TWI612967B - 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 PDFInfo
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- 239000000284 extract Substances 0.000 title claims abstract description 42
- 241001312267 Asplenium australasicum Species 0.000 title description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 21
- 239000000126 substance Substances 0.000 claims abstract description 14
- 206010067125 Liver injury Diseases 0.000 claims abstract description 11
- 238000000605 extraction Methods 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 9
- 231100000753 hepatic injury Toxicity 0.000 claims abstract description 9
- 239000002904 solvent Substances 0.000 claims abstract description 6
- 229940079593 drug Drugs 0.000 claims abstract description 5
- 241001092389 Sorbaria Species 0.000 claims abstract 7
- 230000037396 body weight Effects 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 27
- 230000003908 liver function Effects 0.000 description 11
- 235000004347 Perilla Nutrition 0.000 description 10
- 241000229722 Perilla <angiosperm> Species 0.000 description 10
- 210000003494 hepatocyte Anatomy 0.000 description 8
- 230000017074 necrotic cell death Effects 0.000 description 8
- 241000700159 Rattus Species 0.000 description 7
- 210000004185 liver Anatomy 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 235000002634 Solanum Nutrition 0.000 description 4
- 241000207763 Solanum Species 0.000 description 4
- 241000219784 Sophora Species 0.000 description 4
- 208000006454 hepatitis Diseases 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 239000003053 toxin Substances 0.000 description 4
- 231100000765 toxin Toxicity 0.000 description 4
- 108700012359 toxins Proteins 0.000 description 4
- 244000068988 Glycine max Species 0.000 description 3
- 235000010469 Glycine max Nutrition 0.000 description 3
- 239000000287 crude extract Substances 0.000 description 3
- 231100000283 hepatitis Toxicity 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- WZUVPPKBWHMQCE-UHFFFAOYSA-N Haematoxylin Chemical compound C12=CC(O)=C(O)C=C2CC2(O)C1C1=CC=C(O)C(O)=C1OC2 WZUVPPKBWHMQCE-UHFFFAOYSA-N 0.000 description 2
- 241000700157 Rattus norvegicus Species 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 239000002360 explosive Substances 0.000 description 2
- 231100000234 hepatic damage Toxicity 0.000 description 2
- 230000008818 liver damage Effects 0.000 description 2
- 230000001338 necrotic effect Effects 0.000 description 2
- 239000004006 olive oil Substances 0.000 description 2
- 235000008390 olive oil Nutrition 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 210000003462 vein Anatomy 0.000 description 2
- 241000134854 Aspleniaceae Species 0.000 description 1
- 241001453169 Asplenium Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 231100000354 acute hepatitis Toxicity 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 238000003763 carbonization Methods 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- YQGOJNYOYNNSMM-UHFFFAOYSA-N eosin Chemical compound [Na+].OC(=O)C1=CC=CC=C1C1=C2C=C(Br)C(=O)C(Br)=C2OC2=C(Br)C(O)=C(Br)C=C21 YQGOJNYOYNNSMM-UHFFFAOYSA-N 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000005229 liver cell Anatomy 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 230000007102 metabolic function Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/11—Pteridophyta or Filicophyta (ferns)
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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Abstract
一種南洋山蘇水萃物的用途，係用以製備防治化學性肝損傷的藥物，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/cm2G之壓力下萃取一南洋山蘇樣品1.5~3小時所獲得。 A use of Nanyang Mountain Sorbaria extract for preparing medicines for preventing and treating chemical liver injury, wherein the Nanyang Mountain Soak extract uses water as an extraction solvent at a temperature of 115-125 ° C, 0.35 ~ 0.5 It was obtained by extracting a sample of Nanyangshansu under the pressure of Kg / cm 2 G for 1.5 ~ 3 hours.
Description
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防治化學性肝損傷的藥物的用途。 The present invention relates to the use of a water extract from Nanyang Mountain Perilla, and more particularly to the use of a water extract from Nanyang Mountain Perilla to prepare a medicine for preventing and treating chemical liver injury.
