CN111450144A - Application of ficus microcarpa extract in preparation of medicines for preventing and/or treating diabetes and complications thereof - Google Patents
Application of ficus microcarpa extract in preparation of medicines for preventing and/or treating diabetes and complications thereof Download PDFInfo
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Abstract
The invention discloses application of ficus microcarpa extract in preparation of a medicine for preventing and/or treating diabetes and complications thereof, relates to the technical field of medicines, and finds that the ficus microcarpa extract has a very good effect in the aspect of preventing and/or treating the diabetes and the complications thereof. A large amount of scientific researches and creative labor discover that the ficus microcarpa extract has a very good effect on preventing and/or treating diabetes and complications thereof, particularly has a positive curative effect on type II diabetes and complications thereof, has few adverse reactions, is simple and convenient in preparation method, and is suitable for clinical application. The ficus microcarpa extract can be used independently or can be compounded with other active ingredients for use.
Description
Technical Field
The invention relates to the technical field of medicines, in particular to application of ficus microcarpa extracts in preparation of medicines for preventing and/or treating diabetes and complications thereof.
Background
Diabetes mellitus is a group of metabolic syndromes which are caused by multiple causes and are characterized by chronic hyperglycemia, and typical clinical manifestations comprise polydipsia, diuresis, polyphagia and weight loss, gradual weakness, emaciation, long-term blood sugar increase, damage to large blood vessels and micro blood vessels, and damage to heart, brain, kidney, peripheral nerves, eyes, feet and the like, so that multiple organs and multiple systems of the whole body are damaged. According to incomplete statistics, the diabetic complications are more than 100, and are the most known diseases at present. Clinical data show that about 10 years after the onset of diabetes, 30-40% of patients will develop at least one complication, which is more common to diabetic nephropathy, diabetic retinopathy, diabetic foot, diabetic cardiovascular complications, diabetic cerebrovascular disease, diabetic peripheral neuropathy and the like.
With the development of society, the improvement of the substance living level of people and the change of life style, and the gradual progress of China into the aging society, the number of the old people is greatly increased, and the prevalence rate of diabetes in China is increased year by year. Nowadays, the number of diabetics is the first in the world in China. Chinese adult diabetes prevalence is reported to be 11.6%, and pre-diabetic population is reported to be 50.1%. It is estimated that about 1.139 million diabetic patients and 4.934 million people in adults aged 18 years and older in China (mugwort, hui in leaves, forest plum, etc.. advances in the epidemiological study of diabetes [ J ]. New world of diabetes, 2019,28(9): 581) -583.). Diabetes becomes a chronic non-infectious disease which has serious threat to the health of people besides tumor and cardiovascular and cerebrovascular diseases, and the clinical significance of searching for a medicament with positive curative effect on diabetes and complications thereof is important.
Diabetes belongs to endocrine diseases and is divided into I type and II type, the etiology is complex, the morbidity and pathogenesis are not completely clear at present and can not be radically treated, and the treatment method in the prior art is usually the first choice to develop good living habits, control diet, properly exercise, avoid overeating, various induction factors and the like; if the blood sugar can not be controlled, the hypoglycemic drug or the insulin injection needs to be taken according to the advice of doctors, and not few western medicines have better curative effect but few side effects and are not suitable for all patients (Wang Yanmei, research overview of the type 2 diabetes treatment by the traditional Chinese medicine [ J ]. modern distance education of the traditional Chinese medicine in China, 2017,15(20): 154-.
At present, more and more scholars aim at the field of traditional Chinese medicine compound research to discover a novel medicine for treating diabetes. However, the compound Chinese medicine has complex components, inconvenient administration and low recent curative effect.
Ficus microcarpa is a plant of genus Ficus (Ficus microcarpa) of family moraceae, also known as rohdea japonica or Ficus microcarpa, and is mainly distributed in places such as guangdong, guangxi, and Hainan province. The ficus microcarpa is light in taste and cool in nature, has the effects of clearing heat, relieving exterior syndrome, relieving swelling, relieving pain, clearing damp, relieving pain and the like, and the modern pharmacological research finds that the ficus microcarpa contains chemical components such as terpenes, flavones, aliphatic compounds, steroidal compounds and the like, and the asthma and chronic bronchitis therapeutic drug taking the ficus microcarpa extract as a main component has good effects on relieving cough, eliminating phlegm, relieving asthma and the like.
