TW201907938A - A use of an extract of Asplenium australasicum (J. Sm.) Hook - Google Patents

A use of an extract of Asplenium australasicum (J. Sm.) Hook Download PDF

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TW201907938A
TW201907938A TW106123698A TW106123698A TW201907938A TW 201907938 A TW201907938 A TW 201907938A TW 106123698 A TW106123698 A TW 106123698A TW 106123698 A TW106123698 A TW 106123698A TW 201907938 A TW201907938 A TW 201907938A
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nanyangshan
nanyangshan sushui
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黃昆暄
何淑禎
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景鑫生物科技股份有限公司
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Priority to PCT/US2018/040849 priority patent/WO2019014037A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/11Pteridophyta or Filicophyta (ferns)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/11Pteridophyta or Filicophyta (ferns)
    • A61K36/12Filicopsida or Pteridopsida
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

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Abstract

A use of an extract of Asplenium australasicum (J. Sm.) Hook. in the manufacture of a medicament for treatment of alcoholic hepatitis is disclosed. The extract of Asplenium australasicum (J. Sm.) Hook. is extracted by water at 115-125 DEG C, 0.35-0.5 Kg/cm2G for 1.5-3 hours.

Description

南洋山蘇水萃物的用途  Use of Nanyangshan Sushui Extract  

本發明係關於一種南洋山蘇水萃物的用途,特別關於一種南洋山蘇水萃物應用於製備治療酒精性肝炎的藥物的用途。 The invention relates to the use of a Nanyangshan Sushui extract, in particular to the use of a Nanyangshan Sushui extract for the preparation of a medicament for treating alcoholic hepatitis.

酒精性肝炎(alcoholic hepatitis)係指長期攝取酒精(乙醇)所造成之酒精性肝疾病,主要的臨床症狀為急性黃疸(acute jaundice)、發燒(fever)、體重減輕(weight)等。嚴重的酒精性肝炎患者可能會出現腹水(ascites)及肝腦病變(hepatic encephalopathy)等併發症(complication),甚至導致肝硬化(hepatic cirrhosis)。一般而言,臨床上係以皮質類固醇(corticosteroids)來治療酒精性肝炎的重症患者,然而其試驗結果的變異性大,且無法適用於有腸胃道出血或對類固醇過敏的病人,因此仍需要提供一種南洋山蘇水萃物的用途,以改善前述的問題。 Alcoholic hepatitis refers to alcoholic liver disease caused by long-term intake of alcohol (ethanol). The main clinical symptoms are acute jaundice, fever, weight, and the like. Patients with severe alcoholic hepatitis may experience complications such as ascites and hepatic encephalopathy, and even hepatic cirrhosis. In general, patients with severe cases of alcoholic hepatitis are clinically treated with corticosteroids. However, the variability of the test results is large and cannot be applied to patients with gastrointestinal bleeding or steroid allergy. A use of the Nanyangshan Sushui extract to improve the aforementioned problems.

為解決上述問題,本發明提供一種南洋山蘇水萃物的用途,係將萃取自南洋山蘇之活性成分,應用於製備治療酒精性肝炎的藥物者。 In order to solve the above problems, the present invention provides a use of the Nanyangshan Sushui extract, which is an active ingredient extracted from Nanyangshansu, and is applied to the preparation of a medicament for treating alcoholic hepatitis.

本發明之南洋山蘇水萃物的用途,係應用於製備治療酒精性肝炎的藥物,其中,該南洋山蘇水萃物係水於115~125℃之溫度、0.35~0.5Kg/cm2G之壓力下萃取1.5~3小時所獲得,較佳地,該南洋山蘇水萃物係能夠以口服方式投予一所需個體,且該南洋山蘇水萃物之每天投予該所需個體之劑量為2.5毫升/公斤體重;如此藉由萃取自南洋山蘇之活性成 分,可以降低乙醇所造成之肝功能指數升高的現象及減緩乙醇所造成之肝細胞壞死的現象,因而可以應用於製備治療酒精性肝炎的藥物,為本發明之功效。 The use of the Nanyangshan Sushui extract of the present invention is applied to the preparation of a medicament for treating alcoholic hepatitis, wherein the water of the Nanyangshan Sushui extract is at a temperature of 115 to 125 ° C, 0.35 to 0.5 Kg/cm 2 G. It is obtained by extracting under pressure for 1.5 to 3 hours. Preferably, the Nanyangshan Sushui extract system can be administered orally to a desired individual, and the Nanyangshan Sushui extract is administered to the desired individual daily. The dosage is 2.5 ml/kg body weight; thus, by extracting the active ingredient from Nanyangshansu, the phenomenon of elevated liver function index caused by ethanol and the phenomenon of hepatocyte necrosis caused by ethanol can be reduced, and thus it can be applied. The preparation of a medicament for treating alcoholic hepatitis is the efficacy of the present invention.

