An email message from Ray Saarela to the AMALGAM email list (see directions for access).

By international law Ray holds copright on his text, as of the date he sent the email. In an attempt to make it more readable, I've occasionally inserted comments [like this] or modified the format. Otherwise I've tried to avoid editing, but there's plenty of possibility that I have miscopied or misrepresented his original messages. If you spot problems, please

Ray frequently quoted in full the abstracts of the research he cited, but he also indicated he'd built (and studied) a library full of complete papers. I have omitted the abstracts, relying on you to go read them at PubMed.

Message-ID: <005701bfed4a$7e932ac0$b6cf30d0@->
Date: Thu, 13 Jul 2000 21:17:52 -0700
Subject: Re: YOU GOTTA SEE THIS ON LIPOIC ACID AND HEAVY METALS ETC.

LA facts:

Chemically, The LA people usually refer to is racemic mixture of R and S Alpha-Lipoic acids = +-1,2-Dithiolane-3-pentanoic acid.

R(+) isomer only exists naturally , and is beneficial in moderate doses as energy metabolism enchancer, and as antioxidant, but LA as disulfide does not chelate, and is ineffective as chelator/monotherapy.

The S(-) isomer in the racemic mixtures has been demonstrated inhibitory therefore harmful to some mtabolic processes, taking place of the effective LA, all LA sold contains ~ 50 % of the wrong = S-isomer.

The only naturally existing isomer, R, has 2 main functions in human body ( S isomer is inhibitory and therefore sometimes harmful )

1. AcetylCoASh metabolism cofactor together with cofactor form of Thiamin ( also called B1 vitamin ). Both help in diebetic neuropathy by assisting glucose metabolism ( but not by chelating anything ). This is the energy metabolism effect, additionally, these together help to make NADH from
2. Lipid soluble antioxidant similar to E-vitamin, which is helpful in many situations, however, with Fe3+ reduced LA form can be contributory to increase -OH radical formation. Vitamin C also has pro-radical function with Iron and Copper, so those high in iron and/or copper may want to be conservative with ascorbate and LA.

Reduced LA = DHLA promotes Free Radicals by reducing iron in form of Fe3+ to Fe2+, impairs organic mercury, cadmium and copper detox, depletes liver glutathoine conjugation function, impairs kidney glycinate pathway, in addition to being ineffecient heavy metal chelator, references:

Taking LA every so often will improve energy metabolism of AcetylCoASH just like taking thiamin every so often, taking LA every so often will.

Overall, disulfide Alpha-LA is ineffective as chelator, as it does not chelate, and DMSA is superior in chelating mercury, lead and chelating the bra

It is useful along with thiamin to boost energy metabolism, and as aid for E-vitamin as antioxidant, but not a good chelator, unfortunately, even glutathione is more effective.

References: [followed by more comments of Ray's] - LA is not always safe and cool, and ... it is not effective treating heavy metal poisonings ( but helps with those low in antioxidants and those with glucose metabolism trouble )

1. Effect of lipoic acid on biliary excretion of glutathione and metals.
   (Gregus Z; Stein AF; Varga F; Klaassen CD)
2. Lipoic acid impairs glycine conjugation of benzoic acid and renal excretion of benzoylglycine.
   (Gregus Z; Fekete T; Halászi E; Klaassen CD)
   • Can make all glycination pathway chemicals backfire on LA takers ....
3. Lipoic and dihydrolipoic acids as antioxidants. A critical evaluation.
   (Scott BC; Aruoma OI; Evans PJ; ONeill C; Van der Vliet A; Cross CE; Tritschler H; Halliwell B)
   • Reduced (the chelator that A-LA reduces in body partially to) LA = DHLA produces-OH radicals with iron
4. Antioxidant role of alpha-lipoic acid in lead toxicity.
   (Gurer H; Ozgunes H; Oztezcan S; Ercal N)
   • LA ineffective as chelator monotherapy in heavy metal poisoning ( Note, DMSA superior as chelator )
5. Amyotrophic lateral sclerosis and metallic toxins
   Currier RD, Haerer AF
   • [PubMed indicates "no abstract available]
   • Another reference demonstrating LA ineffective in heavy metal poisoning
   • ( In brief, in the ref., ALL 3 LA treated cases failed to demonstrate ANY improvements whatsoever ( the same with EDTA the only less effective "chelator" than LA for mercury ...)
6. Utilization of renal slices to evaluate the efficacy of chelating agents for removing mercury from the kidney.
   (Keith RL; Setiarahardjo I; Fernando Q; Aposhian HV; Gandolfi AJ)
   • This reference also demonstrates the same, as 4. that LA is 2nd least effective as chelator, only EDTA is poorer chelator fo
7. Interaction of alpha-lipoic acid enantiomers and homologues with the enzyme components of the mammalian pyruvate dehydrogenase complex.
   (Löffelhardt S; Bonaventura C; Locher M; Borbe HO; Bisswanger H)
   • This additional reference shows that the commercial LA on average 50 % contained ingredient S-enantiomer is overall, inhibitory of the pyryvate dehydrogenase metabolism, while the R-one is more activating, so taking the commercial LA can have sometimes, energy inhibiting effects instead of improving effects due to the unnatural S-enantiomer, as no pure natural R-enantiomer provenly containing products are for sale in health food stores. Ie, the usefullness of 50 -50 R-S LA may be down to zero, for diabetic patient, while a product that may contain more S than R may be actually harmful even for this only function it is really useful, while most all thiamin products are free from this wrong enantiomer issue. Benfotiamin has been proven to produce very similar, but stronger benefits in diabetic and alcoholic neuropathies over LA, and it is also similary pyruvate dehydroganase/acetylCoASH metabolism cofactor like LA is.
   • Taking LA in giant doses ( like some booklets suggest unsafely ) will lead to nutritional imbalance of the glucose/citric acid cycle pathways, and can eventually lead to nutritional deficiencies and backfires that happen when one gets depleted of the other AcetylCoASH/Pyruvate metabolism cofactors by the unwise single/monotherapy with LA.

Sadly, there are incompetent authors out there, that suggest unsafe LA monotherapies with every 3-4 hour LA, and even unsafer combo-therapies with LA+DMPS therapies.

Regards, Ray S.

For more information

• Back to the Canary's-Eye Veiw Lipoic Acid page
• More by Ray Saarela:
  • LA as a chelator - Ray's first message on the subject (assuming I've searched correctly), 3 April 1998.
  • LA poisons the brain - 6 March 2000
• To join the AMALGAM list and read the archives for yourself, see directions for access).