Chinese patent application document CN109419978A discloses a traditional Chinese medicine for treating diabetic kidney diseases, and specifically discloses a traditional Chinese medicine consisting of poria cocos, ricepaper pith, rorippa indica, akebia stem, euphorbia kansui, Chinese lobelia herb, sun euphorbia herb, mole cricket, hiraute shiny bugleweed herb, fringed pink, radix stephaniae tetrandrae, clematis armandii, okra root, day lily, white green leaf, Rohdea japonica Roth root, pea, lysimachia christinae Hance, veronicastrum herb and sunflower stem pith, which can be decocted with water for oral administration and can be used for treating diabetic kidney diseases. The compound is prepared by using different parts of twenty Chinese herbal medicines, the preparation process is complex, and the compound is inconvenient to take because the compound needs to be decocted when being taken.
Disclosure of Invention
The present invention is directed to solving at least one of the problems of the prior art. Therefore, the invention provides the application of the ficus microcarpa extract in preparing the medicines for preventing and/or treating the diabetes and the complications thereof, and the ficus microcarpa extract can be better used for preventing and treating the diabetes and the complications thereof.
The invention also provides a pharmaceutical composition for preventing and/or treating diabetes and complications thereof.
The invention also provides a medicine box for preventing and/or treating diabetes and complications thereof.
According to the use of the embodiment of the first aspect of the invention, the usage of the ficus microcarpa extract in preparing the medicines for preventing and/or treating diabetes and complications thereof.
According to some embodiments of the present invention, the ficus microcarpa extract is an extract obtained by subjecting ficus microcarpa to water extraction and then alcohol extraction.
According to some embodiments of the invention, the ficus microcarpa extract is a ficus microcarpa leaf extract.
According to some embodiments of the invention, the diabetes is type II diabetes.
According to some embodiments of the invention, the complication is at least one selected from the group consisting of: diabetic nephropathy, diabetic ocular complications, diabetic foot, diabetic cardiovascular complications, diabetic cerebrovascular disease, diabetic peripheral neuropathy and diabetic skin disease; the diabetic ocular complication is at least one selected from the group consisting of: diabetic retinopathy, diabetes-associated uveitis, and diabetic cataracts.
According to some embodiments of the present invention, the raw materials for preparing the medicament may further include pharmaceutical excipients. The pharmaceutic adjuvant is a conventional pharmaceutic carrier in the field, and can be any suitable physiologically or pharmaceutically acceptable pharmaceutic adjuvant; preferably, the pharmaceutical excipient is selected from at least one of a disintegrant, a diluent, a lubricant, a binder, a wetting agent, a flavoring agent, a suspending agent, a surfactant, or a preservative; more preferably, the disintegrant is selected from at least one of corn starch, potato starch, crospovidone, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, croscarmellose sodium, carboxymethylcellulose calcium, or alginic acid; more preferably, the diluent is selected from at least one of lactose, sucrose, mannitol, corn starch, potato starch, calcium phosphate, calcium citrate or crystalline cellulose; more preferably, the lubricant is selected from at least one of aerosil, magnesium stearate, calcium stearate, stearic acid, talc or anhydrous silica gel; more preferably, the binder is selected from at least one of acacia, gelatin, dextrin, hydroxypropyl cellulose, methyl cellulose or polyvinylpyrrolidone; more preferably, the wetting agent is selected from sodium lauryl sulfate. The flavoring agent can be at least one of aspartame, stevioside, sucrose, maltitol or citric acid; more preferably, the suspending agent is selected from at least one of acacia, gelatin, methylcellulose, sodium carboxymethylcellulose, hydroxymethylcellulose, or aluminum stearate gel; more preferably, the surfactant is selected from at least one of lecithin, sorbitan monooleate, or glyceryl monostearate; more preferably, the preservative is selected from at least one of methyl paraben or propyl paraben.
According to some embodiments of the present invention, the dosage form of the drug is various dosage forms conventional in the art, preferably in solid, semi-solid or liquid form, and may be an aqueous solution, a non-aqueous solution or a suspension, more preferably a tablet, a capsule, a soft capsule, a granule, a pill, an oral liquid, a dry suspension, a drop pill, a dry extract, an injection or an infusion.
