A bitter remedy for a sweet resolution
The fruit Ampalaya, Mormodica Charantia Linn (called Bitter Melon in English for its bitter taste) was discovered as a remedy for the treatment of diabetes.It has been the subject of a thorough and meticulous testing, which demonstrated the effectiveness of Charantia as an adjuvant in the treatment of diabetes.
Botany
Bitter melon or Ampalaya is a creeper of the family of cucurbits. Momordica means 'bite' and refers to the jagged edges of the leaf, appearing as if bitten fissured. The species charantia is from the Greek meaning the beautiful flower. The fruit looks dark green, somewhat like a cucumber with warts. It grows wild up to reach 5 cm, while the wild can be up to 25 cm in length. This plant grows in tropical areas of Asia, Amazonia, Africa and the Caribbean, mostly cultivated and used for medicinal and culinary uses. As reported from several scientific studies, Charantia has been used in the formulation of food supplements such as teas and capsules to lower blood sugar of people with diabetes.
Phytochemistry
Several studies were conducted to unravel the chemical components of M. Charantia and found the following: Amino acids, Sterol glucosides (charantin), Triterpene glycosides (momordiciside), Saponins, alkaloids, aromatic oils, proteins, lectins momorcharine cytokines, fatty acids, Vicine. The documented data shows that extracts of Charantia from leaves and fruits remarkably produce increased and improved glucose tolerance, and that overall hypoglycemic effects (lowered blood sugar) in people with diabetes were significant. An extract from the fruit has been found to stimulate insulin release from isolated pancreatic cells. It may also play a role in the renewal of beta cells, or may permit the recovery of partially destroyed beta cells. The properties of the fruit may also increase glucose uptake (the absorption of a substance) in muscle. Further studies on bitter melon seem to prove that Ampalaya, (M. Charantia Linn) contains proteins (called MRK29) involved in the inhibition of HIV. The momordicina has been identified as important for the activity nemiticida.
Pharmacology
Ampalaya or Bitter Melon has a long history of use as a hypoglycemic agent in Asia, Africa and Latin America. The amazing plant has been called vegetable insulin, according to Ethan Basch, M.D. and colleagues at various facilities in Boston, Massachusetts. It has also been used for cancer, gastrointestinal cramps, infections, infertility and psoriasis. M. Charantia also contains proteins that appear to be active against the poliomyelitis virus. The extracts of the plant bitter melon have been studied and appeared to be pharmacologically active against microbes. It also demonstrated vitro anthelmintic activity (action vermicide) worming AscarisGalli.
V.S. Baldwa and colleagues at the Medical College Hospital, Jaipur, India, and University Hospital, Uppsala, Sweden, an extract of M. Charantia, which they referred to as vegetable insulin, has consistent hypoglycemic effects (it lowers blood sugar) in people with diabetes mellitus. Its action within thirty to sixty minutes is similar to that of standard zinc crystalline insulin, with the peak effect seen after four to twelve hours, compared with two to three hours of regular insulin. Researchers noted that the greatest fall in blood sugar levels was found to be statistically significant. According to a research team at Miyazaki University in Japan and other facilities, Bitter melon contains active compounds in preventing and/or relieving certain diseases, including diabetes, fatty liver, and hardening of the arteries. Bitter melon has a positive protective effect on the walls of arteries. In addition, the fruit steeply reduced the amount of cholesterol and triglyceride levels in the liver, both in the presence and absence of dietary cholesterol. The juice may also help prevent lipid peroxidation damage.
Antitumor activity
Several preliminary studies (in vitro and in vivo) seem to show that bitter melon extracts possess antitumor activity. A study was conducted on the anti-carcinogenic in mice with skin carcinogenesis and it was found to Oral administration of fruit extract protected the mice from developing skin cancer and increased life expectancy compared with controls. The extract also reduced the carcinogenicity induced lipid peroxidation in liver and DNA damage in lymphocytes. It was also found that the extract of the fruit significantly active in liver enzymes such as glutathione S-transferase, glutathione peroxidase and catalase (P <0.001), showing a depression following exposure of the carcinogen. The results suggest a preventive role of water-soluble constituents of bitter melon fruit during carcinogenesis, which is probably mediated by their modulatory effects on enzymes of the biotransformation and detoxification system of the host. The clinical significance of these findings is yet to be determined.
