Cholestin

Related Terms

3Alpha-hydroxy-3,5-dihydromonacolin L, alkaloids, angkak, anka, ankaflavin, arroz de levadura roja (Spanish), Asian traditional fermentation foodstuff, astaxanthin, beni-koju, ben-koji, Chinese red yeast rice, Cholestin?, citrinin, compactin, CRYR, dehydromonacolin K, dihydromonacolin L, DSM1379, DSM1603, ergosterol, flavonoids, GABA, gamma-aminobutyric acid, glycosides, HMG-CoA reductase inhibitors, hon-chi, hong qu, hongqu, hung-chu, hydroxymethylglutaryl coenzyme A reductase, KCCM11832, koji, linoleic acid, lovastatin, M9011, mevinolin, monacolin, monacolin hyroxyacid, monacolin J, monacolin K, monacolin K (hydroxyl acid form), monacolin L, monacolin M, monacolin X, Monascaceae (yeast family), monascopyridine A, monascopyridine B, monascopyridine C, monascopyridine D, monascorubramine, monascorubrin, Monascus, Monascusanka, Monascus purpureus, Monascus purpureus fermentate, Monascus purpureus HM105, Monascus purpureus NTU568, Monascus purpureus Went rice, Monascusruber, monascorubramine, oleic acid, orange anka pigment, palmitoleic acid, Phaffia rhodozyma, phenols, protein, red fermented rice, red koji, red leaven, red mould rice, red rice, red rice yeast, red yeast, red yeast rice extract, rice, RICE products, rubropunctamine, rubropunctatin, RYR, RYRE, saponins, statins, stearic acid, tannins, Xue Zhi Kang, Xuezhikang, yellow anka pigment, Zhi tai, Zhitai.
Selected brand names: Cholestene? (red yeast rice), Cholestin? (containing red yeast rice; no longer available in the United States and Canada), Cholesto-Rite? (red yeast rice, gugulipid, Aspalathus linearis), Health Direct's Red Yeast Rice Vcaps (red yeast rice), Lipolysar, Only Naturals' Red Yeast Rice Plus, Source Naturals' Red Yeast Rice capsules.
Note: Monacolin K, a compound found in red yeast rice, has the same structure as the drugs lovastatin and mevinolin. This bottom line covers Monascuspurpureus, excluding details about related species.

Background

Red yeast rice (RYR) is made from yeast (Monascuspurpureus) grown on rice. It is a dietary staple in some Asian countries. Processed red yeast rice supplements include red yeast rice extract (RYRE), which is any extract of red yeast rice, and Xuezhikang, an alcohol extract of red yeast rice.
RYR contains several compounds known as monacolins, which block the production of cholesterol. One of these, monacolin K, has the same structure as the drugs lovastatin and mevinolin. Studies suggest that RYR use may lead to a 10-33% reduction in low-density lipoprotein (LDL, or "bad") cholesterol. This is a moderate effect, compared to the U.S. Food and Drug Administration (FDA)-approved "statin" drugs. Information on the long-term safety of RYR is limited at this time.
RYR extract (RYRE) has been sold in over-the-counter supplements to lower cholesterol, in the form of products such as Cholestin? (Pharmanex, Inc.). However, the formula has been changed. Cholestin? contains many compounds in addition to monacolin K, including other monacolins, starch, fiber, protein, and fatty acids. Research suggests that this product may treat high cholesterol and triglycerides in both humans and animals. Some studies report that RYR use may increase levels of high-density lipoprotein (HDL, or "good") cholesterol. However, information on the effects of monacolin K alone is lacking.
There has been some controversy between Pharmanex, Inc., the FDA, and statin manufacturers as to whether Cholestin? should be considered a drug or a dietary supplement. The U.S. District Court in Utah ruling in March 2001 states that RYRE is an unapproved drug. Thus, the RYRE known as Cholestin? is no longer available in the United States. Other products containing RYRE alone or in combination products may still be commercially available in the United States, primarily through Internet retailers.
Besides RYR's use for high cholesterol, pigments made by Monascus species have been used to color food in Asian cooking. Future uses of RYR may include decreasing heart disease risk and improving the health of people with diabetes.

Evidence Table

These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. GRADE *
These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. GRADE *


Monacolins, compounds found in red yeast rice extract (RYRE), have been found to have health benefits since the early 1980s. In particular, monacolin K has been marketed as lovastatin and mevinolin. However, due to the large number of compounds that may lower cholesterol other than monacolin K, the cholesterol-lowering mechanism is still unclear. It has been suggested that RYR may block absorption of cholesterol, promote the clearance of cholesterol, or exert antioxidant effects. Overall, results suggest that red yeast rice (RYR) products may lower levels of total and LDL cholesterol in people with high cholesterol. Some studies also suggest increases in HDL cholesterol. More information on long-term safety and effectiveness is needed.

 A


Monacolins, compounds found in red yeast rice extract (RYRE), have been found to have health benefits since the early 1980s. In particular, monacolin K has been marketed as lovastatin and mevinolin. However, due to the large number of compounds that may lower cholesterol other than monacolin K, the cholesterol-lowering mechanism is still unclear. It has been suggested that RYR may block absorption of cholesterol, promote the clearance of cholesterol, or exert antioxidant effects. Overall, results suggest that red yeast rice (RYR) products may lower levels of total and LDL cholesterol in people with high cholesterol. Some studies also suggest increases in HDL cholesterol. More information on long-term safety and effectiveness is needed.

