Ephedra Alternative in Weight Management

By Yousry Naguib, Ph,D
VR (August/September 2003)

Overweight is the number one nutritional problem in the United States. Statistics show that about half of the adult population in the U.S. is overweight (body mass index, BMI 25­ to 30 kg/m2), and 16 percent are obese (BMI is greater than 30) (1).
Although the number of people dieting continues to increase, the rate of obesity also continues to increase. It is not surprising that so many people are searching for the "magic bullet" that will allow them to lose weight quickly and effortlessly. Few weight loss supplements are clinically tested for effi­cacy, yet their proliferation continues.
Being overweight significantly increases a person's risk of developing diabetes, heart disease, stroke, and other diseases that cause morbidity, mortality and high health-care expenditure.
According to the Centers for Disease Control & Prevention, overweight and physical inactivity account for more than 300,000 premature deaths each year in the United States, second only to tobacco-related deaths. This underscores the need for therapeutic strategies to stem this growing epidemic.
The cause of obesity is simply that more calories are consumed than the body burns, and the excess calories are stored as fat tissue. Effective methods for weight reduction are constantly being sought. No one approach, wehether dietetic management, or commercial weight loss program can alone solve the obesity problem.
To determine what it takes to maintain weight loss, a study involving 784 par­ticipants found that participants who lost an average of 66 lbs. and kept off at least 30 lbs. for an average of 5.5 years, expend an average of 2,800 calories per week through physical exercise and eat less than 1,400-1,500 calories daily (2).
Environmental factors include food intake and degree of physical activity. Overeating relative to energy needs is a component of obesity development. An important benefit of exercise during weight loss is that it preserves fat-free mass and allows fat loss that is equiva­lent to or greater than weight loss (3).
As a source of energy, fat provides most of the energy needed. Fat produces more energy (9 kilo calories per gram fat) than carbohydrate (4 kilo calories per gram) or protein (4 kilo calories per gram). The average women weighing 60 kg and 20 percent body fat has stored about one month of energy as fat (4).

ADIPOSE TISSUE
Adipose tissue is specialized connec­tive tissue which functions as the major storage site for fat in the form of triglyc­erides. Adipose tissue is found in two different forms: white adipose tissue (WAT) and brown adipose tissue (BAT). Most adipose tissue is WAT. WAT serves three functions: heat insulation, mechan­ical cushion, and source of energy. Sub­cutaneous adipose tissue, found directly below the skin, acts as a heat insulator in the body.
BAT, which derives its color from rich vascularization and densely packed mitochondria, is found in various loca­tions in the body. The fat in BAT releases energy as heat, which is used in heat production in non-shivering ther­mogenesis and the utilization of excess caloric intake via diet-induced-thermo­genesis.

THERMOGENESIS
Thermogenesis means heat (thermo) creation (genesis), which refers to non-shivering heat production due to meta­bolic energy transformation by processes that do not involve contractions of skele­tal muscles. While all organs contribute to non-shivering thermogenesis accord­ing to their rates of resting metabolism, the principle organ responsible for the activation of thermogenesis is the BAT. During thermogenesis, free fatty acids are oxidized (burned) without producing ATP (adenosine triphosphate)–the energy from the oxidation process is dis­sipated (as heat) into the surrounding tis­sues. Thus, it is considered a metaboli­cally inefficient process.
Thermogenic substances, to increase metabolism and accelerate calorie expenditures, include ephedra, guarana, Citrus aurantium, green tee extract, and white willow bark.
Dietary supplements containing the herbal stimulant ephedra (ma huang) have been widely promoted for weight loss and energy enhancement. However, ephedra has been linked to some health problems, including strokes, heart attacks and seizures.
Ephedra should not be used by anyone with a history of diabetes, heart disease, or thyroid problems. It is not recom­mended for long-term use. The Following is a discussion of possible alternatives.