第1a圖:試驗(A)中,投予本發明南洋山蘇水萃物對肝功能指數GOT/AST的影響結果。 Fig. 1a: Results of the effect of the Nanyangshan Sushui extract of the present invention on the liver function index GOT/AST in the test (A).

第1b圖:試驗(A)中,投予本發明南洋山蘇水萃物對肝功能指數GPT/ALT的影響結果。 Figure 1b: Results of the effect of the Nanyangshan Sushui extract of the present invention on the liver function index GPT/ALT in the test (A).

第2a~2c圖:試驗(B)中,投予本發明南洋山蘇水萃物對肝細胞壞死的影響結果。 2a~2c: In the test (B), the effect of the Nanyangshan Sushui extract of the present invention on hepatocyte necrosis was administered.

為讓本發明之上述及其他目的、特徵及優點能更明顯易懂,下文特舉本發明之較佳實施例,並配合所附圖式,作詳細說明如下: The above and other objects, features and advantages of the present invention will become more <RTIgt;

本發明所述之「南洋山蘇(Asplenium australasicum(J.Sm.)Hook.)」,係指鐵角蕨科(Aspleniaceae)鐵角蕨屬(Asplenium)的植物,其新生嫩葉(young emerging frond)常被作為食用菜葉。 The " Asplenium australasicum (J.Sm.) Hook."" according to the present invention refers to a plant of the Asplenaceae Asplenium , and its emerging emerging frond. Often used as a edible leaf.

本發明之南洋山蘇水萃物,係可以降低乙醇所造成之肝功能指數升高的現象及減緩乙醇所造成之肝細胞壞死的現象,因而可以應用於製備治療酒精性肝炎的藥物,該南洋山蘇水萃物與醫藥學上可以接受之載劑或賦形劑組合形成一醫藥組合物,其中,該南洋山蘇水萃物係可以製備成任何方便食用之型式,如錠劑、膠囊、粉劑、粒劑或液劑等,或者將該南洋山蘇水萃物與其他食品或飲料組合,以適於食用之樣態供生物體以口服方式服用。 The Nanyangshan Sushui extract of the invention can reduce the phenomenon of elevated liver function index caused by ethanol and slow down the phenomenon of hepatocyte necrosis caused by ethanol, and thus can be applied to preparing a medicament for treating alcoholic hepatitis, the Nanyang The aqueous extract of S. sylvestris is combined with a pharmaceutically acceptable carrier or excipient to form a pharmaceutical composition, wherein the Nanyangshan Sushui extract can be prepared into any convenient form, such as tablets, capsules, Powder, granules or liquid preparations, or the combination of the Nanyangshan Sushui extract with other foods or beverages, for the edible form to be taken orally by the organism.

又,本發明之南洋山蘇水萃物係可以供投予一所需個體,例 如以2.5毫升/公斤體重之劑量投予該所需個體,使該南洋山蘇水萃物係所含有之活性成分得以於該所需個體體內作用,降低乙醇所造成之肝功能指數升高的現象及減緩乙醇所造成之肝細胞壞死的現象。 Further, the Nanyangshan Sushui extract of the present invention can be administered to a desired individual, for example, by administering the desired individual at a dose of 2.5 ml/kg body weight to make the activity of the Nanyangshan Sushui extract system. The ingredients act in the desired individual, reduce the increase in liver function index caused by ethanol and slow down the hepatocyte necrosis caused by ethanol.

其中,該南洋山蘇水萃物較佳係可以藉由一包含以下步驟之方法所製得:提供一南洋山蘇樣品;以水作為一萃取溶劑萃取該南洋山蘇樣品;及將南洋山蘇粗萃液進行濃縮,以獲得該南洋山蘇水萃物。 Wherein, the Nanyangshan Sushui extract can be obtained by a method comprising the steps of: providing a sample of Nanyangshansu; extracting the sample of Nanyangshansu with water as an extraction solvent; and using Nanyangshansu The crude extract is concentrated to obtain the aqueous extract of Nanyangshansu.

