Weight Loss, Fat-/Carbohydrate-Uptake Management, Blockers.

CONTROLLING FAT- and
CARBOHYDRATE-UPTAKE

Key words: Weight Loss, Cellulite, Fat-blockers, Enzyme-blockers, Weight Management, Overweight, Cholesterol blocking, Adipose cells, Uptake -control, Polysaccharide /carbohydrate digestion, Fast Food, Glycemic index GI, Ghrelin, Appetite restraining, Phaseolus, Chitosan, Inulin, Guar, Gymnema, Xhoba, Hoodia, Topinambur, Xenical, Insulin-mimic, Lipidplex, Opuntia/Nopal, Meridia, Reductil, Saponification, the "Anti-Obesity Vaccine".

Growing popularity of "fast food" consumption seems to favour over- weight. Why? In a traditional meal a professional cook will compensate "high calorie food" components with low / medium calorie components. And the size of the portions is kept limited.
Fast food is found to hold a combination of high calorie components. This results in more calories per cubic inch or cubic centimeters filling the stomach. Moreover the portions are generous. Research by the British Medical Research Council 94 ), found "the energy density of a typical fast food meal is more than 1½ times higher than an average British meal and 2½ times higher than a traditional African meal".

Worlds lowest income communities as compared to high income (hiI) communities show a low fat consumption (about 10% of total food intake compared to over 40%hiI ) and a higher carbohydrate consumption (75-80% as compared to less than 45%hiI ) please refer to EB 46 ) , Figure 4 "´Dietary energy ... related to´ per capita income".

According to an FAO/WHO report "Carbohydrates in human nutrition" 47 ), an optimum diet should yield at least 55% from carbohydrates.
Some fat components in the human diet are indispensable, omega-6 and omega-3 being the most prominent. Their mutual ratio should be low, like the ratio found in meat from pasture-fed cattle, but dissimilar to the meat from grain-fed cattle 72 ).
Fat contains many calories (joules), and reducing fat storage of individuals with overweight requires much and prolonged effort. The same weight of carbo- hydrate intake has less serious implications for overweight than fat-intake. Therefore "heavyweights" better shift their nutrition pattern from high-fat plus monocarbohydrate (=single, glucose) contents to low-fat plus poly- or oligo-carbohydrate (oligo=few, more than one single) content, 48 ).

It will be clear that fat consumption must be kept moderate and must consist of the right components in the right ratio. However it should never become zero. Humans need some fat; literature states a fair level is 10 grams /day 98 ) the minimum level being 7 grams /day 99 ) . (see also subpage "Some Fat Remains Required" ).

It is easy to reduce the uptake of oligo- and poly-carbohydrates, however hardly practical to prevent uptake of monocarbohydrates, apart from excluding those from the diet as much as possible.

Yet there is a hitch. Large oligosaccharides often consist of a linear chain (amylose) and branched chains (amylopectin). 34 ). These branches may be easily "ripped off" to yield small saccharides. The implication is that two equal-weight big saccharides may differ in one (with the linear chain) being indigestable and the other (a linear chain with branches) being at least partially well digestable. One way to make a mixed chain to loose branches easily is the way the food is prepared. An example is the different contribution to our calorie uptake of rice boiled one minute (medium uptake) and an equal portion boiled six minutes (high uptake).

GLYCEMIC INDEX
A system that enables us to take these different effects of heavy polysac- charides into account is the Glycaemic Index (American: Glycemic) that has been measured by numerous laboratories for a growing number of saccharides. The correct definition for GI adopted from FAO/WHO 35 ) is presented in the sub-page "Glycemic Index". For common use Wolever's 36 ) description reads "The glycemic index (GI) is a classification of foods based on their blood glucose-raising potential."
Knowledge of the GI (tables with hundreds of food entries are easily accessible 37 ) ) offer the individual with some common sense the opportunity to choose from the larger polysaccharides with either a fast raising blood-glucose potential for immediate tough effort or with a slow sustained delivery of blood glucose.

BLOCKING the UPTAKE

of POLYSACCHARIDES
.
Phaseolus Vulgaris (Kidney beans pods) is a phytotherapeuticum well known for preventing the uptake of poly carbohydrates by the small intestine 4 ) 5 ).

Phaseolus is obtainable in small "pharmaceutical" gelatine capsules. It is also delivered in the familiar aluminum medicine strips. The gelatine is dissolved by the gastric juice in about 20 minutes.
Phaseolus contains Glucokinines which neutralize the splitting action of intestine-enzymes. By swallowing Bean-pod simultaneously with poly-saccharides, the disintegration of the carbohydrate chain into mono- saccharides will be prevented. Thus the saccharides can not cross the intestinal-lining and will finally leave the intestinal path unused.

