KR20150036538A - Application of gynura divaricata in preparing medicine or health food for treating hepatitis - Google Patents

Abstract

The high-dose group of white tea alcohols extracts can significantly inhibit the acute liver damage of small rats caused by carbon tetrachloride, and the glutamate pyruvate transaminase (GPT) and It is possible to lower the glutamate oxaloacetic acid transaminase (GOT) and alleviate liver cell degeneration and necrosis.

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention [0001] The present invention relates to a method for preparing a medicament for the treatment of hepatitis of GYNURA DIVARICATA (GYNURA DIVARICATA)

Field of the Invention The present invention relates to the field of Chinese medicine, and more particularly to the use of white tea beans in Chinese medicine as a single ingredient for pharmaceuticals and health foods.

White potato (白子 菜) is also called Baekdang Samchechil (白 背 三七), and asteraceae white porcelain Gynura divaricata (L.) DC. [ G. oualis DC. G. pseudo-china (L.) DC.]. The nickname of white porcelain is the name of the potato ("Gwangju Flora"), the soil of the land, the white porcelain (白 仔 菜 药), the red blood gang (" (刀 刀), 刀 刀 (刀 刀 药), 淸 心 菜, 白血 皮菜, walnut 七 七 (胡豆 七), a great illness红 仙草, and Shingo are the most common species in the world. White porcelain is a perennial plant with a height of 30-60cm and its stem is upright or base is slightly inclined upwards and is woody. When dried, it becomes prone, branches do not split, It is either hairless or covered with short, soft hairs and slightly purple. The leaves are thick and usually concentrated in the lower part, with or without faucets. Leaves are oval, elliptical or obovate type, 2-15cm long, 1.5-5cm wide, with a stumpy or sharp pointed top, basal wedge-like or narrow petiole extending It is a double or slightly heart-shaped, with sawteeth at the edges, cracks in the shape of a lollipop, and rarely complete edges. The upper surface is green, the lower surface is purple, the side veins are 3-5 pairs, and the veins are often connected by a nearly circular long fine mesh, with a sharp black line appearing on drying, and both sides covered with short, soft fur. The petiole is 0.5-4cm long, has short, soft hairs, and the base is egg-shaped or moon-shaped with ears with teeth. The upper leaf is gradually smaller, bract lobed, narrow lanceolate or linear, feathery, with a slight crack, no bark, and a small stem wrapped around it. The diameter of the epididymis is 1.5-2 cm, and usually (2) three to five stems or a conical flower-shaped conical flower shape are arranged at the end of the branch, and the branch is divided into a fork shape. The length of the peduncle is 1-15cm, it is densely covered with soft hairs, and has 1-3 linear bracts. The involucre is a bell-shaped, 8-10 mm long, 6-8 mm wide, and has numerous linear or thread-shaped calyxes at the base. The involucre is 11-14 in one layer, narrow lanceolate, 8-10mm long, 1-2mm wide, with the top gradually becoming acute and forming a long triangle, the edge is the dry cortex and the back has three veins , Short, or almost hairless. The flower is orange-scented, and extends slightly from the gun. The length of the corolla is 11-15mm, the tube is thin, the length is 9-11mm, the upper part is enlarged and the leaf is long oval egg shape, and the top is pointed red. The base of the anther is blunt or lanceolate; Shrub branch is thin, conical appendix, covered with papillary hair. Achenia is columnar, about 5mm long, brown, with 10 rows of bracts, covered with fine hairs; The hairs are white, silky, and 10-12mm long. The fertility period is 8-10 months. Medicinal properties of medicinal plants and herbal medicines are rootstock, with thin and long hairs. The stem has a cylindrical shape, a dark purple color, short hairs covered, alternate leaves and wrinkles, and a complete leaf is an inverted oval shape of long egg-shaped to long circular shape, 5-15 cm long, 2.5-8 cm wide, The tip is blunt or short and pointed. The base has two ears. The edge of the leaf has irregular grooves and serrations. The upper and lower sides have soft hairs. Occasionally you can see headstands or guns. Achenes are dark brown with white hairs. It is weak and the taste is pale. The white porcelain is distributed in Guangdong (Gwangju, Namhae), Haenam (Jungmae, Ayeon, Mangyeong, Baekje, Jungjung, Gyeongsan), Hongkong, Yunnan (Kyungdong, Hongha and Nokchun) and also in northern Vietnam. It is used for bleeding, bronchitis, pulmonary tuberculosis, swallowing, edema, swelling, bruising, rheumatism, uterine bleeding, trauma hemorrhage. Whooping cough, fractures, bleeding wounds, and swelling of the dragon. White porcelain contains n-eicosane, tetracosanol, octacosanoic acid, octacosyl alcohol, palmitic acid, stigmasterol-3-O- Stigmasterol, 3-O-β-D-glucopyranoside, Stigmasterol, β-Sitosterol, Daucosterol, Friedelin, etc. ≪ / RTI > Modern research has shown that there is a certain blood glucose lowering effect.

