This is a download of my research on Berberine today.
Berberine (main active ingredient in coptis and Nexrutine) is undergoing extensive research for cancer with positive results in everything, reminiscent of resveratrol, but research in vivo is very limited. Like RESV, it is metabolized quickly, but unlike resveratrol, most of it's metabolites appear to be active, and it is metabolized in rats as well as humans so animal studies are more applicable. In vivo research indicates oral dosing will have anti-cancer effects. Its researched for cancer (300 pubmed results), reducing blood glucose (79), depression (22), cholesterol (55), and arthritis (12). It is in a lot of herbs.
Berberine is the main non-toxic plant alkaloid in European Elderberry, goldenseal, Amur cork tree bark (Nexrutine extract), Oregon grape (Berberis aquifolium), Chinese Isatis (Isatis tinctoria), and Coptis chinensis aka Chinese Goldthread (Huang-Lian) extract (chinese herbal medicine 1 of the 50 fundamental herbs). But there are 15 coptis species in China that might be used.
Human lung cancer in mice:
http://www.ncbi.nlm....pubmed/21061266
at 0.05% of their diet apparently based on the volume of the food. If you eat 1 kg per day, that's 500 mg. That would be 3 pills/day costing $1/day, $365 per year.
http://www.iherb.com...lets/20873?at=0
2011 research papers:
http://www.ncbi.nlm....pubmed/21496227 cervical
http://www.ncbi.nlm....pubmed/21613449 prostate
http://www.ncbi.nlm....pubmed/21527846 melanoma
http://www.ncbi.nlm....pubmed/21545798 bladder
http://www.ncbi.nlm....pubmed/21443647 liver
http://www.ncbi.nlm....pubmed/21175812 colon
http://www.ncbi.nlm....pubmed/21246838 colon
http://www.ncbi.nlm....pubmed/21196313 skin
http://www.ncbi.nlm....pubmed/21170508 kidney
berberine with 15% oleic acid, 17% tween80 and 17% PEG400 with 50% water gave 6.5 times better delivery.
http://www.ncbi.nlm....pubmed/18717486
It was reported that extending the alkyl chain at position 8 or 13 of the berberine molecule [8- or 13-hexyl-substituted derivatives] strongly improved the cytotoxic activity of berberine [due to better ability to dissolve in fats] 2001 article: http://pubs.acs.org/....1021/np000554f
Nexrutine is the pre-2001 trade name of a bark extract of the cork tree that contains berberine. It's used in arthritis.
600 mg per kg of diet for mice with prostate cancer brought had huge effect
http://clincancerres...9/2784.full.pdf
also against established prostate tumors, 600 mg per kg diet:
http://ar.iiarjourna.../3/857.full.pdf
Bioavailability details for here to bottom
A Harvard author:
"30% to 45 % growth inhibition of S180 tumor by the oral doses of 25uM and 75uM/kg on mouse, compared with 93% in the in vitro study, indicating that the oral absorption of berberine is poor" "animal tests showed that the blood concentration was 100ug /ml, 30 minutes after an oral dose of 400mg. The T1/2 in the stomach was 194 minutes." "The result from clinical test demonstrated that the mean maximum plasma concentration (Cmax) in twenty volunteers was about 0.3 to 0.4 ng /ml after a 300 to 400 mg oral dose of berberine" He speculates that coptis may have absorption benefits. He claimed Ber has low absorption, but one of his references and subsequent wor shows it is just metabolized quickly in rats and humans.
only 0.4 ug/mL as berberine in humans after dosing:
http://www.ncbi.nlm....pubmed/21671182
These findings suggest that berberine undergoes similar biotransformation in rats and humans. Possible metabolic pathways of berberine in rats and humans are proposed. ... Most of the final metabolites were sulfate or glucuronide conjugates. These metabolites are very polar and are easily excreted. ... This study demonstrated that the absorbed berberine is easily metabolized in vivo and its extensive biotransformation may be one of the main reasons for its low oral bioavailability. ...we also investigated the urinary metabolites of berberine after intraperitoneal injection and obtained the same metabolites as those after oral administration, implying that the metabolites of berberine are formed after absorption rather than in gastrointestinal tract....clinical application for treatment of diabetes mellitus (Ni, 1988), hyperlipemia (Kong et al., 2004), arrhythmia, and heart failure (Zeng and Zeng, 1999; Lau et al., 2001; Zeng et al., 2003). [which shows the metabolites are active] Several reports have shown that a high concentration is necessary for berberine to display its in vitro bioactivities (Kong et al., 2004; Yin et al., 2008; Piyanuch et al., 2007). However, the blood-berberine concentration in animals or humans was very low when it was given orally in experimental or clinical doses (Shen et al., 1993; Yu et al., 2000), suggesting that the berberine metabolites might be responsible for the pharmacological effects.
http://dmd.aspetjour...36/11/2159.long
"4 major metabolites of BBR, berberrubine (M1), thalifendine (M2), demethyleneberberine (M3) and jatrorrhizine (M4) were identified in rat’s livers....BBR's metabolites remained to be active on BBR's targets (InsR, LDLR, and AMPK) but with reduced potency."
http://www.ncbi.nlm....9-5876-9-62.pdf
M4 jatrorrhizine is used for a lot of medicinal purposes including noncompetitively inhibiting monoamine oxidase, decreases multidrug resistance in cancer cells, and reduces blood sugar by increased aerobic glycolysis (berberine is used in diabetics).
"Three protoberberine alkaloids, berberine chloride, berberrubine chloride and thalifendine chloride were isolated from the roots of Fibraurea chloroleuca Miers, and found to show significant cytotoxic activity with one or more human cancer cell-lines and cultured P-388 cells."
http://onlinelibrary...070406/abstract