詳而言之,該南洋山蘇樣品係可以為南洋山蘇之成熟老葉(三年以上,背面分布孢子),較佳係可以預先將該南洋山蘇樣品於110~120℃之溫度下進行乾燥(將100克南洋山蘇樣品乾燥至20克),得到一南洋山蘇乾燥物;此外,該南洋山蘇樣品亦可以預先碎成粉粒(粒徑約為1~2mm),以增加該南洋山蘇樣品與該萃取溶劑之接觸表面積,藉此提升後續萃取之萃取效率。 In detail, the sample sample of Nanyangshansu may be mature mature leaves of Nanyangshansu (more than three years, spores are distributed on the back), and it is preferable to carry out the sample of Nanyangshansu in advance at a temperature of 110-120 °C. Drying (100 g of Nanyangshansu sample is dried to 20 g) to obtain a dried Nanyangshan Su; in addition, the Nanyangshansu sample can also be pre-crushed into powder (having a particle size of about 1 to 2 mm) to increase the The contact surface area of the Nanyangshansu sample with the extraction solvent, thereby improving the extraction efficiency of the subsequent extraction.

舉例而言,每4.8公斤之南洋山蘇樣品係能夠混合該萃取溶劑,使二者總體積達80公升,並於115~125℃之溫度、0.35~0.5Kg/cm2G之壓力下進行萃取1.5~3小時,上述萃取亦可以重複數次,使該南洋山蘇樣品所富含之活性成分可以完整溶出於該萃取溶劑,此為本發明所屬技術領域中具有通常知識者所廣泛應用,在此不加以贅述。 For example, every 4.8 kg of Nanyangshansu sample can mix the extraction solvent to a total volume of 80 liters, and extract at a temperature of 115-125 ° C and a pressure of 0.35-0.5 Kg/cm 2 G. 1.5~3 hours, the above extraction may also be repeated several times, so that the active ingredient rich in the sample of Nanyangshansu can be completely dissolved in the extraction solvent, which is widely used by those having ordinary knowledge in the technical field of the invention. This will not be repeated.

前述之南洋山蘇粗萃液可以經過減壓濃縮及冷凍乾燥,以獲得該南洋山蘇水萃物,藉由此一程序,係可以使該南洋山蘇水萃物之活性成分更加濃縮,是以僅需使用少量之該南洋山蘇水萃物即可以發揮最佳療效。 The aforementioned Nanyangshan Su crude extract liquid can be concentrated under reduced pressure and freeze-dried to obtain the Nanyangshan Sushui extract. By this procedure, the active ingredient of the Nanyangshan Sushui extract can be more concentrated. The best effect can be achieved by using only a small amount of the Nanyangshan Sushui extract.

為證實本發明之南洋山蘇水萃物係可以降低乙醇所造成之肝功能指數升高的現象及減緩乙醇所造成之肝細胞壞死的現象,遂將每4.8公斤之南洋山蘇樣品萃取所得之南洋山蘇粗萃液,經過減壓濃縮及冷凍乾燥獲得共800克之南洋山蘇水萃物粉末,另將5克之南洋山蘇水萃物粉末 溶於20毫升之水後,進行以下試驗。 In order to confirm that the Nanyangshan Sushui extract of the present invention can reduce the phenomenon of elevated liver function index caused by ethanol and slow down the phenomenon of hepatocyte necrosis caused by ethanol, the 4.8 kg of Nanyangshansu sample is extracted. The Nanyangshan Su crude extract was concentrated under reduced pressure and freeze-dried to obtain a total of 800 g of Nanyangshan Sushui extract powder, and another 5 g of Nanyangshan Sushui extract powder was dissolved in 20 ml of water, and the following test was carried out.

(A)南洋山蘇水萃物對肝功能指數的影響 (A) Effect of extract of Nanyangshan Sushui on liver function index

本試驗係選用雄性Wistar大鼠(200~250g)進行試驗,分別以如第1表所示之南洋山蘇水萃物連續經口灌食各組大鼠4天(每天一次),於第4天經口灌食50%乙醇水溶液,24小時候犧牲各組大鼠,經心臟採血取得血清,以分析各組大鼠的肝功能指數,其結果如第1a、1b圖所示。 In this study, male Wistar rats (200-250 g) were used for the test. The rats in each group were continuously orally administered with the Nanyangshan Sushui extract as shown in Table 1 for 4 days (once a day). Tianjingkou was fed with 50% ethanol aqueous solution. At 24 hours, rats in each group were sacrificed. Serum was collected by cardiac blood sampling to analyze the liver function index of each group of rats. The results are shown in Figures 1a and 1b.

請參照第1a、1b圖所示,濃度為2.5mL/kg的南洋山蘇水萃物可以有效降低乙醇所造成之肝功能指數升高的現象(第A2組)。 Please refer to the figures 1a and 1b. The concentration of 2.5mL/kg of Nanyangshansu water extract can effectively reduce the increase of liver function index caused by ethanol (Group A2).

