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Orally active fraction of momordica charactia, active peptides thereof, and their use in the treatment of diabetes

A diabetes, active technology, applied in the field of diabetes, can solve the problems of unclear hypoglycemic components and mechanism of action

Inactive Publication Date: 2000-05-31
CALYX THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the hypoglycemic components and mechanism of action are still unclear.

Method used

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  • Orally active fraction of momordica charactia, active peptides thereof, and their use in the treatment of diabetes
  • Orally active fraction of momordica charactia, active peptides thereof, and their use in the treatment of diabetes
  • Orally active fraction of momordica charactia, active peptides thereof, and their use in the treatment of diabetes

Examples

Experimental program
Comparison scheme
Effect test

example 1A

[0051] The following examples are by way of illustration and not limitation. Example 1A. Isolation and Purification of Active Components in Bitter Melon Extract

[0052] Fresh immature bitter gourd fruits are washed, dried, and the seeds removed. Puree is mixed in phosphate buffered saline or deionized water. The suspension was centrifuged at 12,000 xg, then filtered under vacuum through a 0.22[mu] sterile filter (from Whatman). The clarified supernatant was passed sequentially through 30 kDal, 10 kDal and 3 kDal cut-off membranes (from Amicon filtration). Use SDS-20%-polyacrylamide gel electrophoresis to analyze the components that flow out through the cut-off membrane of 0.45 μ (the first step), 0.22 μ (the second step) and 10kDal (the third step), and the results are shown in Figure 1A middle. The fraction after the third purification step appears as a single band smaller than that of human insulin. As evident from gel electrophoresis analysis, the purified fractions d...

example 2

[0066] Figure 11 It shows the hypoglycemic activity of MC6.1 and its derivatives MC6.2 and MC6.3 in the oral glucose tolerance test of normal rats. Compared with the vehicle treatment group, these three polypeptides effectively reduced the blood sugar level in the experiment.

[0067] The hypoglycemic activity of MC6.2 (peptide of 11 amino acids) was further verified in diabetic rats. SD rats with an average body weight of 200 g were injected with streptozotocin at an amount of 40 mg per kg body weight. Such as Figure 12 As shown, after oral administration of MC6.2 to diabetic rats (average blood sugar 330 mg / dl) at a dose of 100 micrograms / rat (0.5 mg / kg body weight), the blood sugar level was significantly lower than that of the control group.

[0068] The hypoglycemic activity of MC6.2 (11 amino acid peptide) was tested on non-obese diabetic (NOD) mice. Such as Figure 13 As shown, daily oral administration of MC6.2 to NOD mice had a more significant effect on blood ...

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PUM

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Abstract

A water soluble extract of M.charantia named MC6, methods for its preparation and methods for its use in the treatment of hyperglycemic disorders are provided. The active MC6 is characterized by moving as a single band on SDS-PAGE having a molecular weight of less than 10 kDal, and by comprising three peptides. Also provided is a peptide component of MC6 named MC6.1, as well as analogues and mimetics thereof. The active MC6, MC 6.1, MC6.2, and MC6.3 exhibit hypoglycemic activity, even following oral administration. Also provided are methods of using the active agents to treat hyperglycemic disorders, particularly diabetes, where the active agents are preferably orally administered.

Description

[0001] FIELD OF THE INVENTION The field of the invention is diabetes. Background of the invention [0002] Non-insulin-dependent diabetes mellitus (NIDDM or type II diabetes) is the fourth leading cause of death in the United States, afflicts 5-7% of the world's population, and its impact is increasing in Western countries. When you have diabetes, your body either doesn't produce enough insulin or doesn't produce enough insulin, leading to elevated levels of glucose in your blood, a condition medically known as hyperglycemia. Although people of any age can develop diabetes, most people with diabetes are over the age of 45. The disease appears to run in families, and individuals who are overweight are at increased risk. [0003] Diabetes is a chronic disease that has no cure and is associated with several other medical conditions. It is the leading cause of blindness in people aged 25-74. 10% of diabetic patients have kidney disease. Diabetes mellitus is the most common cau...

Claims

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Application Information

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IPC IPC(8): A61K38/00A01N37/18A61K31/78A61K36/00A61K36/42A61K38/04A61K38/06A61K38/08A61K38/10A61K38/17A61P3/10C07K7/06C07K7/08C07K14/415C07K14/52
CPCA61K36/42A61P3/10A61K2300/00A61K38/011A61K38/04
Inventor B·纳格S·麦迪彻拉S·D·沙玛
Owner CALYX THERAPEUTICS
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