According to some embodiments of the present invention, the mode of administration of the drug may be a mode of administration conventional in the art, including but not limited to injection or oral administration. The injection can be intravenous injection, intramuscular injection, intraperitoneal injection, intradermal injection or subcutaneous injection.
According to some embodiments of the present invention, the preparation method of the ficus microcarpa extract comprises the following steps: the ficus microcarpa is prepared into the ficus microcarpa extract in the form of dry extract. The preparation method of the ficus microcarpa dry extract is not particularly limited, and the preparation method of the ficus microcarpa dry extract recorded in 2015 edition of Chinese pharmacopoeia is preferably adopted.
According to some embodiments of the invention, the preparation method of ficus microcarpa extract comprises the following steps: decocting Ficus microcarpa with water, collecting liquid phase, concentrating, extracting with ethanol, concentrating the ethanol extract, and drying.
According to some embodiments of the invention, the method comprises the steps of:
s1, decocting leaves of Ficus microcarpa in water for more than two times, mixing decoctions, filtering, concentrating the filtrate to obtain fluid extract with a relative density of 1.00-1.20 at 80 ℃, cooling, and adding ethanol to make the ethanol content reach 60%;
s2, standing for more than 12 hours, then filtering, and recovering ethanol from the filtrate;
s3, concentrating to form thick paste with the relative density of 1.10-1.50 at 50 ℃, drying below 80 ℃, and crushing into fine powder to obtain the ficus microcarpa extract.
The use of the medicament prepared according to the invention has at least the following beneficial effects: the invention provides a new application of ficus microcarpa extract in preventing and/or treating diabetes and complications thereof, and the inventor discovers that the ficus microcarpa extract has a very good effect in preventing and/or treating the diabetes and the complications thereof through a large amount of scientific research and creative labor, particularly has a positive curative effect on type II diabetes and complications thereof, has few adverse reactions, is simple and convenient in preparation method, and is suitable for clinical application. The ficus microcarpa extract can be used independently or can be compounded with other active ingredients for use.
According to a second aspect of the present invention, a pharmaceutical composition is provided, comprising ficus microcarpa extract, further comprising an H-receptor blocker; preferably, the H receptor blocker is H1A receptor blocker, preferably, the H receptor blocker is at least one selected from the group consisting of: chlorpheniramine, cetirizine, or loratadine.
According to some embodiments of the invention, the mass ratio of the ficus microcarpa extract to the H-receptor blocker is 50-500: 1; preferably, the mass ratio of the ficus microcarpa extract to the H receptor blocker is 100-300: 1. The invention discovers that the effect of the ficus microcarpa extract and the H receptor blocker after being compounded according to a certain proportion on preventing/treating liver lesion is better than the effect of the ficus microcarpa extract when being used alone to a certain extent, and the scheme of the invention can obtain better treatment effect by using only a very small amount of H receptor blocker, thereby further improving the curative effect of the traditional Chinese medicine and simultaneously reducing the adverse effect brought by the traditional chemical medicine.
Histamine (Histamine) is an autologous active substance, which is produced in vivo by decarboxylation of histidine by histidine decarboxylase and can affect various physiological functions of the body. Histamine activation depends on its corresponding receptor, which has H1、H2、H3And H4The four subtypes, which are involved in the pathogenesis of many diseases, especially allergic diseases, are extremely important factors; therefore, the use of H receptor blockers capable of antagonizing histamine action is also becoming widespread. The research of the invention finds that the H receptor blocker belongs to H in particular1Chlorpheniramine maleate serving as a receptor blocking agent can be compounded with ficus microcarpa extract, and has a very good curative effect on diabetes and complications thereof.
The compositions according to embodiments of the present invention have at least the following benefits: the ficus microcarpa extract can be used as an active ingredient alone or in combination with other active ingredients for preventing and/or treating liver diseases in the using process, and the effect is more obvious after the two are combined.
According to a third aspect the invention relates to a kit comprising: preparations containing ficus microcarpa extract and preparations containing an H receptor blocker; wherein, the content of ficus microcarpa extract and H receptor blocker in the medicine box is prepared according to the daily dosage standard as follows: ficus microcarpa extract: 0.2-2.0 g/day; h receptor blockers: 2-6 mg/day.
The term "administered dose" as used herein is an amount capable of alleviating or delaying the progression of a disease, degenerative or injurious condition. Depending on the particular disease being treated, as well as other factors including age, weight, health, severity of symptoms, route of administration, frequency of treatment, and whether other medications are concomitant during treatment.
