Hepatiguard

We encounter environmental toxins everywhere; from the air we breathe to the water we drink. These toxins can build up in our bodies, particularly in our liver. Hepatiguard is designed to support healthy liver function using four well researched ingredients. The result is a well-designed formula that supports men and women of all ABO blood types.

Hepatiguard comprises four synergistic ingredients:

Milk Thistle Standardized Extract (from Silybum marianum Seed, standardized to 80% Silybin/silymarin). The applicable parts of milk thistle are the seed and above ground parts. The seed is most commonly used medicinally. Silymarin, the active constituent of the milk thistle seed, consists of four flavonolignans called silibinin (silybin), isosilybinin, silichristin (silychristin), and silidianin. Silibinin makes up about 70% of silymarin. (1,2) When ingested, silymarin undergoes enterohepatic recirculation and has higher concentrations in liver cells.

Silymarin is a potent inhibitor of tumor necrosis factor (TNF). The cytotoxicity, inflammation, and apoptosis induced by TNF are effectively blocked by silymarin. Although the mechanism of this effect is not clear, it probably involves intracellular signaling. (3) Silybin is an antioxidant, a free radical scavenger, and an inhibitor of lipid peroxidation. (4) In vitro, silybin has shown an affinity for binding to p-glycoprotein, a transporter thought to be involved in the drug resistance of cancer cells. (5)

Several activities seem to contribute to the therapeutic effect of silymarin in liver disease. Silymarin seems to cause an alteration of the outer hepatocyte cell membrane that prevents toxin penetration. It also stimulates nucleolar polymerase A, resulting in increased ribosomal protein synthesis, which can stimulate liver regeneration and the formation of new hepatocytes. There is also some evidence that suggests that silymarin might have antifibrotic, anti-inflammatory, and immunomodulating effects that could also be beneficial in liver disease. (6) Silymarin and silybin inhibit beta-glucuronidase, which might help protect against hepatic injury and possibly colon cancer. Inhibition of beta-glucuronidase is thought to reduce the hydrolysis of glucuronides into toxic metabolites in the liver and intestine. (7)

Preliminary evidence indicates that milk thistle constituents might protect against kidney damage. In vitro, silibinin and silicristin can protect the kidney cells from nephrotoxic drugs such as acetaminophen, cisplatin, and vincristine. Silibinin and silicristin also appear to have a regenerative effect on kidney cells, similar to the effects on hepatic cells. (8)

There is some interest in using milk thistle for prostate cancer. In vitro research shows that silymarin and silibinin have antiproliferative effects on androgen-responsive prostate cancer cells. (9)

The above ground parts seem to have some estrogenic activity. A milk thistle plant extract appears to enhance estradiol binding to estrogen receptors and enhance estradiol-induced transcription activity in estrogen-responsive cells. (10) There is also preliminary evidence that suggests that milk thistle might affect drug metabolism. In vitro, silymarin and its flavonolignan, silibinin, inhibit cytochrome P450 2C9 (CYP2C9) and cytochrome P450 3A4 (CYP3A4), the major phase 1 hepatic enzyme. However, silymarin does not seem to affect the metabolism of indinavir (Crixivan), a CYP3A4 substrate, in healthy volunteers. (11) In vitro, silymarin and silibinin also inhibit uridine diphosphoglucuronosyl transferase (UGT), the major phase 2 enzyme that is responsible for glucuronidation. (12,13,14)

Bupleurum Root (from Bupleurum chinense).  The applicable part of bupleurum is the root. (15) Compounds isolated from Bupleurum species used in traditional Chinese medicine include saikosaponins, polysaccharides, and polyacetylenes. Saikosaponins are triterpenoid saponins, known as saikosides. (16) While the saikosaponin content of some species is very similar, that of other species varies considerably, as well as pharmacologic activity. (17, 18) The saikosaponin content is highest in Bupleurum falcatum (2- 8%) and Bupleurum chinense (1.7%). For infections, including the flu and the common cold, bupleurum is theorized to work by improving immune function.

Bupleurum falcatum is reported to cause proliferation of B-lymphocytes and stimulate them to produce immunoglobulins in vitro. It is also reported to stimulate in vitro macrophage activity, possibly by increasing the number of antibody-binding sites on the cell surface. (19) The constituent saikosaponin-d has immunoregulatory actions on T-lymphocytes, including promotion of interleukin-2 (IL-2) production and IL-2 receptor expression. (20) It also increases macrophage activity, IL-1 production and antibody response. (21) Bupleurum also is reported to have antitussive properties. (16) For peptic ulcers, bupleurum is thought to decrease gastric acid and pepsin secretion and have mucosal protecting effects. (22,23) Bupleurum is also reported to have antitumor, antibacterial, anti-inflammatory, antispasmodic, antioxidant, antiplatelet, and hepatoprotectant effects; however these effects have not been demonstrated in humans. (22-34)

Phyllanthus amarus Leaf Standardized Extract (standardized to 3% Bitter Principles).  The applicable part of the plant is the leaf. The principal constituents phyllanthine (bitter constituent) and hypophyllanthine (non-bitter compound) are isolated from the leaves. Phyllanthus contains these two lignans, as well as alkaloids, and bioflavonoids (e.g., quercetin and catechin), and geraniin, a tannin which is an in vitro anti-viral agent. While it remains unknown as to whether all of these ingredients have an anti-viral effect, research shows that this herb acts primarily on the liver. This action in the liver confirms its historical use as a remedy for jaundice.