肝臟為人體中以代謝功能為主的器官，並扮演去除毒素的角色。當人體接觸化學毒素時，化學毒素會被運送到肝臟以進行代謝，然而大量的化學毒素的累積卻會造成化學性肝損傷，而使人體出現急性肝炎(acute hepatitis)甚或猛爆性肝炎(fulminant hepatitis)等症狀。 The liver is the body's main organ with metabolic functions and plays a role in removing toxins. When the human body comes into contact with chemical toxins, the chemical toxins will be transported to the liver for metabolism. However, the accumulation of a large amount of chemical toxins will cause chemical liver damage, which will cause acute hepatitis or fulminant in the human body. hepatitis) and other symptoms.
猛爆性肝炎係指肝功能突然的嚴重喪失，目前認定以肝臟移植為最佳的治療方法，惟捐贈之肝臟取得不易，且手術後常見合併禁忌症，因此仍以防治化學性肝損傷，進而避免猛爆性肝炎的發生為第一手段。 Explosive hepatitis refers to the sudden and severe loss of liver function. Currently, liver transplantation is considered to be the best treatment method. However, donated liver is not easy to obtain, and contraindications are common after surgery. Therefore, it is still used to prevent chemical liver damage. Avoiding the occurrence of explosive hepatitis is the first resort.
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，應用於製備防治化學性肝損傷的藥物者。 In order to solve the above problems, the present invention provides the use of a water extract of Nanyang Mountain Perilla, which is an active ingredient extracted from Nanyang Mountain Perilla, and is used to prepare a drug for preventing and treating chemical liver injury.
本發明之南洋山蘇水萃物的用途，係應用於製備防治化學性肝損傷的藥物，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2~6毫升/公斤體重；如此藉由萃取自南洋山蘇之活性成分，可以降低四氯化碳所造成之肝功能指數升高的現象及減緩四氯化 碳所造成之肝細胞壞死的現象，因而可以應用於製備防治化學性肝損傷的藥物，為本發明之功效。 The use of the Nanyang Mountain Perilla water extract is used for preparing medicine for preventing and treating chemical liver injury. The Nanyang Mountain Perilla water is at a temperature of 115-125 ° C and 0.35 ~ 0.5Kg / cm 2. It is obtained by extracting under the pressure of G for 1.5 ~ 3 hours. Preferably, the Nanyang Mountain Sophora extract can be administered orally to a desired individual, and the Nanyang Mountain Sophora extract is administered daily to the required The dosage of the individual is 2 ~ 6 ml / kg body weight; in this way, the active ingredient extracted from Nanyangshansu can reduce the increase of liver function index caused by carbon tetrachloride and slow the liver caused by carbon tetrachloride. The phenomenon of cell necrosis can therefore be applied to the preparation of a medicament for preventing and treating chemical liver injury, which 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: In the test (A), the effect of administering the water extract of Nanyang Mountain Solanum officinalis according to the present invention on the liver function index GOT / AST.
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。 Fig. 1b: In the test (A), the effect of administering the water extract of Nanyang Mountain Solanum officinalis according to the present invention on the liver function index GPT / ALT.
第2a~2d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。 Figures 2a to 2d: In the test (B), the effect of administering the water extract of Nanyang Mountain Solanum officinalis according to the present invention on hepatocyte necrosis.
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：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。 In order to make the above and other objects, features, and advantages of the present invention more comprehensible, the following describes the preferred embodiments of the present invention and the accompanying drawings in detail, as follows: "Su ( Asplenium australasicum (J.Sm.) Hook.)" Refers to a plant of the genus Asplenium of the Aspleniaceae family, and its young emerging frond is often used as a vegetable leaf.
本發明之南洋山蘇水萃物，係可以降低四氯化碳所造成之肝功能指數升高的現象及減緩四氯化碳所造成之肝細胞壞死的現象，因而可以應用於製備防治化學性肝損傷的藥物，因而可以應用於製備防治化學性肝損傷的藥物，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 water extract of Nanyang Mountain Solanum according to the present invention can reduce the phenomenon of increasing liver function index caused by carbon tetrachloride and slow down the phenomenon of hepatocyte necrosis caused by carbon tetrachloride, so it can be used for preparing chemical properties Medicine for liver injury can be used to prepare medicine for prevention and treatment of chemical liver injury. The Nanyangshan sour water extract is combined with a pharmaceutically acceptable carrier or excipient to form a pharmaceutical composition, wherein the Nanyangshan The sour extract can be prepared into any convenient form, such as lozenges, capsules, powders, granules, or liquids, etc., or the Nanyangshan sour extract can be combined with other foods or beverages to be suitable for consumption. The state is for the organism to take orally.
