Herbs with Antidepressant Effects
Scott Mendelson in Herbal Treatment of Major Depression, 2019
Silymarin has potent anti-inflammatory and antioxidant effects. The in vivo antioxidant effects of silymarin have been shown in numerous studies of its hepatoprotective effects. Silymarin almost completely blocked the oxidative cirrhotic damage of CCl4 in the livers of rats. Serum transaminases remained within normal limits, and lipid peroxidation in liver tissue was prevented.4 In a similar study, silymarin prevented increases in transaminases after treatment with CCl4, and also prevented decreases in superoxide dismutase, glutathione reductase, glutathione -S-transferase, and glutathione in liver tissue. CCl4-induced increases in serum pro-inflammatory cytokines including TNF-α, TGF-β1, and IL-6 were also attenuated.5
The Rational Use of Dietary Supplements, Nutraceuticals, and Functional Foods for the Diabetic and Prediabetic Patient
Jeffrey I. Mechanick, Elise M. Brett in Nutritional Strategies for the Diabetic & Prediabetic Patient, 2006
Silymarin, or milk thistle (Silibum marianum), is best known for its beneficial effects in patients with viral or alcoholic hepatitis. Silymarin contains polyphenolic flavonoids and antioxidants that act to decrease glutathione oxidation, stabilize membranes, and normalize malondialdehyde concentrations [72]. Velussi et al. [73] conducted a 12-month open controlled study of 60 patients with insulin-requiring T2DM and alcoholic cirrhosis, receiving silymarin, 600 mg/day. They demonstrated improved glycemic control (decreased mean glucose from 202 mg/dL to 172 mg/dL and A1C from 8% to 7.2%) and decreased insulin requirements (55 to 42 units/day) with the treatment (evidence level 3) [73]. In another multi-center prospective randomized controlled trial (PRCT), a new oral formuation of silybin-β-cyclodextrin given to 60 patients with T2DM and alcoholic hepatitis was associated with improved fasting glucose (174 mg/dL to 148 mg/dL) (evidence level 3) [74]. Silymarin may also hold promise for patients with T1DM. Silymarin induces β-cell cytoprotection and improves GSIS by inhibiting cytokine-induced NO production and suppressing c-Jun N-terminal kinase (JNK) and Janus kinase (JAK)/signal transducers and activators of transcription (STAT) pathways [75]. The relative safety of silymarin has been demonstrated in clinical studies (grade C).
Nutraceutical Intervention for Treatment of Alcoholism and Drinking Problems
Raj K. Keservani, Anil K. Sharma, Rajesh K. Kesharwani in Nutraceuticals and Dietary Supplements, 2020
Chemically, silymarin is a cluster of flavonoids (silibinin, silidianin, and silicristin), that aid in repairing damaged liver cells caused by alcohol and other noxious ingredients. Silymarin also helps in keeping new liver cells from being destroyed by the same substance(s), reduces inflammation (effective in liver inflammation or hepatitis), and is a powerful antioxidant. It also helps in the recovery process by supporting and healing the liver, detoxifying the body. It is typically used to treat liver cirrhosis, chronic hepatitis (liver inflammation), toxin-induced liver damage (including the prevention of severe liver damage) from Amanita phalloides (death cap) mushroom poisoning, and gallbladder disorders (Greenlee et al., 2007; Tamayo and Diamond 2007).