Anti-ulcer
The traditional use of bitter melon in the treatment of ulcers is supported by several studies that seem to prove its anti-ulcer ethanol induced ulcer in rats.The antibacterial activity against H. pylori further contribute to this protective effect.
Immunomodulating activity
Extracts of bitter melon and isolated components have a variable effect on the immune system. It was shown to be immune stimulant in some studies and some immunosuppressive conditions (allograft rejection). The clinical significance is not known yet because it appears to be strongly dependent on the type of extract, the dosage and administration. The immunomodulating activity may explain its traditional use in psoriasis, which is now known to be an autoimmune disease.
Hypoglycaemic Activity
The hypoglycemic activity of bitter melon is the most studied and most significant. The activity of the fruits, seeds, leaves and whole plant has been confirmed in animal studies.
Diabetes induced by Alloxan
Diabetes mellitus can be induced in animals by partial pancreatectomy or by administration of diabetogenic drugs such as alloxan, streptozotocin, dithizone and serum anti-insulin.These agents selectively destroy β-cells of islets of Langerhans. Alloxan, a product derived from acid oxidized uric acid, is one of the most commonly used models of experimental diabetes.
A study examined the hypoglycemic effects of thirty most popular Indian herbal anti-diabetes as Indica Cochin, tragi involucrata, Gymnema Sylvestre, Momordica charantia and Pterocarpus carrier, and was found to be the most powerful. In this experiment, rats with diabetes induced by alloxan, bitter melon reduced the initial reading of blood glucose from 244 mg / dL to 119 mg / dl after a single dose of 250 mg / kg of extract for two weeks. Not and 'was found sugar in the urine after two weeks.
Another study confirmed that both the aqueous alcoholic extract of the fruits of bitter melon exerts hypoglycaemic effects in rats with acute diabetes induced by alloxan. Different doses of both extracts produced a significant reduction after one week (p <0.01). The maximum hypoglycemic effect was observed after three weeks of 200 mg / kg / day of extract. In rats with chronic diabetes induced by alloxan, 200 mg / kg / day of bitter melon extract reduced the levels of plasma glucose by 64% in a month, increasing to a 70% reduction after four months. A recent study documented using three different extracts of fruits, an extract made from methanol on dried fruit, an extract of chloroform also based on dried fruit and an aqueous extract prepared from fresh fruits. These extracts were then dried and pulverized. Extracts were compared to glibenclamide for their hypoglycemic effects in rats with diabetes induced by alloxan. The data were extracted powder orally at a dose of 20 mg / kg bw and glibenclamide at a dose of 0.1 mg / kg. As you can see from Table 1, all three extracts lowered the blood glucose level. The effect of chloroform extract is minimal, with the aqueous extract is more effective and similar to that of glibenclamide.
Table 1
Comparison of the effectiveness of different extracts of bitter melon with glibenclamide on percentage reduction in blood glucose of rats with diabetes induced by alloxan.
| Extract | Reduction | Reduction |
| After 1 week | Week 4 | |
| Active group | Active group | |
| Ethanol extract | 49,2 | 39,0 |
| Chloroform | 3,9 | 3,8 |
| Water extract | 49,0 | 50,8 |
| Glibenclamide | 50,8 | 51,5 |
| Diabetic untreated | 270,9 | 359,8 |
Diabetes induced by streptozotocin:
Administration of bitter melon has demonstrated improved glucose tolerance significantly in rats with diabetes induced by streptozotocin, and a model of human insulin-dependent diabetes.A study was conducted comparing the bitter melon and metformin (500 mg / kg of alcohol extract of bitter melon) in plasma, the glucose levels were reduced by 26% (p <0.002) at 3.5 h after administration where 200 mg / kg metaformina caused a reduction of 40-50% (p < 0.001).The data from this study suggest that bitter melon lowers the levels of plasma glucose by stimulating the synthesis of glycogen in the liver, and is unlikely to act as a stimulant for insulin secretion. In another study of rats with streptozotocin-induced diabetes, bitter melon extract induced a reduction of about 22.7% in plasma glucose levels after two months. The alteration in liver and skeletal muscle of glycogen content and levels of glucokinase, hexokinase, glucose-6-phosphate and phosphofructokinase liver in diabetic mice were partially restored after administration of bitter melon. In similar conditions, the extract reduced the blood glucose of streptozotocin-induced 15.37%, 18.68% and 22.86% in 40th, 50th and 60th days respectively. Compared to diabetic control, treatment with bitter melon extract allowed a 36% increase in glycogen in both liver and skeletal muscle in a 5% reduction of renal glycogen content. The overall results suggest that bitter melon can increase glucose utilization and the formation of glycogen. The results further suggest that bitter melon is most effective when insulin is secreted by beta cells in the pancreas that are capable of responding. However, even when damaged, the extract would continue to produce hypoglycemic effect suggesting a direct effect of insulin-like.
