Bioavailability of Betulinic Acid, a DIY anti-cancer supplement with an increasing popularity

Introduction

Betulinic acid and its precursor, betulin, are mainly found in the bark of the Betula alba (white birch) tree. The bark can contain up to 35% of betulin. This tree is fast-growing and very common in North America and Europe. The raw bark is readily available in large quantities since it is a waste product in the paper and furniture manufacturing industries. Betulinic acid can also be manufactured easily from betulin in a 2-step semi-synthetic process with a general yield of about 71%.
Betulin and betulinic acid can show up on a supplement-facts or cosmetics label in many disguises:

(3.beta.)-Lup-20(29)-ene-3,28-diol,
18211-63-7,
473-98-3,
AI3-62999,
AIDS-002710,
AIDS002710,
Betulin,
Betuline,
Betulinic alcohol,
Betulinol,
Betulol,
C08618,
C08631,
EINECS 207-475-5,
Lup-20(29)-ene-3,28-diol,
(3beta)-. Lup-20(29)-ene-3beta,28-diol,
Lup-20(30)-ene-3beta,28-diol,
Messagenin,
NSC 4644,
NSC4644,
NSC692218,
Triterpenoid,
Trochol,
ZINC04082884]

Therapeutic background

Betulinic acid was found to have promising therapeutic properties. Investigated so far were its anti-cancer activity (especially for melanoma and skin cancer cells), its anti-inflammatory and anti-malarial effects, its effect on high LDL cholesterol levels and in particular its anti-HIV-1 activity. These observations resulted in the incorporation of betulinic acid in the Rapid Access to Intervention Development (RAID) program of the U.S. National Institute of Health.

Summarizing, betulinic acid is in particular a very promising new chemotherapeutic agent for the treatment of HIV infections and cancer. Because of its potential clinical application for the treatment of cancer and HIV infection, several studies aimed at determining the effect of betulinic acid in mammals have been initiated. As far as we know so far no research has been done investigating the effect of betulinic acid in humans.

So far, the main obstacle for its use is its poor solubility in aqueous solutions (like blood serum and water). Research trying to find a solution for this problem is on-going.

Dietary supplements based on Betulinic Acid

In the meantime, the dietary supplement industry discovered these research results and did not hesitate to try and generate some profit.
Several manufacturers are promoting betulinic acid capsules, tablets and tinctures as a DIY cure against cancer etc. In their descriptions of the properties they place a lot of emphasis on the potential therapeutic power of betulinic acid, but fail to mention the dosage required to achieve that therapeutic effect (in laboratory conditions oral doses of 250 - 500 mg per kilo of bodyweight were used - this means an average person of ~75 kgs should have to consume 38 - 80 capsules @ 500 mg daily) and the fact that betulinic acid is not bioavailable in its pure form due to its extremely poor solubility in aqueous solutions. It will simply pass through your body without leaving much traces. The fact that all research was done using mouse models and petri-dishes is usually also left unmentioned.

Researchers are still studying betulinic acid. Based on in vitro evidence, betulinic acid may decrease human spermatozoa mobility, which can be a serious contra-indication. Further testing is needed to find out whether it is completely safe for humans.

The Chaga mushroom

An interesting, related subject is the Chaga mushroom, a very popular medicinal mushroom that is parasitic to the birch tree and also contains a low percentage of betulinic acid (up to 2%). There are claims that state the Chaga Betulinic Acid has a better bioavailability, but it is unclear why this should be the case. We might dedicate a future article to this.

Conclusion

In the meantime, summarizing, we can only say this: betulinic acid supplements are most likely a waste of money. They will not do any harm nor will they do any good, simply because the bioavailability of BA is very poor and, apart from that, the dosage is way too low to have any effect.Therapeutic effects are unlikely to occur.