Silymarin nanoemulsion against human hepatocellular carcinoma: development and optimization
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Usama Ahmad, Juber Akhtar, Satya Prakash Singh, Farhan Jalees Ahmad, Sahabjada Siddiqui
Silymarin is obtained from the purified extract of seeds and fruits of Silybum marianum (commonly known as milk thistle plant). It has been used for centuries as an herbal medicine and food supplement for the treatment of liver and gallbladder disorders, including hepatitis, cirrhosis, jaundice, and to protect the liver against poisoning from chemical and environmental toxins, including snake bites, insect stings, mushroom poisoning, and alcohol. Most of the medicinal compounds found in milk thistle are present in high concentrations in the seeds. These compounds include silymarin, which is composed of three isomer flavonolignans: silybin, silydianin, and silychristin [1]. Silybin is considered the major and most active component of silymarin [2,3]. It inhibit the hepatotoxin binding to receptor sites on the hepatocyte membrane; reduction of glutathione oxidation to enhance its level in the liver and intestine; antioxidant activity; and stimulation of ribosomal RNA polymerase and subsequent protein synthesis, leading to enhanced hepatocyte regeneration [4]. However, despite such potential benefits, silymarin is able to produce little effect in vivo both in humans and in animals due to its poor bioavailability. The four major causes of limited silymarin bioavailability are extensive phase II metabolism, low permeability across intestinal epithelial cells, low aqueous solubility, and rapid excretion in bile and urine. These factors necessitate the incorporation of silymarin into a form that can augment its bioavailability [5].
Silymarin loaded floating polymer(s) microspheres: characterization, in-vitro/in-vivo evaluation
Published in Pharmaceutical Development and Technology, 2020
Afaf A. Ramadan, Asmaa M. Elbakry, Hatem A. Sarhan, Salwa H. Ali
Silymarin is 3, 5, 7-trihydroxy-2-[3-(4-hydroxy-3-methoxy phenyl)-2-(hydroxy-methyl)-1,4-benzodioxan-6-yl]-4-chromanone. It is administered mainly as anti-hepatotoxic drug. As it is considered a free radical scavenger, with hepato-protective activity, so it is recommended to be administered for treatment of liver diseases from different etiology (Federico et al. 2017). Also silymarin possess an antioxidant activity, inhibit lipid peroxidation and stabilize the membrane. It is considered a complex mixture of four flavonolignan isomers (silybin, isosilybin, silydianin and silychristin). Thus silymarin is considered a drug of interest for its wide pharmacological effect. Silymarin is characterized by yellow color and very poor solubility in water (0.04 mg/ml) which make it a good candidate for gastro-retentive drug delivery system (Arora et al. 2005). Encapsulation of Silymarin inside microspheres leads to high efficiency of drug release accompanied with control of this release from polymeric membrane which leads to maintained concentration with longer time. Silymarin suffering from short lasting action, low enzymatic stability and fast clearance, thus it is considered an excellent model drug for gastro-retentive dosage form.
Characterization of glutathione conjugates derived from reactive metabolites of seven silymarin isomers
Published in Xenobiotica, 2019
Yan Chen, Jing Yu, Xu Wang, Hui Li, Xu Mao, Ying Peng, Jiang Zheng
Drug metabolizing enzymes and transporters may be inhibited or induced by some biologically active ingredients of herbal medicines, thereby changes in pharmacokinetic behaviors and metabolism may cause drug-drug interactions (DDIs) (Ekins et al., 2003). Silymarin is an inhibitor of varieties of enzymes and transporters (Beckmann-Knopp et al., 2000; Gerhauser et al., 2003; Kosina et al., 2005; Mooiman et al., 2014; Sridar et al., 2004; Venkataramanan et al., 2000; Zuber et al., 2002), which could change the pharmacokinetic parameters of some drugs with small therapeutic window, leading to even severe DDI. Metabolic interaction is the highest frequency of occurrence among the mechanisms of DDIs (Liu et al., 2003). Several mechanism-based inactivators of P450 enzymes have shown some clinical relevance of drug-drug interactions, such as mibefradil (Sekiguchi et al., 2011), clarithromycin and erythromycin (Akiyoshi et al., 2013), and some consequently brought on withdrawal of the drugs from the market. This encouraged us to investigate the metabolic activation of silymarin to facilitate the understanding of biochemical mechanism of DDIs.
Related Knowledge Centers
- Amanita Phalloides
- Cirrhosis
- Diastereomer
- Silybum
- Flavonolignan
- Silychristin
- Fatty Liver Disease
- Metabolic Dysfunction–Associated Steatotic Liver Disease
- Child–Pugh Score
- Stat3