The term "prevention" as used herein means preventing or reducing the development of diabetes and its complications after use in the presence of possible diabetic factors.
The term "treating" as used herein means to reduce the extent of, or cure to normalize, or slow the progression of diabetes and its complications.
Additional aspects and advantages of the invention will be set forth in part in the description which follows and, in part, will be obvious from the description, or may be learned by practice of the invention.
Detailed Description
In order to explain the technical content, the objects and the effects of the present invention in detail, the following description will be given with reference to the embodiments. The test methods used in the examples are all conventional methods unless otherwise specified; the materials, reagents and the like used are commercially available reagents and materials unless otherwise specified.
The first embodiment of the invention is as follows: a preparation method of a medicine for preventing and/or treating diabetes and complications thereof comprises the following steps:
s1, taking dry leaves of Ficus microcarpa, decocting in water twice, mixing decoctions, filtering, concentrating the filtrate to fluid extract with relative density of about 1.1 at 80 deg.C, cooling, and adding ethanol to make ethanol content reach 60%.
S2, standing for more than 12 hours, then filtering, and recovering ethanol from the filtrate. Concentrating to obtain soft extract with relative density of 1.30 at 50 deg.C, drying below 80 deg.C, and pulverizing into fine powder to obtain Ficus microcarpa dry extract.
S3, suspending the dry extract prepared by the above steps in 1% (w/w) sodium carboxymethyl cellulose solution to obtain the finished product.
The second embodiment of the invention is as follows: a pharmaceutical composition for preventing and/or treating diabetes and its complications comprises Ficus microcarpa dry extract (prepared by S2 of example 1) and chlorphenamine maleate, and is prepared by mixing Ficus microcarpa dry extract and chlorphenamine maleate at ratio of 90:0.2 (or 450: 1), and suspending in 1% (w/w) sodium carboxymethylcellulose solution.
The third embodiment of the invention is as follows: a pharmaceutical composition for preventing and/or treating diabetes and its complications comprises Ficus microcarpa dry extract (prepared according to method S2 in example 1) and cetirizine, and is prepared by mixing Ficus microcarpa dry extract and cetirizine at a ratio of 450:1, and suspending in 1% (w/w) sodium carboxymethylcellulose solution.
The fourth embodiment of the invention is as follows: a pharmaceutical composition for preventing and/or treating diabetes and its complications comprises Ficus microcarpa dry extract (prepared according to method S2 in example 1) and loratadine, and is prepared by mixing Ficus microcarpa dry extract and loratadine at a ratio of 450:1, and suspending in 1% (w/w) sodium carboxymethylcellulose solution.
The first comparative example of the invention is as follows: a medicine for preventing and/or treating liver diseases is metformin.
The second comparative example of the present invention is: a medicine for preventing and/or treating liver diseases is prepared by decocting Rohdea japonica Roth in water according to CN109419978A example 1, filtering, collecting filtrate, and concentrating to obtain extract. Suspended in a 1% (w/w) sodium carboxymethylcellulose solution.
The application of the drugs or drug compositions prepared in the above examples 1 to 4 and comparative examples 1 to 2 to the treatment effect of diabetes and complications thereof was verified, and the specific examples are as follows:
(Mono) alloxan-induced treatment of diabetes
1. Experimental methods
1.1 establishment of rat diabetes model
The method is characterized in that 105 male rats with the body weight of 120 Wistar male rats of 6 weeks with similar body weight are fed adaptively for 1 week, and are randomly selected for molding, before molding, 120 rats are fasted for 16h, and Fasting Blood Glucose (FBG) is measured before tail vein blood sampling, wherein the molding method comprises the steps of intraperitoneal injection of alloxan according to the dose of 155mg/kg, after 5 days, the fasting for 16h is carried out for re-measurement of the FBG, the FBG is determined to be successful at the time of molding, and the FBG is not less than 14 mmol/L, and the rest 15 male rats are injected with physiological saline with the same amount and are set as normal.
1.2 pharmaceutical intervention
The rats successfully molded were randomly divided into 15 rats each (105 rats were successfully molded) in the model group, the control example group, the example three group and the example four group, and the drug administration was started at 2d after the molding, 1 time per day for 4 weeks.