 A


Human studies suggest that RYR use may improve blood flow through widened vessels and reduced inflammation. However, further research is needed in order to determine the effect of RYR on heart disease symptoms and mortality.

 C


Human studies suggest that RYR use may improve blood flow through widened vessels and reduced inflammation. However, further research is needed in order to determine the effect of RYR on heart disease symptoms and mortality.

 C


Although it has not been well studied in humans, RYR has been found to reduce blood sugar and increase insulin in animal research. Early human studies also suggest that RYR may have benefits in diabetes. Further research is needed before firm conclusions can be made.

 C


Although it has not been well studied in humans, RYR has been found to reduce blood sugar and increase insulin in animal research. Early human studies also suggest that RYR may have benefits in diabetes. Further research is needed before firm conclusions can be made.

 C


Early evidence suggests that RYR may benefit liver health in people who have diabetes. However, more studies are needed before conclusions can be made.

 C


Early evidence suggests that RYR may benefit liver health in people who have diabetes. However, more studies are needed before conclusions can be made.

 C
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)

Tradition / Theory

The below uses are based on tradition, scientific theories, or limited research. They often have not been thoroughly tested in humans, and safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. There may be other proposed uses that are not listed below.

Dosing

Adults (18 years and older)
Red yeast rice (RYR) should be taken with food. A dose of 1,200 milligrams of red yeast powder in the form of capsules has been taken by mouth twice daily with food. In Asia, the average consumption of naturally occurring RYR is 14-55 grams daily.
To treat coronary heart disease, 1,200-2,400 milligrams of Xuezhikang has been taken by mouth daily for 2-12 weeks. Xuezhikang has also been taken by mouth at doses of 0.3-0.6 grams twice daily for 4-4.5 years on average (range: 0.5-7 years). Xuezhikang has been taken by mouth at a dose of 1,200 milligrams daily for 12 weeks to 24 months.
To treat diabetes, two capsules of 300 milligrams of Monascus extract have been taken by mouth for eight weeks.
To treat high cholesterol, 1,200-2,400 milligrams of Cholestin? has been taken by mouth 1-2 times daily for up to 12 weeks. Doses of 600-1,800 milligrams RYR have been taken by mouth up to three times daily for 8-24 weeks. Two capsules of 300 milligrams of RYR product have been taken by mouth daily for 1-3 cycles of eight weeks each. Doses of 600-3,600 milligrams of Xuezhikang/RYR have been taken by mouth 1-2 times daily for up to one year. A dose of 2-4 capsules of Xuezhikang has been taken by mouth twice daily for 8-12 weeks. A dose of five capsules of 0.5 grams of Xuezhikang has been taken by mouth twice daily for two months. Doses of 0.6-3.6 grams of RYR extract have been taken by mouth daily for four weeks to 4.5 years. Doses of 0.6-1.2 grams of Monascus purpureus rice preparation have been taken by mouth 1-2 times daily for eight weeks to one year, with dose adjustment depending on cholesterol levels and tolerance. Five Zhitai capsules have been taken by mouth twice daily (for a dose of five grams daily) for two months. Three Zhibituo tablets (0.35 grams each) have been taken by mouth three times daily for a total of 3.15 grams daily. One to two capsules of Xuezhikang have been taken by mouth 2-3 times daily for up to 24 weeks. Four capsules of RYR (HypoCol?, Wearnes Biotech & Medicals Pte, Singapore) have been taken by mouth daily for 16 weeks.
To treat fatty liver, 0.6 grams of RYR have been taken by mouth twice daily for 12 weeks.

Safety

The U.S. Food and Drug Administration does not strictly regulate herbs and supplements. There is no guarantee of strength, purity or safety of products, and effects may vary. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy. Consult a healthcare provider immediately if you experience side effects.

Interactions

Interactions with Drugs
Red yeast rice (RYR) may increase the risk of bleeding when taken with drugs that increase the risk of bleeding. Some examples include aspirin, anticoagulants (blood thinners) such as warfarin (Coumadin?) or heparin, antiplatelet drugs such as clopidogrel (Plavix?), and nonsteroidal anti-inflammatory drugs such as ibuprofen (Motrin?, Advil?) or naproxen (Naprosyn?, Aleve?).
RYR may affect blood sugar levels. Caution is advised when using medications that may also affect blood sugar. People taking drugs for diabetes by mouth or insulin should be monitored closely by a qualified healthcare professional, including a pharmacist. Medication adjustments may be necessary.
RYR may cause low blood pressure. Caution is advised in people taking drugs that lower blood pressure.
RYR may interfere with the way the body processes certain drugs using the liver's cytochrome P450 enzyme system. As a result, the levels of these drugs may be increased in the blood and may cause increased effects or potentially serious adverse reactions. People using any medications should check the package insert and speak with a qualified healthcare professional, including a pharmacist, about possible interactions.
RYR may also interact with agents that may affect the immune system, agents that may affect the nervous system, agents that may harm the liver, agents that may increase the risk of muscle fiber breakdown, agents that may treat heart disorders, agents that may treat retrovirus infections (HIV), alcohol, antibiotics, anticancer agents, antifungals, anti-inflammatory agents, antiobesity agents, cardiac glycosides, cholesterol-lowering agents, cyclosporine, digoxin, fibric acid derivatives, levothyroxine, macrolides, protease inhibitors, ranitidine, skin agents, statins, stomach agents, and thyroid hormones.

Attribution

This information is based on a systematic review of scientific literature edited and peer-reviewed by contributors to the Natural Standard Research Collaboration (www.naturalstandard.com).

Bibliography

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