It is an object of the present invention to provide a kind of novel use of white pigments capable of effectively protecting the liver.

The object of the present invention is realized as follows: In the treatment of hepatitis in white porcelain, in the application to the manufacture of medicaments or health food products, the medicaments or health foods are prepared by mixing a bagasse extract with a conventional amount of a pharmaceutically acceptable auxiliary material Is a clinically acceptable formulation to be manufactured.

The white raspberry extract is a water extract or an alcohol extract.

The water extract is prepared by adding 8 to 12 times of water to white flour, stirring for 1.5 to 2 hours, adding 5 to 8 times of water to the residue, adding the extract for 1 to 1.5 hours Followed by filtration.

The alcohol extract is prepared by adding 75% to 90% of ethanol to 8 to 12 times of white flour, refluxing for 1.5 to 2 hours, adding 75 to 90% of water to the residue, For a period of time, combining the extract with the filtrate, and recovering and concentrating the ethanol.

The formulation is a pharmaceutically acceptable granule, capsule, tablet or fabric solution.

The present invention has been found to have a significant inhibitory effect on the acute liver injury caused by CCl ₄ in a high dose group of white algae extract and water extract, and the serum glutamate pyruvate transaminase (GPT) , And glutamate oxaloacetic acid transaminase (GOT) to lower hepatocyte denaturation and necrosis.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, the present invention will be described in more detail with reference to some specific embodiments of the present invention, but the present invention is not limited to these embodiments.

Example  1 (water extraction)

The extract was extracted by adding 8 times water to white porcelain and extracted for 2 hours in the first step and 8 times in water for the second time. After extracting for 1.5 hours, the extract was combined, filtered, concentrated and dried to obtain brown A powder phase is obtained. The yield of the extract (the final powder yield divided by the weight of the injected drug) is 6-10%.

Example  2 (water extraction)

The white liquor was extracted by adding 10 times of water. The extract was extracted for 1.5 hours in the first step, 6 times in water was added for the second time, and the extract was extracted for 1.2 hours. After the extract was combined with the filtrate, A powder phase is obtained. The yield of the extract is 6-10%.

Example  3 (water extraction)

The extract was extracted by adding 12 times water to white porcelain and extracted for 1.5 hours in the first step and 5 times in water in the second time. The extract was then extracted for 1 hour. After the extract was combined with the filtrate, A powder phase is obtained. The yield of the extract is 6-10%.

Example  4 (Alcohol Extraction)

80% alcohol was added to white porcelain, and the mixture was refluxed for 2 hours. Then, 80% by volume of water was added to the residue, and the mixture was allowed to stand for 1.5 hours. The extract was combined, filtered and ethanol was recovered, And dried to obtain a brown powdery phase. The yield of the extract is 6-8%.

Example  5 (Alcohol Extraction)

90% alcohol was added to white porcelain, and the mixture was refluxed for 1.5 hours. Then, 90% by volume of water was added to the residue, and the mixture was stirred for 1 hour. The extract was combined, filtered and ethanol was recovered, And dried to obtain a brown powdery phase. The yield of the extract is 6-8%.

Example  6 (Alcohol Extraction)

Twelve times 75% alcohol was added to white porcelain, refluxed for 2 hours, 75% of water was added to the residue, and the mixture was allowed to stand for 1.5 hours. The extract was combined, filtered and ethanol was recovered, And dried to obtain a brown powdery phase. The yield of the extract is 6-8%.

Example  7 (granule)

Prescription: Calculate with 1 part of the water extract obtained in Example 1, 2.5 parts of sucrose and 1.5 parts of dextrin, depending on the weight part.

Preparation method: Extract powder is added to sucrose and dextrin and mixed well to prepare granules, which are then dried and separated.

Appearance: This product is a yellowish brown granule, taste a little sweet.

DOSAGE AND ADMINISTRATION: Take 7.5g once a day and take it in boiled water 2-3 times a day.

Example  8 (granule)

Prescription: Calculate with 1 part of the water extract obtained in Example 3, 2.5 parts of sucrose and 1.5 parts of dextrin, depending on the weight part.

Preparation method: Extract powder is added to sucrose and dextrin and mixed well to prepare granules, which are then dried and separated.

Appearance: This product is a yellowish brown granule, taste a little sweet.

DOSAGE AND ADMINISTRATION: Take 2.5g once a day and take 2 ~ 3 times a day in boiled water.

Example  9 ( Capsule )

Prescription: Calculated by weight part, 1 part of alcohol extract obtained in Example 4 and 2 parts of starch.