Of these, the control group was given 2ml of 200mg/kg BW metformin (metformin tablets suspended in 1% sodium carboxymethylcellulose solution); the control group was administered 2ml of the extract of Rohdea japonica Roth with a crude drug amount of 1.3g/kg BW; example group 2ml of ficus microcarpa extract (the ficus microcarpa dry extract prepared in example 1 was suspended in 1% sodium carboxymethylcellulose solution) with 90mg/kg BW; example two groups were given 2ml of Ficus microcarpa extract at 90mg/kg BW and chlorpheniramine maleate at 0.2mg/kg BW; example three groups were given 2ml of ficus microcarpa extract at 90mg/kg BW and cetirizine at 0.2mg/kg BW; example four groups were given 2ml of ficus microcarpa extract at 90mg/kg BW and loratadine at 0.2mg/kg BW; the normal group and the model group were given an equivalent amount of 1% sodium carboxymethylcellulose solution.
1.3 measurement of index
(1) Observing the general condition of the rat in the experimental process;
(2) after the experiment is finished, fasting is carried out for 16h, and FBG is measured;
(3) following FBG measurement, rats were gavaged with glucose at a 2g/kg BW dose for glucose tolerance measurements at 0 (i.e., FBG), 30, 60, 90 and 120 min.
2. Results of the experiment
2.1 general status comparison of rats
The rats in the normal group have smooth hair color, good spirit, free movement, quick response, smooth breathing, normal food intake and water drinking, obviously increased body mass along with the prolonging of the feeding time and no death. The rats in the model group and the rats in the control example have dry hair, obviously increased diet and water intake, gradually reduced weight and obviously moist padding. The conditions of the rats in the control group and the rats in the examples 1 to 4 are obviously improved compared with those in the model group and the control group.
2.2 comparison of FBG groups
FBG was measured for each group and the test results are shown in table 1:
table 1 comparison of FBGs in each group (mmol/L, n 15)
| Group of | Before treatment | After treatment |
| Normal group | 5.95±0.33* | 5.90±0.42* |
| Model set | 22.79±3.20 | 22.48±4.24 |
| Control example group | 22.53±4.21 | 12.16±1.32* |
| Two groups of comparison examples | 22.18±6.48 | 21.43±5.32 |
| Group of embodiments | 22.61±6.74 | 15.83±2.04* |
| Two groups of embodiments | 22.90±4.32 | 13.71±1.25*# |
| Example three groups | 22.08±5.53 | 14.08±3.26*# |
| Example four groups | 21.96±4.57 | 14.50±2.24*# |
Note: comparison with model group<0.05; two groups of examples, three groups of examples and four groups of examples are compared with one group of examples,#P<0.05。
as can be seen from table 1, FBG was significantly increased in the model group rats compared to the normal group (P <0.05), indicating that animal molding was successful. Compared with the model group, the two groups of FBGs in the comparison example have no obvious change; FBG was significantly reduced (P <0.05) in the control group, the example two groups, the example three groups, and the example four groups given drug treatment, and significantly lower (P <0.05) in the example two groups, the example three groups, and the example four groups.
2.3 comparison of glucose tolerance results for each group
After the initial FBG measurement, 2g/kg BW glucose was orally administered, and the glucose tolerance of each group of rats was measured, the results are shown in the following Table 2:
table 2 comparison of blood glucose measurements at different time points (mmol/L, n 15)
| Group of | 0min | 30min | 60min | 90min | 120min |
| Normal group | 5.90±0.42* | 12.50±1.94* | 8.73±1.39* | 6.43±1.21* | 6.05±0.92* |
| Model set | 22.48±4.24 | 32.31±3.22 | 29.83±5.18 | 27.30±4.09 | 25.78±5.21 |
| Control example group | 12.16±1.32* | 26.06±6.14* | 24.31±2.34* | 19.51±2.92* | 16.41±2.05* |
| Two groups of comparison examples | 21.43±5.32 | 30.78±6.09 | 28.46±7.09 | 26.66±4.35 | 24.35±4.10 |
| Group of embodiments | 15.83±2.04* | 29.49±3.82* | 27.14±4.27* | 23.45±2.17* | 18.74±1.13* |
| Two groups of embodiments | 13.71±1.25*# | 25.93±4.59*# | 25.55±2.33*# | 21.65±3.30*# | 17.70±1.37*# |
| Example three groups | 14.08±3.26*# | 26.43±5.08*# | 26.80±3.17*# | 21.80±3.09*# | 18.01±1.21*# |
| Two groups of embodiments | 14.50±2.24*# | 27.11±4.32*# | 25.83±4.88*# | 22.03±4.55*# | 17.26±3.04*# |
Note: comparison with model group<0.05; two groups of examples, three groups of examples and four groups of examples are compared with one group of examples,#P<0.05。
as can be seen from table 2, blood glucose peaks at 30min for each group of rats and subsequently decreases; the normal group of rats had substantially decreased to the initial level 90 min; the remaining groups remained high for 120 min. The blood glucose values at the time points of the model group and the control example group were the highest, the blood glucose values of the other administration groups were significantly lower than the model group (P <0.05), and the blood glucose values of the example two groups, the example three groups, and the example four groups were significantly lower than the blood glucose values of the example one group (P < 0.05).
