, Mitchell P.
Oberlies, Nicholas H.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

Milk thistle (Silybum marianum) extracts, one of the most widely used dietary supplements, contain a mixture of six major flavonolignans (silybin A, silybin B, isosilybin A, isosilybin B, silychristin, and silydianin) and other components. However, the pharmacokinetics of the free individual flavonolignans have been only partially investigated in humans. Furthermore, antioxidant effects of the extract, which may underlie the basis of many therapeutic effects, have not been thoroughly assessed.

Author(s): 
Zhu, Hao-Jie
Brinda, Bryan J.
Chavin, Kenneth D.
Bernstein, Hilary J.
Patrick, Kennerly S.
Markowitz, John S.
Publication Title: 
The Journal of Organic Chemistry

The mechanism for the biomimetic synthesis of flavonolignan diastereoisomers in milk thistle is proposed to proceed by single-electron oxidation of coniferyl alcohol, subsequent reaction with one of the oxygen atoms of taxifolin's catechol moiety, and finally, further oxidation to form four of the major components of silymarin: silybin A, silybin B, isosilybin A, and isosilybin B. This mechanism is significantly different from a previously proposed process that involves the coupling of two independently formed radicals.

Author(s): 
Althagafy, Hanan S.
Meza-Aviña, Maria Elena
Oberlies, Nicholas H.
Croatt, Mitchell P.
Publication Title: 
Journal of Natural Products

Peroxisome proliferator-activated receptor gamma (PPARγ) is a key regulator of glucose and lipid metabolism. Agonists of this nuclear receptor are used in the treatment of type 2 diabetes and are also studied as a potential treatment of other metabolic diseases, including nonalcoholic fatty liver disease. Silymarin, a concentrated phenolic mixture from milk thistle (Silybum marianum) seeds, is used widely as a supportive agent in the treatment of a variety of liver diseases. In this study, the PPARγ activation potential of silymarin and its main constituents was investigated.

Author(s): 
Pferschy-Wenzig, Eva-Maria
Atanasov, Atanas G.
Malainer, Clemens
Noha, Stefan M.
Kunert, Olaf
Schuster, Daniela
Heiss, Elke H.
Oberlies, Nicholas H.
Wagner, Hildebert
Bauer, Rudolf
Dirsch, Verena M.
Publication Title: 
National Toxicology Program Technical Report Series

Milk thistle extracts have been used as medicinal herbs in the treatment of liver cirrhosis, chronic hepatitis (liver inflammation), and gallbladder disorders. Treatment claims also include lowering cholesterol levels; reducing insulin resistance; reducing the growth of cancer cells in breast, cervical, and prostate gland cancers; and antiviral activity. Other reported uses of milk thistle in folk medicine include as a treatment for malarial fever, bronchitis, gallstones, jaundice, peritonitis, uterine congestion, varicose veins, and as a milk production stimulant for nursing mothers.

Author(s): 
National Toxicology Program

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