Effects on hyperglycemia with hypercholesterolemia
The effects of the watery extract lipoproteins and cholesterol has been studied and compared with glibenclamide. In diabetic rats triglyceride levels were reduced both the aqueous extract of bitter melon with glibenclamide (69% and 65% respectively), while total cholesterol as HDL levels remained unchanged.High levels of VLDL were reduced with either the extract of bitter melon with glibenclamide. These results suggest that the effects of the aqueous extract of bitter melon are comparable to those of glibenclamide in improving not only hyperglycemia, but also the imbalance of the lipoproteins.
Another study found that intake of dried and powdered fruit of bitter melon for 14 days to rats with either cholesterol-free diet rich in cholesterol caused an 'increase in HDL cholesterol and a significant reduction in serum triglycerides and the total concentration of cholesterol in the liver.
An interesting finding of this study is that bitter melon consistently lowered the concentration of glucose in the blood of rats fed cholesterol-free diet, but not in rats whose diet was rich in cholesterol.
With all the studies and researches done, we could claim that Bitter melon helps reduce levels of triglycerides, which are often elevated in diabetics, and improves the balance of lipoproteins.
However, to maintain efficacy, patients should also observe a low cholesterol diet.
Summary of the effects of hypoglycemic
The various effects of bitter melon have been summarized in Table 2. The clinically significant activity is still under study. However, it was shown that bitter melon increases the insulin levels in healthy animals, neither insulin resistance both in animals and in diabetic patients.
It is likely that the overall hypoglycemic activity is tied to extra-pancreatic activity that promotes the storage of glucose in muscle and liver, while suppressing the excessive production of glucose in the liver. This would be similar to the effect of metformin. It has been observed that the anti-diabetic activity of bitter melon could be similar to that of metformin.
Table 2:
Overview of hypoglycemic activity of bitter melon. Quoted in a recent article in a magazine JK Grover and SP Yadav.
| Attività Pancreatica |
Improvement of beta cells promotes or mimics insulin |
| Attività Extra Pancreatica |
Increase in muscle GLUT4 protein transport |
Increase the use of glucose in the liver and muscle tissues |
|
| Inhibition of glucose-6-phosphate and fructose 1-6 bisphosphate in the liver and stimulation of red cell activity and glucose-6-phosphate dehydrogenase, liver | |
| Inhibition of glucose transport by brush enzymes of the small intestine | |
| Re-establishment of depressed activity of enzymes in the liver, metabolism responsabilecarbohydrate (Including hexokinase, glucoskinase, metabolism of carbohydrates (including hexokinase, glucokinase, phosphofructokinase) phosphofructokinase) |
The prevention of diabetes complications
The complications and negative feedback of diabetes, with serious damage to the kidneys, eyes, nerves and blood vessels are known.