CITRUS AURANTIUM
Citrus aurantium, also known as bitter orange or Zhi Shi, has been used for thousands of years in traditional Chinese medicine. Citrus aurantium contains five adrenergic (resembling epinephrine) amines: synephrine, octopamine, horde-nine, tyramine and N-methyl tyramine. Citrus aurantium can help burn fat, build lean muscle mass and increase physical performance without the side effects of ephedra.
Synephrine and octopamine are spe­cific beta-3 agonists meaning they stim­ulate cells to break down fat, in a process called lipolysis. Ingestion of 8

 oz. of juice from citrus aurantium con­taining m-synephrine (57 meg per ml) by healthy subjects with normal blood pressure was shown to be safe and had no significant effect on heart rate and blood pressure. The study suggested that individuals with severe hypertension, and people taking monoamine oxidase inhibitors and decongestion medications should refrain from citrus aurantium (6).

HYDROXYCITRIC ACID
Hydroxycitric acid is a popular dietary supplement purported to be energy enhancing and fat burning. Hydroxyc­itric acid is an active ingredient that is extracted from the South Asian fruit Garcinia cambogia, which is about the size of an orange and looks similar to a small pumpkin. It reportedly promotes weight loss, in part, through suppression of appetite (7).
Animal studies indicated that hydroxyc­itric acid suppresses the fatty acid synthe­sis, lipogensis, food intake, and induced weight loss. However, few clinical studies have shown controversial findings.
Hydroxycitric acid is a potent inhibitor of the enzyme citrate lyase. The conver­sion of carbohydrates into fat requires an enzyme called ATP-citrate lyase. ATP is a nucleotide present in all living cells, which serves as an energy source for many metabolic processes and is required for ribonucleic acid synthesis. The enzyme catalyzes the cleavage of citrate into acetyl coenzyme A, which is responsible for cholesterol and fatty acid synthesis de novo. Prevention of convert­ing excess calories into fat in turn slows the production of cholesterol and triglyc­erides. At the same time, the liver is able to synthesize more glycogen, amplifying the satiety signal to the brain and sup­pressing appetite and food carvings.
The efficacy of hydroxycitric acid in weight loss management was demon­strated in a double blind, placebo-con­trolled study involving 89 mildly over­weight females, who were randomly, assigned to either a placebo or 400 mg caplets of Garcinia cambogia 30-60 min­utes prior to meals for a total dose of 1.2
hydroxycitric acid per day. Over 12 weeks, both groups lost body weight with the active group achieving a significantly greater reduction (3.7 kg versus 2.4 kg) (8).
A recent study published in JAMA­Journal of the American Associtaion examined the efficacy of Garcinia cam­bogia for body weight and fat mass loss in overweight human subjects. In this double-blind, placebo-controlled trial, 135 overweight men and women subjects were randomly assigned to receive either 1,500 mg of hydroxycitric acid per clay or placebo, along with a high fiber diet, for 12 weeks. Hydroxycitric was taken 30 minutes before meals three times per day. Both groups lost a significant amount of weight, 9 and 7 lbs. for the placebo and hydroxycitric acid groups, respectively. The study concluded that Garcinia cambogia failed to produce sig­nificant weight loss and fat mass loss beyond that observed with placebo (9).
Opponents have postulated that the high-fiber diet used in the study may have limited the gastrointestinal absorp­tion of hydroxycitric acid, thus rendering the study ineffective and leading to the disappointing results (10).

CHROMIUM SUPPLEMENTS
Chromium is an essential nutrient required for maintaining of proper sugar and fat metabolism. Chromium is pre­sent throughout our body, with the high­est concentration being in the liver, kid­ney, spleen, bone, brain and muscle.
Chromium is poorly absorbed, only 2 to 10 percent of dietary intake being absorbed. Organic chromium, such as chromium picolinate (Chromax manu­factured by Nutrition 21), and niacin-bound chromium (ChromeMate made by InterHealth) are absorbed more effi­ciently than inorganic chromium such as chromium chloride.
Researchers at the University of Texas, Austin showed that young obese women taking 600 mcg of chromium (as niacin bound chromium) daily for two months. with a moderate diet and exer­cise regimen, saw significant weight loss and lowered insulin response to an oral glucose load. Chromium supplementa­tion amplifies insulin receptor tyrosine kinase activity, which explains the rela­tionship between chromium and its effects in diabetes (11).