Older studies published in India were reportedly conducted with Phyllanthus niruri, which is thought to be indigenous to the West Indies. (35) A report from India mentions Phyllanthus niruri is a synonym for Phyllanthus amarus; however, although these appear to be different species they have similar effects. (36-38) Phyllanthus niruri, is also known as Chanca piedra, which is thought to have multiple properties: antispasmodic, antiviral, bactericidal, antipyretic, and diuretic. It is also thought that chanca piedra reduces blood sugar and protects the liver; however, not all of these properties are supported by scientific evidence. (39) In vitro, the constituent niuriside, inhibits specific HIV-protein binding activity, but does not protect cells from acute HIV infection. (40) Preliminary studies in humans show Phyllanthus amarus, has diuretic, hypotensive and hypoglycemic effects. (41)

Turmeric Root (from Curcuma longa).  The applicable part of turmeric is the rhizome. Turmeric’s major active constituents are curcuminoids including curcumin (diferuloylmethane), a yellow pigment. It seems to have anti-inflammatory activity, possibly by inhibiting cyclooxygenase-2 (COX-2), prostaglandins, and leukotrienes. (42-45) Turmeric also exhibits chemopreventive and growth inhibitory activity against several tumor cell lines. It seems to induce apoptosis in cancer cells and may inhibit angiogenesis. (45-47) Curcumin might have antithrombotic effects. Preliminary research suggests it might inhibit platelet-activating factor and arachidonic acid platelet aggregation, possibly by interfering with thromboxane synthesis. (48) Other preliminary research suggests that turmeric might also have antioxidant and immunostimulatory effects. (44,49) It also seems to have activity against some bacteria, human immunodeficiency virus (HIV), and the protozoan Leishmania amazonensis. (44)

Turmeric/Curcumin, even in the common spice, long used in Indian cooking and long used by Ayurvedic practitioners, is a potent inhibitor of polyamine synthesis.

• Alcohol-related liver disease. Preliminary clinical research suggests that milk thistle taken orally might be helpful for treating alcoholic liver disease. (50-55)
• Diabetes. Preliminary clinical evidence suggests that the milk thistle constituent silymarin can reduce insulin resistance in people with coexisting diabetes and alcoholic cirrhosis. (56)
• Toxin-induced liver damage. Some research suggests milk thistle may limit liver damage after exposure to industrial toxicants such as toluene and xylene. (57) Most clinical studies of milk thistle’s effectiveness have used a specific extract standardized to 70-80% silymarin (Legalon).
• Preliminary evidence indicates that milk thistle constituents might protect against kidney damage. In vitro, silibinin and silicristin can protect the kidney cells from nephrotoxic drugs such as acetaminophen, cisplatin, and vincristine. Silibinin and silicristin also appear to have a regenerative effect on kidney cells, similar to the effects on hepatic cells. (58)
• Silymarin is a potent inhibitor of tumor necrosis factor (TNF). The cytotoxicity, inflammation, and apoptosis induced by TNF are effectively blocked by silymarin.
• In traditional Chinese medicine, bupleurum is not usually used alone, but rather as part of various herbal remedies. Bupleurum is the primary herb in dozens of classical formulations which serve a wide variety of harmonizing activities, and all of which regulate body energy, allowing it to flow freely and in a balanced manner, and for relieving blockages in the body and then discharging the toxin safely out of the system.
• Phyllanthus amarus, commonly used in Ayurvedic medicine, has been shown to be anti-viral, hepatoprotective, hypoglycemic, and to be of potential use in the treatment of Hepatitis B, jaundice, diabetes, and viral diseases including acute hepatitis, chronic persistent hepatitis, and part of the treatment for chronic active hepatitis.
• The antioxidant, anti-inflammatory and anti-carcinogenic properties of turmeric and curcumin are undergoing intense research. Tests in Germany, reported July 2003, found that “All fractions of the turmeric extract preparation exhibited pronounced antioxidant activity...” Turmeric extract tested more potent than garlic, devil’s claw, and salmon oil. (59)
• Turmeric is a potent inhibitor of the liver enzyme ornithine decarboxylase. This has the effect of lowering the production of polyamines, chemicals that act with insulin to encourage tissue growth and weight gain.

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