In conclusion, compared with the prior art, the scheme of the embodiment of the invention can obviously improve the fasting blood glucose of the type 2 diabetes model rat, inhibit the rise of the blood glucose after glucose is orally taken, and improve the tolerance degree of the rat to the glucose no matter the extract is independently used as an active ingredient and compounded with other active ingredients, which shows that the ficus microcarpa extract has a very good treatment effect when being used as an active ingredient for treating type II diabetes.
Streptozotocin-induced diabetes treatment
1. Experimental methods
1.1 establishment of rat diabetes model
The method is characterized in that 120 Wistar male rats with similar body weights and 6 weeks old are fed adaptively for 1 week, 105 male rats are randomly selected for molding, before molding, the 120 male rats are fasted for 16h, and the Fasting Blood Glucose (FBG) is determined firstly after tail vein blood sampling.
1.2 pharmaceutical intervention
The rats successfully molded were randomly divided into 15 rats in each of the model group, the control group, the example two groups, the example three groups and the example four groups (105 rats were successfully molded), and the drug administration was started at 2d after molding, 1 time per day for 4 weeks.
Of these, the control group was given 2ml of 200mg/kg BW metformin (metformin tablets suspended in 1% sodium carboxymethylcellulose solution); the control group was administered 2ml of Rohdea japonica Roth extract with a crude drug amount of 1.3g/kg BW; example group 2ml of ficus microcarpa extract dosed 90mg/kg BW; example two groups were given 2ml of Ficus microcarpa extract at 90mg/kg BW and chlorpheniramine maleate at 0.2mg/kg BW; example three groups were given 2ml of ficus microcarpa extract at 90mg/kg BW and cetirizine at 0.2mg/kg BW; example four groups were given 2ml of ficus microcarpa extract at 90mg/kg BW and 0.2mg/kg BW loratadine; the normal group and the model group were given an equivalent amount of 1% sodium carboxymethylcellulose solution.
1.3 measurement of index
(1) Observing the general condition of the rat in the experimental process;
(2) after the experiment is finished, fasting is carried out for 16h, and FBG is measured;
(3) detection of retinopathy: the slit lamp detects the retinopathy and lenticular opacity of the rat, and the pathological degree is scored as follows, wherein the score is 0: the fundus is normal, and the optic nerve disc and the large and small blood vessels are all clearly visible; 1 minute: the crystals are slightly turbid, the number of blood vessels is less than that of the normal fundus, and only small blood vessels are invisible; and 2, dividing: the crystals were moderately turbid, with major vessels and optic disc clearly visible, but large and small vessels not visible; and 3, dividing: the crystals are more turbid, the major vessels and the optic disc are slightly visible, and the large and small vessels are completely invisible; and 4, dividing: severe crystal turbidity, blurred optic disc in fundus images.
(4) Detection of renal function: collecting blood from orbital venous plexus, and detecting the content of Creatinine (CRE) and urea nitrogen (BUN).
2. Results of the experiment
2.1 general status comparison of rats
The rats in the normal group have smooth hair color, good spirit, free movement, quick response, smooth breathing, normal food intake and water drinking, obviously increased body mass along with the prolonging of the feeding time and no death. The rats in the model group and the rats in the control example have obviously increased diet and water intake, gradually reduced weight and obviously moist bedding. The conditions of rats in the control example group, the example two groups, the example three groups and the example four groups are obviously improved compared with those of the model group.