GUARANA
Guarana, obtained from the dried seeds of the Amazonian Paullinia cupana, is rich in caffeine and is used in Brazil for the production of stimulants, soft drinks, and sweets. In a recent clini­cal study published in the Journal of Human Nutrition and Dietetics, a herbal preparation containing yerba mate (leaves of Ilex paraguayenis), guarana and damiana (leaves of Turnera diffusa var. aphrodisiaca) was shown to signifi­cantly delay gastric emptying, reduce the time to perceived gastric fullness and induce weight loss over 45 days in over­weight patients. The herbal preparation resulted in more weight reduction (5kg) than placebo (0.3kg) over 45 days (12).

GREEN TEA EXTRACT
Green tea (Camellia sinensis) is a potent source of antioxidants; sipping green tea regularly may help to prevent various types of diseases, and may help heal gum infections. Because green tea contains astringent tannin compounds, it may ease indigestion and upset stomachs.
A 1999 small study reported in the American Journal of Clinical Nutrition reported increased energy expenditure and fat oxidation in men who took a green tea extract as opposed to a placebo or caffeine alone (13).

WHITE WILLOW BARK
The bark of the willow tree (Salix alba) has been used in China for cen­turies to alleviate pain and fever. The active ingredient in white willow is salicin, converted into salicylic acid in the body. The first aspirin (acetylsali­cylic acid) was made from a salicin herb. Willow bark is said to have thermogenic properties and can boost metabolism.

CARNITINE
Carnitine is essential for a variety of important physiological functions in energy metabolism. It shuttles fatty acids to the mitochondria (the "powerhouse" of the cell where energy is produced) to undergo oxidation, and produce energy. Carnitine is a short-chain nitrogen con­taining carboxylic acid and is not an amino acid.
Carnitine is found in meat and dairy foods. and a well balanced diet provides significant amounts of carnitine as well as the essential nutrients needed for its biosynthesis, which include the amino acids 1-lysine and methionine, vitamin C. and iron.
In a recent pilot study, joint administra­tion of pyruvate, hydroxycitrate and Car­nitine to obese subjects was associated with body-fat loss (14). In another double-blind trial, 36 moderately overweight pre-menopausal women were instructed to ingest either 2 g of carnitine or the same amount of lactose twice daily for eight weeks. All subjects walked 30 min­utes for four days a week. No significant difference in body composition (total body mass, fat mass) between the carni­tine and control groups was observed, thereby casting doubt on the efficacy of carnitine in weight loss (15).

CHITOSAN
Chitosan is a non-digestible fiber derived from the shells of crabs, lobsters, and other crustaceans. Chitosan-based supplements are sold as fat trappers. They purportedly block fat absorption and cause weight loss without food restriction. In a recent study 15 subjects consumed two capsules five times per day (4.5g chitosan/day), 30 minutes before each meal for four days. Their feces were analyzed for fat content. Chi­tosan supplementation increased fecal fat excretion by 1g/day, to 7g/day. These results indicate that the effect of chitosan on fat absorption is not significant (16).
In another study, 50 obese women (22­59 years, BMI greater than 30) received two tablets (750 mg chitosan pr tablet) three times daily before each main meal for six months. Low caloric diet and physical activity were recommended. At the end of the study, significantly higher weight loss was noted in the chitosan­supplemented group (15.9 kg) than in the placebo group (10.9 kg). The study con­cluded that chitosan is safe and can be used in the treatment of obesity (17).
Chitosan may block the absorption of fat-soluble nutrients such as vitamins A, E. D. and K. So, it is recommended to take a vitamin supplement at least an hour or so before the chitosan. People allergic to shellfish should not take chitosan.