It has been shown that bitter melon reduces or delays the complications of diabetes in the animals studied. It 'been shown that bitter melon lowers levels of serum creatinine, albumin in urine, urine volume and weight in mice with diabetes induced by streptozotocin. The complication of diabetes and disabling diabetic neuropathy is more frequent, which causes pain in the limbs, sexual dysfunction, gastrointestinal, genitourinary and cardiovascular symptoms. The extract of bitter melon (200 mg / kg) administered to diabetic animals for 50 days produced a pain reduction in the tails of mice compared with controls. The effectiveness of bitter melon was considered also in the prevention of cataracts of rats with diabetes caused by alloxan. The experimental group was treated with a daily dose of 200 mg / kg of extract of bitter melon freeze-dried and dissolved in water for 4 months. All eight animals in the untreated group developed cataract (stage IV) after 3 months, but none group of mice treated with bitter melon developed cataracts during the four months of the experiment. Oral administration of bitter melon extracts for 1 month produced a 64% reduction in serum glucose levels compared to the level of 48 hours. After two months of treatment, glucose levels decreased by 67%.
Syndrome X
The metabolic syndrome known as Syndrome X (insulin resistance syndrome or syndrome Reaven) is characterized by a group of metabolic risk factors in a person. These include central obesity (excessive fat tissue in and around the abdomen) atherogenic dyslipidemia, insulin resistance or glucose intolerance, pro-thrombotic state (eg, high values of inhibitors in blood fibrinogen or plasminogen activators), high blood pressure (130/85 mm Hg or higher) and a inflammation (e. g. high sensitivity C-reactive protein in blood). Overweight and / or obesity, physical inactivity and genetic factors are the main causes of this syndrome.People with metabolic syndrome are at high risk of coronary disease, other diseases related to plaque buildup in artery walls (eg, stroke and peripheral vascular disease) and type 2 diabetes. It has been shown that a diet high in fructose induces the onset of the syndrome X. It 'been shown that bitter melon extract (400 mg / day for 15 days) prevents hyperglycemia (63.5 mg versus the 75.78 mg / dl (p <0.001) and hyperinsulinemia (7, 78 ng / dl v 15.04 ng / dl in controls, P <0.001) in rats fed a diet of rice fructose.
Clinical trials
Clinical studies with bitter melon are quite a few and methodologies were supported by a number of subjects, and were based on training set of bitter melon. Further studies tend to confirm the traditional use of bitter melon to treat diabetes. An extract of bitter melon has demonstrated a reduction in blood glucose in nine subjects with type 2 diabetes on oral glucose tolerance test (50 g). Fried bitter melon consumed daily has been shown to produce a small but significant improvement in glucose tolerance in diabetic patients with no increase in insulin levels in serum. It demonstrated that the pulp of this vegetable, bitter melon, reduces significantly the serum glucose and postprandial (after meal) in '86% of cases, and fasting glucose in 5% of cases in 100 patients with moderately from type 2 diabetes. It has been observed that the juice of bitter melon improves glucose tolerance in type 2 diabetes.
Security
A study on alloxan-induced diabetic rats comparing the effects of the aqueous extract of bitter melon with glibenclamide in a period exceeding four weeks, found that levels of uric acid and creatinine did not seem to increase, indicating an absence of any significant damage to the kidneys. Levels of SGOT were lowered and with the bitter melon extract Aquos with glibenclamide (21% and 46% respectively), the SGPT was also lowered by 14% and 12% respectively. These results suggest that both treatments have a protective effect, contrary to the organ damage that diabetes causes. At the end of a 30 day treatment histological changes of liver or kidneys were not observed. The authors concluded that the extract of Bitter melon aqueous 20 mg / kg can reverse hyperglycemia in rats induced dall'allosana without toxicity to the liver or kidneys (after 4 weeks) and could be prescribed safely to patients with diabetes.
A sub-acute toxicity study found that at the end of a two month study period with 200 mg / kg / day of freeze-dried bitter melon extract did not produce any change in the statistical sense values of significant leukocytes (the WBC), erythrocytes ( RBC), hemoglobin, hematocrit, mean corpuscular volume (MCV) and mean concentration of hemoglobin (MCH).
The possible anti-fertility effects, teratogenic and abortifacient effects of some constituents, and because of the lack of detailed information, the use of extract of bitter melon is not recommended during pregnancy or those who plan to make a family.
Bitter melon has not been classified by the American Herbal Products Association or evaluated by the European Commission, Germany. M. Charantia is available as a dietary supplement in the United States under the Dietary Supplements Health and Education Act of 1994 (DSHEA).