Gymnema (frequently G. sylvestre GS, sometimes G. inodorum) is another phytotherapeutic, widely used by physicians in India for the treatment of Diabetes type 1&2. It is also known as Gurmar or Gurmarbooti and as Meshasringi.
Its action differs from that of Phaseolus. It acts when the glucose is already in the blood by improving glucose uptake into cells 49 ) and likely by improving the secretion of insulin 50 ). In addition to its blood sugar lowering capacity it prevents the conversion of the Acetyl Coenzyme-A into fatty acids.

One research group reports "Our studies suggest that the com- ponent of Gymnema inodorum inhibits the increase in the blood glucose level by interfering with the intestinal glucose absorption process" 51 ).

Thus it blocks the fatty acid synthesis in the conversion-chain 52 ) from carbo- hydrates to fat. Gymnema has also some other interesting capacities specifically useful to help diabetics; these will not be discussed here, see 53 )
The pharmaceutical industry did also develop enzyme-blockers, like those based on Acarbose, an aminosaccharide. Phaseolus and Acarbose are also prescribed for Diabetics Type II 7 ) 8 ).
Bean-pod capsules/pills can be put easily in a ladies bag or in the little pocket of a jacket. During a "carbohydrate-rich" meal one can swallow some capsules/pills without being perceived. There are two drawbacks: one must remain continuously on the alert for carbohydrates, and the method by definition will not function on Mono- Saccharides, like Glucose and Fructose, as explained.

LOCK & KEY PRINCIPLE
The action of enzymes in the splitting of poly-saccharides (syn. carbo- hydrates) is based on the "Lock & Key" principle. In a lock (the specific enzyme) fits a key (a definite polysaccharide). This principle was described by Emil Fischer (Nobel laureate Chemistry 1902). The function of an enzyme- blocker like that in bean pods is to occupy locks so that the polysaccharides can not dock and the enzyme can not disintegrate the polysaccharide 6 ), so that polysaccharide /carbohydrate digestion is prevented. The enzyme in this case is alpha-amylase (plants, bacteria, yeasts, etc use beta-amylase).
It is essential that the carbo-blocker is at the right place at the right time, to become effective. The right place is where the amylase is in the thin intestine and the right time is when the amylase is there. So fat /carbo-blockers must be taken when the incident begins. This is opposed to f.e. food-supplements that have to be taken as a total amount per 24 hours, not necessarily associated with any food intake.

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Blocking the Uptake of

TRIGLYCERIDES

The uptake of fat can be blocked too. Three approaches will be mentioned:

º	complexing by saponification;
º	physical adsorption of fat;
º	blocking of the lipase enzyme.

Use of Fat- and Carbo-blockers offer a major contribution to live to the basic principle : "Weight change is the weight difference between stuff going-in and stuff going-out"

COMPLEXING by saponification

Classic saponification is based on boiling the fat, adding alkali-ions simultaneously.
This causes the fat (triglyceride) to break up into a mono- glycerid plus two fatty acids 20 ) which combine with an alkali-ion at once (making soap).
In the small intestine foreign enzymes take over the conversion function from "cooking" if blocking of the fat uptake is pursued. Freed fatty acids immediately combine with a peptide. This is called "complexing". The bigger combined molecules can not cross the lining of the intestine (as the smaller fatty acids would have done) to the lymphatic system. These big molecules will follow the intestine path and leave the body with the stools.

An example of a bacterial-pharmaceutical fat-blocker is Lipidplex from Biotics Research Corporation, Houston Texas US. It contains a Lipase and a Mg-Peptide 9 ).

Policy Statement,
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ADSORPTION of FAT

This method uses chitosan, a product made by many industrial laboratories from chitin. Chitin is found in the shield of shell-fish ranging from squids to crabs and shrimp. It is a long polysaccharide, a biopolymer, some times referred to as the "cellulose- fiber" of animals.
To produce chitosan this polysaccharide is stripped from three-quarters of its acetyl side- groups in the laboratory, leading to two changes: it looses its rigid structure (becoming a soluble gel) and it is positively charged, attracting fat like the loaded plastic foil scraps that keep sticking to your fingers. There is alpha- and beta-chitosan, beta being reported to be the more active one.
Medical applications of chitosan 26 ) are numerous, see abstracts, excerpts, references.
Its use as a fat blocker is based on its capacity to physically adsorb ("d"!) fat in the stomach and intestines by electrostatic binding, so that the lipase is prevented to split the fat into smaller units that could have passed the lining of the small intestine. Chitosan plus fat will leave the body unused with the stools.

USING PACKAGED -- DIETS The body must be supplied with a basic level of carbohydrates, peptides or proteins, minerals and (pro-)vitamins. When supply is short muscular tissue may be broken down. Visit also FAQ, Answer 3 , at this site.
When considering a packaged- diet cure, check the description or insert, if / how it meets the basic level requirement. Please consult a physician specialized in weight reduction methods.