Preparation method: Extract powder is added to starch and mixed well to form granules, which are dried and encapsulated.

Appearance: This product is capsules, the contents are dark brown granules or powder, taste slightly.

DOSAGE AND ADMINISTRATION: Take 3 capsules once or twice or three times a day.

Example  10 (tablet)

Prescription: Calculate the amount of the alcohol extract obtained in Example 5, the starch 2 parts, and the amount of magnesium stearate, based on the weight.

Preparation method: Extract powder is added to starch and mixed evenly to prepare granules, which are then dried and then purified by adding magnesium stearate.

Appearance: This product is a dark brown tablets, taste a little bit.

DOSAGE AND ADMINISTRATION: Take 3 tablets once or twice a day.

Hereinafter, the drug action principle and beneficial effects of the present invention will be described in more detail by way of experiments:

1. Materials and Methods

1) Experimental drug: white water extract (1.3 g of herbal medicine / ml) and alcohol extract (2.6 g of herbal medicine / ml)

Bifendate dotted pillow, Gwangju Sungguk (Pharmaceutical) Stock Co., Ltd., Lot No .: JF40021.

2. Animals NIH small rat, SPF, male, body weight 18-22g. Laboratory animal quality certificate number: 2006A051; SPF class laboratory animal environmental condition acceptance certificate number: 2006B023; SPF grade laboratory animal production license number: SCXK Guangdong 2011-0015; Animal is provided by Southern Medical University animal experiment center.

3. Major Chemical Reagents and Measuring Devices: Aminotransferase (ALT) assay kit, Zhongshan North Biotech Biotechnology Co., Ltd., Lot No: 121881; Aspartic acid transaminase (AST) assay kit, Nakayama North Biotechnology Co., Ltd., Lot number: 120921; Carbon tetrachloride solution, analytical reagent, Tianjin City Boryeong Fine Chemical Co., Ltd., Lot No: 111010; Formaldehyde solution, analytical reagent, lot No. 20111007, Guangdong Guanghua Chemical Co., Ltd.; Anhydrous ethanol, analytical reagent, lot number 20110416, Tianjin City Jinpung Chemical Co., Ltd.; Dimethylbenzene, Analytical Reagent, Lot No 20101224, Guangdong Guanghua Chemical Industry Co., Ltd.; Hematoxylin, biotite, lot No. 060408, Beijing Chungang Biological Technology Co., Ltd. Fluka import packaging; Eosin Y, Biotyping site, Lot No. 20050912, China East China Normal University Chemical window; ECHO LCD Biochemistry Analyzer is produced in Italy. OLYMPUS AU5421 type automatic biochemical analyzer, OLYMPUS production in Japan; OLYMPUS BH-2 fluorescence microscope, OLYMPUS production in Japan; BECKMANTM30 low temperature centrifuge, manufactured by BACKMAN, USA; LEICA RM2135 type tablet cutter, produced by LEICA in Germany; SARTORIUS electronic balance, produced by SARTORIUS Germany.

The animals were divided into two groups: normal control group, model group, biphenate group (0.2 g / kg), water extract high dose group (1.12 g / kg), water extraction intermediate dose group (0.56 g / (0.28 g / kg), the alcohol extraction high dose group (1.12 g / kg), the alcohol extraction intermediate dose group (0.56 g / kg) and the alcohol extraction low dose group (0.28 g / kg). Twelve rats per group were administered gastrointestinal tract once a day for seven consecutive days. The normal control group and the model group received gastrointestinal administration of the same volume of tap water. The gastrointestinal administration volume was 0.25 ml / 10 g small mice and they were fed freely. One hour after administration of the last gastrointestinal tract, 0.2 ml / volume of 0.12% (by volume) carbon tetrachloride (pure peanut oil) was injected intraperitoneally. After 16 hours, the eyeballs were harvested and blood was collected. The serum was taken by centrifugation, and then glutamate pyruvate transaminase (GPT) and glutamate oxaloacetate transaminase (GOT) were detected Respectively.

5. Pathological examination: The hepatic lobe was fixed with neutral formalin, dehydrated by conventional method, and the section (4 micron) was wax-embedded, HE stained, and the pathological changes of the liver tissue were observed with an optical microscope. The extent of hepatic tissue damage was classified as grade 4 (1): grade 0 (-), normal liver structure, denaturation, necrosis, and inflammatory cell infiltration not evident; Ⅰ (+), liver lobular structure is still normal, some hepatocytes are seen to be cloudy and swollen, balloon shaped deformation or fat degeneration, dot necrosis scattered; Ⅱ class (++), liver lobular structure is not clear, distinct small necrosis is visible, accompanied by inflammatory cell infiltration; Ⅲ class (+++), liver lobular structure is not clear, distinct necrosis is seen, and inflammatory cell infiltration is accompanied.