Interaction with drugs
Ampalaya or Bitter melon may have additive effects when consumed in combination with other hypoglycemic agents.
In a clinical study, 8 out of 9 subjects were tested an additive effect to reduce glucose after taking bitter melon or frying the fruit together with sulfonylurea. In rats, the glucose lowering effect of sulfonylurea tolbutamide was enhanced after ingestion of bitter melon juice.
Directions:
Type 1 Diabetes - supportive treatment, reduction of long-term complications
Type 2 diabetes - blood sugar control and reduce long-term complications.
Syndrome X - insulin - resistance, obesity.
Obesity - reducing the risk of developing diabetes.
Digestive disorders including ulcers
Dosage:
The dried powders and extracts used in experimental studies have not been chemically defined and researchers disagree on what type of extract is more effective. Some studies suggest that the extract of the fruit is more effective. A study found that the ethanol extract was ineffective, still significant activity has been confirmed for the alcoholic extracts, as well as dried fruit powder in other studies. These findings illustrate the complexity of producing effective herbal extract and suggest that the aqueous extract-alcohol could give a broader spectrum activity.The bitter melon leaves are commonly used as a decoction. A cup of leaves is boiled in three cups of water. This decoction is taken one to three times a day. The fruit is also eaten fried or taken as juice. However, since the fruit is extremely bitter, it is often taken dried in powder form for tablets or capsules. The dose of dry powder in capsules range from 3-15 g per day. The standardized extract has a variation that is typically 100-200 mg three times daily. The ratio of the extract and the drug varies from 4:1 to 20:1. The extracts are generally standardized to 3-7% of the compound and 0.5-1% charantia, bitter melon.
Conclusion:
Bitter melon is more effective nell'iperglicemia moderate (mild diabetes in the trial of the reduction was 50-60%). In severe diabetes the effect is minor. The improvement is slower compared to sulfonylurea or insulin. The effects of bitter melon insulin differ in four aspects: 1) has a hypoglycaemic effect on oral administration, 2) has a delayed onset of action, 3) increases the peripheral utilization of glucose with insulin independent tissues, 4) and activity and longer duration. Like insulin, bitter melon has hypoglycemic activity. It Increases the glycogen content of skeletal and liver and increases the enzymes involved in glycogenesis. Bitter melon may be more effective in reducing elevated serum glucose when patients follow a diet low in cholesterol.
Bitter melon may be useful in reducing long-term complications in type 1 diabetes. It may help control hyperglycemia, insulin resistance and hyperlipidemia in type 2 diabetes and in patients with syndrome X. Additional clinical trials are needed to strengthen the clinical efficacy in treating these disorders.
Important Reminder:
Melandia for Charantiaitalia is not responsible for any adverse effects or consequences resulting from the use of the suggestions, preparations, or procedures presentend in this site. Should any questions concerning preparations and procedures in taking M. Charantia, we strongly advise to consult a professional healthcare provider or medical practitioner.
Reference List
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review. J Ethnopharmacol 2004, 93 (1):123-132.
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on the glucose tolerance in maturity onset diabetes. J Ethnopharmacol 1986, 17 (3) :277-282.
(40) Virdi J, Sivakami S, Shahani S, Suthar AC, Banavalikar MM, Biyani MK. Antihyperglycemic
Effects of three extracts from Momordica charantia. J Ethnopharmacol 2003, 88 (1):107-111.
(41) SS Rathi, JK Grover, V. Vatsa The effect of Momordica charantia and Mucuna pruriens in
experimental diabetes and Their Effect on key carbohydrate metabolic enzymes in Involved
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84 (1):105-108.
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charantia in a validated animal model of diabetes. Pharmacol Res 1996; 33 (1):1-four.
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charantia in a validated animal model of diabetes. Pharmacol Res 1996; 33 (1) :1-4.
(49th) Jayasooriya AP Sakono M Yukizaki C, Kawano M, Yamamoto K, Fukuda N. Effects of
Momordica charantia powder on serum glucose levels and lipid parameters in rats fed Various
with cholesterol-free and cholesterol-enriched diets. J Ethnopharmacol 2000, 72 (1-2): 331 -
336.