(B)南洋山蘇水萃物對壞死之肝細胞的影響 (B) Effects of Nanyangshan Sushui extract on necrotic hepatocytes

本試驗同樣選用雄性Wistar大鼠進行試驗,分別以如第2表所示之南洋山蘇水萃物連續經口灌食各組大鼠4天(每天一次),於第4天經口灌食50%乙醇水溶液,24小時候犧牲各組大鼠,收取肝臟後,切片並進行蘇木素-伊紅染色(hematoxylin and eosin stain、H&E stain),結果分別如第2a~2c圖所示。 In this experiment, male Wistar rats were also used for the test. The rats of each group were continuously orally fed for 4 days (once a day) with the Nanyangshan Sushui extract as shown in Table 2, and were orally administered on the 4th day. After 50% ethanol aqueous solution, rats in each group were sacrificed at 24 hours. After receiving liver, sections were sliced and subjected to hematoxylin and eosin stain (H&E stain). The results are shown in Fig. 2a~2c, respectively.

請參照第2b圖所示,經口灌食50%乙醇水溶液之第B1組大鼠之肝臟出現大量空泡;而預先經口灌食濃度為2.5mL/kg的南洋山蘇水萃物之第B2組大鼠之空泡則有減緩的狀況,顯示本發明之南洋山蘇水萃物可以有效減緩乙醇所造成之肝細胞壞死的現象。 Referring to Figure 2b, a large amount of vacuoles appeared in the liver of the B1 group of rats fed orally with 50% ethanol solution; and the extract of Nanyangshan Sushui with a pre-oral feeding concentration of 2.5 mL/kg The vacuoles of the rats in the B2 group were alleviated, indicating that the Nanyangshan Sushui extract of the present invention can effectively alleviate the phenomenon of hepatocyte necrosis caused by ethanol.

綜合上述,本發明之南洋山蘇水萃物的用途係藉由萃取自南洋山蘇之活性成分,可以降低乙醇所造成之肝功能指數升高的現象及減緩乙醇所造成之肝細胞壞死的現象,因而可以應用於製備治療酒精性肝炎的藥物,為本發明之功效。 In summary, the use of the Nanyangshan Sushui extract of the present invention can reduce the phenomenon of elevated liver function index caused by ethanol and slow down the phenomenon of hepatocyte necrosis caused by ethanol by extracting the active ingredient from Nanyangshansu. Therefore, it can be applied to the preparation of a medicament for treating alcoholic hepatitis, which is an effect of the present invention.

雖然本發明已利用上述較佳實施例揭示,然其並非用以限定本發明,任何熟習此技藝者在不脫離本發明之精神和範圍之內,相對上述實施例進行各種更動與修改仍屬本發明所保護之技術範疇,因此本發明之保護範圍當視後附之申請專利範圍所界定者為準。 While the invention has been described in connection with the preferred embodiments described above, it is not intended to limit the scope of the invention. The technical scope of the invention is protected, and therefore the scope of the invention is defined by the scope of the appended claims.

Claims (3)

一種南洋山蘇水萃物的用途,係應用於製備治療酒精性肝炎的藥物,其中,該南洋山蘇水萃物係以水作為一萃取溶劑,於115~125℃之溫度、0.35~0.5Kg/cm 2G之壓力下萃取一南洋山蘇樣品1.5~3小時所獲得。 The invention relates to a medicine for treating alcoholic hepatitis, wherein the Nanyangshan Sushui extract uses water as an extraction solvent at a temperature of 115 to 125 ° C, 0.35 to 0.5 Kg. A sample of Nanyangshansu was extracted under the pressure of /cm 2 G for 1.5 to 3 hours. 如申請專利範圍第1項所述之南洋山蘇水萃物的用途,其中,該南洋山蘇水萃物係以口服方式投予一所需個體。  The use of the Nanyangshan Sushui extract as described in claim 1 wherein the Nanyangshan Sushui extract is administered orally to a desired individual.   如申請專利範圍第2項所述之南洋山蘇水萃物的用途,其中,該南洋山蘇水萃物之每天投予該所需個體之劑量為2.5毫升/公斤體重。  The use of the Nanyangshan Sushui extract as described in claim 2, wherein the Nanyangshan Sushui extract is administered to the desired individual at a dose of 2.5 ml/kg body weight per day.  
TW106123698A 2017-07-14 2017-07-14 A use of an extract of asplenium australasicum (j. sm.) hook. TWI615146B (en)

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TW106123698A TWI615146B (en) 2017-07-14 2017-07-14 A use of an extract of asplenium australasicum (j. sm.) hook.
PCT/US2018/040849 WO2019014037A1 (en) 2017-07-14 2018-07-05 Method for treating alcoholic hepatitis
CN201810763544.1A CN109248180A (en) 2017-07-14 2018-07-12 Application of Nanyang mountain perilla water extract

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