CONJUGATED LINOLEIC ACID
Conjugated linoleic acid (CLAi is a collective name for a mixture of several isomers (or chemical forms) of octadeca­dienoic acid in which the two double bonds are conjugated. CLA is the main omega-6 polyunsaturated fatty acid in the diet: and it is found in grass-fed beef and lamb, dairy products, and most vegetable oils, such as sunflower, safflower, and flaxseed oils. The most commonly isomer of CLA found in the diet is cis-9 / trans-(1. CLA contents of dairy products range from 3 to 9 mg per gram fat, of which the cis-9 / trans-11 CLA isomer makes up 70 to 90 percent of the total CLA.
A recent randomized double-blind, placebo-controlled study on 20 healthy exercising humans of normal body weight showed that the body fat of sub­jects who took 600 mg CLA three times daily for 12 weeks was significantly reduced, as compared to the placebo-group (18).
CLA has also been shown to reduce body fat mass (BFM) in humans in a dose dependence manner. In a random­ized double blind study, 60 overweight or obese volunteers were divided into five groups receiving either placebo (9 g olive oil), or CLA in doses of 1.7, 3.4, 5.1, or 6.8 g per day for 12 weeks. The CLA group showed a significant reduc­tion in BFM as compared to the placebo. The study indicates that 3.4 g of CLA per day is enough to reduce BFM (19).
Researchers at Uppsala University in Sweden reported similar findings. Fifty-three healthy men and women, ages 23 to 63, were randomly assigned to supple­mentation with CLA (4.2g/day) or olive oil for 12 weeks. Body fat was decreased by 7.8 percent in CLA-group, but not in the control-group. No change in body weight was observed in either group (20).

LOW-CARBOHYDRATE DIET
High-protein, low-carbohydrate diets claim to promote weight loss and improve blood glucose control. The advantage of this diet is its low calories which results in weight loss. With a high-protein intake and strict limitation of carbohydrates, water stored with glycogen (carbohydrate) is released. This rapid loss of fluid is an initial boon to dieters looking for fast results.
It is claimed that protein stimulates the release of glucagon. a hormone that raises the level of blood glucose and counteracts the action of insulin. No long-term research is available to docu­ment that high-protein, low-carbohy­drate diets maintain weight loss (21).
The major concern with the high-pro­tein, low-carbohydrate diets is that nutri­ents (such as vitamins A, B-6, and E, thi­amin, folate, calcium, magnesium, potas­sium, and dietary fiber) found in grains, fruits, vegetables, milk, and other carbo­hydrate-containing foods are eliminated.

5-HYDROXYTRYPTOPHAN
The amino acid 5-hydroxytryptophan, or 5-HTP, extracted from the seeds of the Griffonia simplicifolia plant, is thought to increase serotonin levels in the brain. Serotonin is a neurotransmitter that regu­lates mood and thus can be linked to mood-related eating behaviors. Individu­als should consult with their healthcare professional before taking 5-HIP. as the amino acid may interact with other med­ications and can have potentially serious side effects.

LAGERSTROEMIA SPECIOSA
Lagerstroemia speciosa, commonly known as Crepe Myrtle, grows widely in the Philippines, India, Malaysia, and China. It is a popular folk medicine in the Philippines, and a tea made from the leaves has been used for the treatment of diabetes. The leaves contain the bioac­tive compounds corosolic acid and ellag­itannins, which have been shown to pos­sess anti-diabetic activity. Extracts from the leaves of the plant are now commer­cially available.

WHITE KIDNEY BEANS
Phaseolamin, an extract from white kidney beans (Phaseolus vulgaris), is sold as a starch blocker since it has the ability to inhibit the starch-digesting enzyme, alpha amylase.

 

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