2.2 comparison of FBG groups
The FBG test results for each group are shown in table 3 below:
table 3 comparison of the FBGs (mmol/L, n 15)
| Group of | Before treatment | After treatment |
| Normal group | 6.02±0.55 | 5.88±0.34* |
| Model set | 25.90±4.35 | 26.43±3.81 |
| Control example group | 25.98±2.64 | 15.74±2.02* |
| Two groups of comparison examples | 26.22±4.06 | 25.77±5.09 |
| Group of embodiments | 26.06±6.92 | 18.86±3.36* |
| Two groups of embodiments | 25.94±3.76 | 17.01±2.19*# |
| Example three groups | 26.23±5.80 | 16.80±4.31*# |
| Example four groups | 26.45±7.14 | 16.45±5.10*# |
Note: comparison with model group<0.05; two groups of examples, three groups of examples and four groups of examples are compared with one group of examples,#P<0.05。
as can be seen from table 3 above, FBG of the model group rat is significantly increased (P <0.05) compared to the normal group, indicating that animal modeling is successful. Compared with the model group, the two groups of FBGs in the comparison example have no obvious change; FBG was significantly reduced (P <0.05) in the control group, the example two groups, the example three groups, and the example four groups given drug treatment, and significantly lower (P <0.05) in the example two groups, the example three groups, and the example four groups.
2.3 comparison of retinopathy scores for groups
The results of the retinopathy scores for each group are shown in table 4 below:
table 4 comparison of retinopathy scores for each group (
Minute)
Note: comparison with model group<0.05; two groups of examples, three groups of examples and four groups of examples are compared with one group of examples,#P<0.05。
as can be seen from Table 4, the model group rats were crystallographically turbid and had severe retinopathy (P <0.05) compared to the normal group. There was no significant improvement in the two groups of control examples compared to the model group, with the remaining drug-treated groups of control example, and example four having significantly reduced retinopathy scores (P <0.05), and with the groups of example, and example four having significantly lower scores (P < 0.05).
2.4 renal function comparison of groups
The results of the renal function index tests for each group are shown in table 5 below:
table 5 comparison of renal function after treatment (n ═ 15)
| Group of | CRE(μmol/L) | BUN(mmol/L) |
| Normal group | 25.63±3.21* | 4.24±0.27* |
| Model set | 83.37±10.48 | 10.10±2.21 |
| Control example group | 56.48±8.63* | 7.77±1.32* |
| Two groups of comparison examples | 81.25±11.23 | 9.89±2.06 |
| Group of embodiments | 64.88±4.62* | 8.47±1.40* |
| Two groups of embodiments | 54.28±4.70*# | 7.37±0.88*# |
| Example three groups | 57.60±6.27*# | 7.26±1.20*# |
| Example four groups | 59.40±8.42*# | 7.10±0.91*# |
Note: comparison with model group<0.05; two examples and three examplesGroup, example four groups were compared to one group of examples,#P<0.05。
as can be seen from Table 5, the CRE and BUN content in the model group rats was significantly increased (P <0.05) compared to the normal group, indicating that the animals had impaired renal function. Compared with the model group, the values of the two groups of the control example are not obviously changed, the CRE and BUN contents of the group of the control example, the group of the example, the two groups of the example, the group of the example and the group of the example are obviously reduced (P <0.05), and the CRE and BUN contents of the group of the example, the group of the example and the group of the example are obviously lower than that of the group of the example (P < 0.05).
In conclusion, the ficus microcarpa extract obtained by water extraction and ethanol extraction can obviously reduce the blood sugar of model rats, improve retinopathy and reduce the contents of CRE and BUN in animal serum; however, the effect is not observed in the two groups of the comparison examples, which shows that compared with the prior art, the ficus microcarpa extract obtained by water extraction and alcohol extraction in the embodiment of the invention has obvious effect of reducing blood sugar, and has very good treatment effect on diabetes, diabetic retinopathy and diabetic nephropathy. In addition, the curative effect can be further improved after the ficus microcarpa extract is compounded with chlorphenamine maleate, cetirizine and loratadine.
The above description is only an embodiment of the present invention, and not intended to limit the scope of the present invention, and all equivalent modifications made by the present invention in the specification or directly or indirectly applied to the related technical field are included in the scope of the present invention.
