Hypoglycemic active part and hypoglycemic effective component of madder, preparation method and application thereof
A technology of effective parts and active ingredients, which is applied in the effective part of madder for lowering blood sugar and its preparation, can solve the problems of high cost and intestinal side effects, and achieve safe price, good social value and economic value, and a wide range of sources of diabetes treatment drugs Effect
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Embodiment 1
[0022] This example is the extraction method and preliminary activity screening of each extract of Rubia radiata, that is, the effective part.
[0023] The preparation method of the effective part of madder for lowering blood sugar is as follows: crush 500 g of madder rhizome, moisten with acetic acid, extract twice with chloroform and methanol respectively at room temperature, filter, recover the solvent, and obtain the effective part of chloroform for lowering blood sugar (Rc, 4.5g) and methanol hypoglycemic effective fraction (Rm, 12.8g).
[0024] Activity assay:
[0025] Method: Microplate method
[0026] Principle: α-D-glucosidase catalyzes the hydrolysis of 4-nitrobenzene-α-D-glucopyranoside (PNP-G) to produce nitrophenol (PNP, a yellow substance with maximum absorption at around 400m), α -Glycosidase inhibitors can inhibit the binding of α-glucosidase to the substrate to reduce the release of PNP. The enzyme inhibitory activity of the extract was calculated by the ch...
Embodiment 2
[0036] This example is a method for preparing the active ingredient, that is, the active compound, from the active part of Rubia chloroform under the guidance of activity.
[0037] The specific method is: the effective part of chloroform (4.5g) obtained in Example 1 is subjected to 200-300 mesh silica gel column chromatography, petroleum ether-acetone gradient elution (95:5-9:1), and 4 parts are obtained, of which Fraction 3 (Rc-3, 1.6 g) had α-glucosidase inhibitory activity (Table-2). This part was eluted by silica gel H column chromatography, petroleum ether-acetone (15:1), combined by TLC detection, and subjected to Sephadex LH-20 column chromatography, acetone eluted to obtain compound 1 (12.5mg), compound 2 (5.5mg ) and compound 3 (120.7 mg).
Embodiment 3
[0039] This example is the determination of the activity of the compounds in Rubia radiata inhibiting α-glucosidase.
[0040] Measuring method: with embodiment 1.
[0041] Determination results: The experimental results are shown in Table 2. The initial screening inhibition rates of the three compounds were all higher than the positive control Acarbose, while the IC 50 Values are all lower than 50μg·mL -1 , far less than the clinically commonly used hypoglycemic drug Acarbose (IC 50 =1081.27μg·mL -1 ), has high α-glucosidase inhibitory activity, and can be developed as an active ingredient of madder for α-glucosidase inhibition.
[0042] The α-glucosidase inhibitory activity of active ingredient in table 2 madder
[0043]
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