X-Message-Number: 8286 From: Brian Rowley <> Subject: Life Extension Supplements: Screens on Lower Organisms Date: Thu, 5 Jun 1997 22:40:27 -0700 What follows are arguments in favor of screening life extension supplements on lower organisms (e.g., fruit flies, rotifers and nematodes), and ideas for carrying out such screens. MORTALITY STUDY SHORTAGE There are countless drugs which *might* delay mortality, but which no one has tested for mortality effects. Doug Skrecky dug up all Medline-accessible fruit fly mortality studies where anti-aging drugs were screened since 1966 and the result was a pile no taller than an inch. The rodent mortality study literature is equally scant. The fact is, not many scientists want to bother with mortality studies because they (a) take a long time and are therefore slow to publish (b) are expensive and (c) are about aging (criticism and cynicism about life extension). Most drug companies are similarly not interested in mortality studies, although they test their drugs for long term toxicity. We're at a stage where the chemists and molecular biologists have grossly outstripped the gerontologists. We've got an array of exciting drugs and hormones to test which might extend the life span, but few pharmacologists who will test them. Take DHEA and even many vitamins, for example--much excitement, no reliable mortality data (however Richard Weindruch at the Univ. of Wisconsin at Madison is now doing a proper DHEA mortality study). MULTI-DOSE TRIALS What mortality data exists is almost entirely from one-dose experiments. For example, melatonin mortality studies I've seen test only one dose of melatonin. My training in pharmacology (an MS) has led me to believe that many doses should be tried in drug trials. One wants to know (1) what is the maximum achievable effect of the drug (efficacy), (2) how much of the drug do you have to take for an effect (potency) and (3) how much of the drug is too much (toxicity). Only multiple dose screens give you this information. Another reason to test multiple drug concentrations is that drugs bind to totally different receptors (and have totally different effects) at different doses. At low doses, vasopressin is a brain peptide that influences cognition. At higher doses, it is a brain peptide influencing cognition that also acts as an anti-diuretic hormone. At even higher doses, its action as a brain peptide changes, it has an anti-diuretic effect and now also raises the blood pressure. A one-dose drug trial for vasopressin, as for all other drugs, would be virtually meaningless. One answer is to test anti-aging drugs on lower organisms, which would allow more drugs to be tested at more dose levels, faster, cheaper and with greater sample sizes. COMBINATIONS OF ANTI-AGING DRUGS Multi-dose screens for life extension drugs are rare enough. Rarer still are *combination* drug screens, which would reveal synergistic effects between different agents. If the process of aging is multifactorial, a series of interventions might be necessary. The ultimate aim is to develop an optimized "cocktail" of agents, each ingredient acting synergistically. If 5 mg of drug A increases life span by 10%, and 5 mg of drug B increases life span by 10%, by how much will 5 mg of *both* drugs increase life span? Possibly by more than 10%, unless the drugs have bad interactions or work by the same mechanism. Of course, before testing drugs in combination, one first needs to establish that both agents have an effect, and the dosages needed for optimal effect should first be determined. SCREENING LIFE EXTENSION SUPPLEMENTS ON LOWER ORGANISMS Can the use of lower organisms (e.g., fruit flies) be justified? After all, the goal is to slow mammalian aging, not fruit fly aging. Fruit flies don't die of the same causes as humans, just as paramecia don't die of the same causes as fruit flies. Nonetheless, even these 3 seemingly unrelated species are related metabolically; fruit flies, humans and paramecia share a number of key enzymes, including cytochrome c and other respiratory chain enzymes, ATP synthetase enzymes, superoxide dismutase (SOD)... In fact, fruit flies, humans and paramecia share basic longevity assurance mechanisms: all have antioxidant defense enzymes, DNA repair enzymes... Fruit flies and lower organisms have similarities to mammals at the metabolic, if not gross level, so there is some theoretical justification in screening anti-aging drugs on lower organisms. There is also empirical justification: treatments which delay mortality in lower animals often delay mortality in higher animals. For example, melatonin delays mortality in rotifers, as well as mice. Mice are mammals while rotifers are microorganisms not even made up of separate cells (they're just teensy columns of polynucleated protoplasm). Do rotifers die of the same causes as mice? Apparently not, as mice die of cancer, kidney disease, vascular disease... none of which affect rotifers. Yet the effect of melatonin on rotifer mortality successfully predicts a similar effect in mice. If a scientist tested melatonin on rotifers as a preliminary screen for a subsequent mouse trial, he would not be misled by the result. Another example: Caloric restriction delays mortality in paramecia, rotifers, daphnia (a fresh-water shellfish 2-3 millimeters long), spiders, fish, mice, rats, and (I think) guinea pigs. Yet it cannot be said that paramecia, rotifers, daphnia or spiders die from the same causes as rats. At least, not if one defines cause of death anthropocentrically using end-stage outcome terms like "heart attack, cancer, stroke...", instead of a more general phrase like, "progressive malfunction of life maintenance processes common to all species leading to weakening at the molecular level which increases susceptibility to a variety of stochastic disease processes". The effect of caloric restriction on the mortality of paramecia, rotifers, daphnia and spiders predicts a similar effect on mouse mortality--that's evidence in favor of using lower organisms as screens for anti-aging treatments, and also suggests some commonalities of aging mechanisms across phylogenies. There are exceptions: caloric restriction does not delay mortality in amoeba or fruit flies, so it only works on 8/10 of the species I know about. Still, what delays mortality in a lower organism delays mortality in a mammal often enough to justify using lower organisms as screens, and often enough to propose the existence of common mechanisms of aging that span phylogenies. The accuracy of lower organismal data, in terms of predictive power for longevity effects in rodents, surely goes up the more species of lower organism you use to do screens. For example, if an anti-aging supplement extends the life span of rotifers I would be interested. However, if the same supplement could be shown to also extend the life span of nematodes and fruit flies, I would be very, very interested. In fact, I would want to try it out on long-lived strains of mice as a fair bet. I've dreamt of creating an "invention factory" for life extension drugs, where supplements are screened at multiple doses with high sample sizes, first alone and then in (hopefully synergistic) combinations. Such rigorous, exhaustive screens would be possible using lower organisms; mortality data from rotifers is obtainable within a week, data from nematodes is obtainable within a month, data from fruit flies is obtainable within 2 months... the winning drug combinations, effective in more than one lower organism, could then be tested on long-lived strains of rodents. Soon I will post an outline of Materials and Procedures for some supplement screens I'll be doing this summer, during which time I will test 5-6 dose doublings of pikamilone (nicotinoyl-GABA), melatonin, centrophenoxine and other supplements in search of anti-aging effects. I owe many thanks to Doug Skrecky whose idea it was to do fruit fly screens in general, and whose experience and impeccable reading of the literature have given me some great insights. I also give big thanks to Dr. Robert Ettinger, who has agreed to fund the research. Brian Rowley P.S. Stephen Spindler's lab (where I will be doing my Ph.D. starting this September) is also testing supplements for anti-aging effects, probably including in vitro work. Life doesn't get much more exciting than this for a life extension fanatic :-> Rate This Message: http://www.cryonet.org/cgi-bin/rate.cgi?msg=8286