Claims (10)
1. Application of ficus microcarpa extract in preparing medicine for preventing and/or treating diabetes and complications thereof is provided.
2. Use according to claim 1, characterized in that: the ficus microcarpa extract is a ficus microcarpa leaf extract.
3. Use according to claim 1, characterized in that: the diabetes is type II diabetes.
4. Use according to claim 1, characterized in that: the complication is at least one selected from the group consisting of: diabetic nephropathy, diabetic ocular complications, diabetic foot, diabetic cardiovascular complications, diabetic cerebrovascular disease, diabetic peripheral neuropathy and diabetic skin disease; the diabetic ocular complication is at least one selected from the group consisting of: diabetic retinopathy, diabetes-associated uveitis, and diabetic cataracts.
5. Use according to claim 1, characterized in that: the raw materials for preparing the medicine also comprise pharmaceutic adjuvants; preferably, the pharmaceutical excipient is selected from at least one of a disintegrant, a diluent, a lubricant, a binder, a wetting agent, a flavoring agent, a suspending agent, a surfactant, or a preservative; more preferably, the disintegrant is selected from at least one of corn starch, potato starch, crospovidone, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, croscarmellose sodium, carboxymethylcellulose calcium, or alginic acid; more preferably, the diluent is selected from at least one of lactose, sucrose, mannitol, corn starch, potato starch, calcium phosphate, calcium citrate or crystalline cellulose; more preferably, the lubricant is selected from at least one of aerosil, magnesium stearate, calcium stearate, stearic acid, talc or anhydrous silica gel; more preferably, the binder is selected from at least one of acacia, gelatin, dextrin, hydroxypropyl cellulose, methyl cellulose or polyvinylpyrrolidone; more preferably, the wetting agent is selected from sodium lauryl sulfate; more preferably, the flavoring agent is at least one of aspartame, stevioside, sucrose, maltitol, or citric acid; more preferably, the suspending agent is selected from at least one of acacia, gelatin, methylcellulose, sodium carboxymethylcellulose, hydroxymethylcellulose, or aluminum stearate gel; more preferably, the surfactant is selected from at least one of lecithin, sorbitan monooleate, or glyceryl monostearate; more preferably, the preservative is selected from at least one of methyl paraben or propyl paraben.
6. Use according to claim 1, characterized in that: the dosage form of the medicament is in a solid, semi-solid or liquid form; preferably an aqueous solution, non-aqueous solution or suspension; more preferably tablet, capsule, soft capsule, granule, pill, oral liquid, dry suspension, dripping pill, dry extract, injection or infusion.
7. A pharmaceutical composition for preventing and/or treating diabetes and its complications, characterized in that: comprises ficus microcarpa extract and also comprises an H receptor blocker.
8. The pharmaceutical composition for the prevention and/or treatment of diabetes and its complications according to claim 7, characterized in that: the H receptor blocker is H1A receptor blocker, preferably, the H receptor blocker is at least one selected from the group consisting of: chlorpheniramine, cetirizine, or loratadine.
9. The composition of claim 7, wherein: the mass ratio of the ficus microcarpa extract to the H receptor blocker is 50-500: 1; preferably, the mass ratio of the ficus microcarpa extract to the H receptor blocker is 100-300: 1.
10. A kit for the prevention and/or treatment of diabetes and its complications, characterized in that: the kit comprises: preparations containing ficus microcarpa extract and preparations containing an H receptor blocker; wherein, the content of ficus microcarpa extract and H receptor blocker in the medicine box is prepared according to the daily dosage standard as follows: ficus microcarpa extract: 0.2-2.0 g/day; h receptor blockers: 2-6 mg/day.
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| CN102342977A (en) * | 2011-07-15 | 2012-02-08 | 吉林敖东集团大连药业股份有限公司 | Keteling capsule and preparation method thereof |
| CN102949456A (en) * | 2011-08-30 | 2013-03-06 | 江守训 | Preparation method of ficus microcarpa extract and medicament or wound binder for promoting wound healing |
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| CN102342977A (en) * | 2011-07-15 | 2012-02-08 | 吉林敖东集团大连药业股份有限公司 | Keteling capsule and preparation method thereof |
| CN102949456A (en) * | 2011-08-30 | 2013-03-06 | 江守训 | Preparation method of ficus microcarpa extract and medicament or wound binder for promoting wound healing |
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