Simultaneous use of different fat blocking approaches is not recommended.

When the uptake of fatty acids in the intestine lining is hampered uptake of necessary fat-soluble vitamins may also be reduced. It concerns A, D, E and K vitamins. Prescribing fat blockers sup- plements of these vitamins can be administered at the same time.

Please MIND.

Fat-/Carbo-blockers (more or less) prevent further increase of weight, resulting from "menu incidents". However blockers are not truly effective in reducing existing overweight.

USERS ARE RESPONSIBLE.

					In these pages descriptions only are given. Descriptions may not be interpreted as instructions. The authors emphasize that none of the descriptions will preserve from side-effects, injury, harm, damage, if any, resulting from putting into practice. The correctness of the supplied information is not vouched for. No guarantee is given that the aimed effect(s) will be achieved. Who applies, carries all responsibility. Before you pass on to self-treatment/ /self-medication, you ought to consult a physician and your pharmacist. The descriptions presented in these webpages do not replace the examination by, and consultation of a physician.

APPETITE Restraining Food ingredients and Medicine

Appetite restraining food ingredients are used to restrict the want for food intake. An example is ground Guar fibre 25 ) , which gives the sensation of a filled stomach by its absorption of fluid.
Another is inulin as supplied by the tubers of Helianthus tuberosus. It was brought from the American continent to Europe ages ago and is known by its original Indian name Topinambur. It is also known as "sweet potato" though it has nothing to do with the potato plant. This name however indicates its usage: it has a rich content of the sweet carbo- hydrate inulin that is closely related to sucrose. However it has a slightly different chemical structure for which the human body has no enzyme to split it up. So it is sweet but cannot be taken up and leaves the intestinal path.
Its primary function is as ballast like guar. There are indications 32 ) that the substitution of sugar by inulin also smoothes the swinging of the glucose level between hyperinsulinemi and hypoglykemia in the long run. (Hypoglykemia is a frequent inducement for food intake.)

Xhoba (Hoodia). One more example of an Appetite Restrainer or Appetite Suppressor is the South African Hoodia or, as it is called by the Bushmen Xhoba. The Hoodia is a cactus, a succulent (plant adapted to store water) of the Asclepiadaceae family 89 ). It has been used by the bushmen to avoid hunger sensation and thirst for millennia. Its way of functioning is not published yet pending submission of patent applications 90 ) . It is undergoing the required pharmacological test phases and is expected to become commercially available in 2004.

Pharmaceutical inhibitors. Appetite restraining can also be induced pharmaco-logically by inhibiting 56 ) nervous signal transmission. Their effect is that the signals of an emptied stomach are suppressed implying a continued feeling of food saturation. 57 ). A related effect is that the usual decrease in basal metabolism (see our subpage on "Yo-yo effect" ) does not occur.
An example of a pharmaceutical inhibitor is the Meridia pill, in Europe known as Reductil / Zolium / Reduxato, a Sibutramine 58 ) manufactured by BASF/Knoll. The nature of operation of a sibutramine implies potential interaction with other drugs and potential side-effects. Therefore the medication is restricted to physicians.

Another example, still under development, is a so called Insulin mimic. It is known from tests with rats (central intra-cerebro-ventricular administration) that receptors in the brain are sensitive to insulin, with the effect that appetite will be reduced. For an imagined self-medication two options would be either as a pill or as injections like diabetics are accustomed to. However insulin would hardly survive the guts when given as a pill. From diabetics is known that their insulin injections do not reduce appetite and their overweight tends to increase. So the insulin administered this way does not reach the brain receptors. A complication is that insulin also affects metabolism in the usual way.
The idea worked out by Merck Research Laboratories and Un of Cincinnaty College of Medicine is a small molecule they have built, mimicking the effect of insulin on the brain receptors. This insulin-mimic does pass the guts and reaches the brain receptors. As said, the concept is under development, for human use 73 ).