및 등급/빈도분포표 자료로 표시하였으며, spss 8.0 통계 소프트웨어 One-Way ANOVA LSD 또는 Dunnett T3법 및 Nonparametric Test 2 Independent Samples Tests법으로 데이터를 처리하였다.6. The experimental data

Data were analyzed using SPSS 8.0 statistical software One-Way ANOVA LSD or Dunnett T3 method and Nonparametric Test 2 Independent Samples Tests.

2. Test results:

1) Liver function test result

The results of the test for serum glutamic acid pyruvate transaminase (GPT) and glutamate oxaloacetic acid transaminase (GOT) in small rats are shown in Table 1.

By group GPT (U / L) GOT (U / L) Normal group
Model Group
Biphen Dating Group
Water Extraction High Capacity Group
Water Extraction Medium Capacity Group
Water Extraction Low Capacity Group
Alcohol Extraction High Capacity Group
Alcohol Extraction Intermediate Capacity Group
Alcohol Extraction Low Capacity Group 43 ± 6 **
317 ± 112
47 ± 9 **
178 ± 63 *
193 ± 74
230 ± 81
162 ± 90 *
231 ± 75
224 ± 105 113 ± 17 **
303 ± 96
240 ± 73
135 ± 29 *
173 ± 71
262 ± 87
220 ± 31 *
238 ± 79 *
292 ± 68

, N=12)][Serum GPT, GOT results of small mice in each experimental group (

, N = 12)]

Note: * compared to the model group, P <0.05; ** compared to the model group, P <0.01.

Table 1 shows that both serum and glutamic acid pyruvate transaminase (GPT) and glutamate oxaloacetate transaminase (GOT) were significantly elevated (P <0.01); In the biphenate group, serum transaminase significantly decreased (P <0.01); Both the serum glutamate pyruvate transaminase (GPT) and the glutamate oxaloacetic acid transaminase (GOT) in the high dose group of white porcelain water extract and alcohol extract were all significantly lowered (P <0.05); (P < 0.05) of the intermediate dose group of glutamate oxaloacetic acid transaminase in white alchohol extracts.

2) Effect of acute liver injury on liver histopathologic damage in small rats

As a result, hepatocytes were arranged radially around the central vein, hepatocyte colony, hepatic capillaries were arranged regularly, liver lobular structure was complete, In some animal hepatocytes, pathologic changes such as edema of the hardness and necrosis of the stomach were observed. The small rats of the CCL ₄ model group showed that most of the hepatocytes were annular, with turbid edema in the central vein, cytoplasmic swelling, and balloon-shaped deformation. Hepatic cells distributed in the hepatic lobule central vein and hepatic capsule were papillary, pancreatic or necrotic necrosis, accompanied by pathologic changes such as inflammatory cell infiltration. The biphenate group and white liquor extraction and water extraction high dose groups were able to significantly reduce hepatocyte necrosis (P <0.05), indicating that high-dose white sugar alcohols extraction and water extraction groups protect against hepatic damage due to CCL ₄ intraperitoneal injection .

Table 2: Pathological effects of acute liver injury tissues due to CCL ₄ in each experimental group of small rats

Note: The P value is the result of comparing each group with the model group.

3. Experimental Conclusion:

In this experiment, we found that the inhibitory effect of CCl ₄ on the acute liver injury of small rats was significantly inhibited by the extraction of white porcelain alcohol and the high water extract group. In addition, serum glutamate pyruvate transaminase (GPT) and glutamic acid Oxaloacetic acid transaminase (GOT) was lowered to reduce hepatocyte denaturation and necrosis.

Claims (5)

In the treatment of hepatitis in white porcelain,
Wherein the medicament or the health food is a clinically acceptable preparation which is prepared by mixing a white tea extract with a conventional dose of a pharmaceutically acceptable auxiliary material. The method according to claim 1,
Wherein the white raspberry extract is a water extract or an alcohol extract, and wherein the white raspberry extract is a water extract or an alcohol extract. 3. The method of claim 2,
The water extract is prepared by adding 8 to 12 times of water to white porcelain, agitating for 1.5 to 2 hours, adding 5 to 8 times of water to the residue, adding the extract for 1 to 1.5 hours, And then filtering and concentrating the resulting product. 3. The method of claim 2,
The alcohol extract is prepared by adding 75 to 90% ethanol of 8-12 times to white flour, refluxing for 1.5-2 hours, adding 75% ~ 90% of water to the residue, Which comprises collecting the extracts for a period of 1.5 hours, filtering the extracts, and recovering and concentrating the ethanol. The method according to claim 1,
Wherein the preparation is a clinically acceptable granule, capsule, tablet or fabric solution.