The "APPETITE HORMONE" GHRELin
A recent, exciting discovery is the "Appetite hormon" Ghrelin 74 ). Scientists were researching a Growth-Hormone RELeasing hormone, found one, and coined it correspondingly GHRELin. Ghrelin (a peptide of 28 amino acids) was originally discovered in rats; the human ghrelin is homologous to rat ghrelin apart from two amino acids, according to 74 ). It acts upon receptors of the hypothalamus and pituitary in the brain and seems to regulate Growth hormone secretion.
The ghrelin hormone is produced in the stomach and at some more places 75 ). It is released into the bloodstream and DOES reach the pituitery (for this it needs to attach to a fatty acid as a "dispatch-rider"). Amazingly the ghrelin hormone has more functions, one being to provoke the hunger sensation and also to influence fat metabolism so that more is stored in fat tissue.
A review about the different functions of ghrelin is published in The Scientist 85 ). Important names: K. Kangawa, M. Helman, D.E. Cummings.
What is the relation to the leptin-hormone function ( see the subpage leptin )? There is a competitive interaction between ghrelin and leptin in feeding regulation 76 ). Also inter-meal ghrelin levels displayed a diurnal (~day-time) rhythm that was exactly in phase with that of leptin 77 ).
The challenge now is to develop either a ghrelin-blocker that locks the receptor cells or to block the enzyme that couples ghrelin to its fatty acid carrier. An alternative might be to go through nature with a fine comb to find a blocker similar to the natural carbo-blocker phaseolus described in this page.

The anorectic (="appetiteless") hormone fragment PYY 121 ) In the early eighties the PeptideYY (with amino acids 3-36) was discovered. It is secreted by the Ileocolonic (last part of thin intestine, colon) endocrine cells. PYY reduces appetite. Researchers at the Imperial 122 ) College, London University found that obese subjects had relatively low plasma levels of PYY. PPY is released when a person eats protein-rich foods.
The "Anti-Obesity Vaccine"
A new development (2006) is the idea 120 ) to attach (parts of) a vaccine to the ghrelin molecules. The immune system will react (antibodies) to these so that the pertinent ghrelin hormone-molecule is made inactive. It works with rats. The rats lost weight even with maintained level of food intake. This means reduced metabolism, part of the calorie intake leaves the digestive tract unused. Less ghrelin implies less fat storage, less hunger, less metabolism. Questions to be answered still are: what may happen if and when the levels of ghrelin become (too) low and how to stop the action of the immune system if you want to.

Appetite restraining is not effective to all individuals. People with overweight do not eat because they are very hungry, except for a rare exception, but because of a social event or stress or habit or (derailed?) conditioning. Some suffer occasionnally from chewing-mania or at least are chewing-happy. For these people it is effective to chew much low-calorie food: fruit (apples etc.), large quantities of vegetables. At a reception: raw pieces of cucumber, gherkins, cauliflower, etc.

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Blocking the ENZYME lipase

Enzyme blocking according to the "lock & key" principle is described in the left column.
The enzyme lipase that should split tri- glycerides is neutralized by the enzyme- blocker. Then the triglycerides remain too big to pass the intestine lining and again leave the intestinal path unused.
An example is Xenical (chemical component: orlistat) supplied by ROCHE 21 ). For Xenical a prescription is required.
Lipidplex and Chitosan enjoy OTC (=over the counter) -status.

GLUEING TOGETHER SMALL
CARBO-HYDRATES

Beside the option to prevent enzymes to split larger poly sac- charides through the Key & Lock principle exists the option to "glue" (small) poly-saccharides together to larger ones that cannot pass the intestine wall. That is done by the substance pectin familiar from stiffening juices to jellies. Many fruits contain pectin; citrus rinds form the industial source for pectin production.
A familiar product said to have weight reduction capacity is the family of "apple-slimming" devices. They are based on the pectin won from pomace a residue from apple-cider presses.
The material of many plants combine pectin with water-absorbing fibre and other qualities.
An example is the cactus Opuntia ficus -indica, known in Mexico and South America as Nopal or Indian fig prickley pear 38 ). It is also well known in Northern Africa and Israel. A cultivar without spines is the OFI-cv-Osser. Its pectin prevents smaller poly sac- charides from being digested, its water absorbing capacity fills stomach and intestines. It has one of the lowest GI's measured: 7 at the glucose=100 "reference scale". It is sold in gelatin capsules.

The blocking of (animal) cholesterol
.

A striking blocking mechanism is the clog- ging of cholesterol receptors by phytosterols. Phytosterols are the vegetable variant of animal sterols (=cholesterol). The effect of blocking is again that the uptake of an un- wanted component (in this case cholesterol) is prevented. Phytosterols in turn cannot be digested by humans.86 )

Supplements to Diets.
.

Many "dieters" know that their nutrition- package requires little fat and few carbo- hydrates. Not many dieters realize that chan- ging to a reduced package implies a risk of missing essential nutrients: the nutrition- package must contain more than a minimal daily dose of amino-acids (for assembling body-proteins) and a fair amount of vitamins and minerals. Phytotherapeutic diet supplements for that reason often contain additions to cover the essential nutrients.

Different effects from Gastric-bypass or Diets on Ghrelin-production 103 )
.

The active part of a stomach-wall has been limited by a gastric bypass. So production of Ghrelin, and its effect on stimulating appetite, is decreased. Applying an intake restricting diet on the contrary will provoke the Ghrelin production to its full extend. This has been shown by Cummings cs. 83 )