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2~6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，而可以降低四氯化碳所造成之肝功能指數升高的現象及減緩四氯化碳所造成之肝細胞壞死的現象。 In addition, the Nanyang Mountain Sophora extract system of the present invention can be administered to a desired individual, for example, at a dose of 2 to 6 ml / kg body weight, the desired body is administered to the Nanyang Mountain Sophora extract The contained active ingredients can act in the body of the required individual, and can reduce the phenomenon of liver function index increase caused by carbon tetrachloride and slow the phenomenon of hepatocyte necrosis caused by carbon tetrachloride.
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。 Among them, the Nanyangshansu water extract is preferably prepared by a method including the following steps: providing a Nanyangshansu sample; using water as an extraction solvent to extract the Nanyangshansu sample; and The crude extract was concentrated to obtain the Nanyangshansu extract.
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 Nanyangshansu sample can be the mature old leaves of Nanyangshansu (more than three years, with spores distributed on the back). Preferably, the Nanyangshansu sample can be processed in advance at a temperature of 110 ~ 120 ° C. Drying (drying 100g Nanyangshansu sample to 20g) to obtain a dried Nanyangshansu sample; In addition, the Nanyangshansu sample can also be crushed into powder particles (particle size about 1 ~ 2mm) in advance to increase the The contact surface area of the Nanyang Shansu sample and the extraction solvent improves the extraction efficiency of 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 be mixed with the extraction solvent so that the total volume of the two reaches 80 liters, and the extraction is performed at a temperature of 115 to 125 ° C and a pressure of 0.35 to 0.5 kg / cm 2 G The above extraction can be repeated several times for 1.5 ~ 3 hours, so that the active ingredients contained in the Nanyangshansu sample can be completely dissolved in the extraction solvent. This is widely used by those with ordinary knowledge in the technical field to which this invention belongs. This will not be repeated here.
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 crude extract of Nanyang Mountain Perilla can be concentrated under reduced pressure and freeze-dried to obtain the Nanyang Mountain Perilla water extract. With this procedure, the active ingredients of the Nanyang Perilla water extract can be more concentrated. Therefore, only a small amount of the Nanyangshan sour water extract can be used to achieve the best effect.
為證實本發明之南洋山蘇水萃物係可以降低四氯化碳所造成之肝功能指數升高的現象及減緩四氯化碳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 extract of Nanyang mountain sour extract of the present invention can reduce the phenomenon of liver function index increase caused by carbon tetrachloride and slow the phenomenon of hepatocyte necrosis caused by carbon tetrachloride, the amount of Nanyang per 4.8 kg The crude extract of Nanyang Mountain Soya extract obtained from the extraction of Sansu samples was concentrated under reduced pressure and freeze-dried to obtain a total of 800 grams of Nanyang Mountain Soya extract powder, and 5 grams of Nanyang Mountain Soya extract powder was dissolved in 20 ml of water. Perform the following tests.
(A)南洋山蘇水萃物對肝功能指數的影響 (A) Effect of extract from Nanyang Mountain Soda 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天以腹腔注射四氯化碳(溶於橄欖油中，濃度為20%)，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。 This test was performed on male Wistar rats (200-250g). The rats of each group were continuously orally administered with the water extract of Nanyang Mountain as shown in Table 1 for 4 days (once a day). Tian was injected intraperitoneally with carbon tetrachloride (dissolved in olive oil at a concentration of 20%). Rats of each group were sacrificed at 24 hours, and blood was collected from the heart to obtain serum. The liver function index of each group of rats was analyzed. 1a, 1b.
請參照第1a、1b圖所示，濃度為2~6mL/kg的南洋山蘇水萃物可以有效降低四氯化碳所造成之肝功能指數上升的問題(第A2、A3組)。 Please refer to Figures 1a and 1b. The concentration of 2 ~ 6mL / kg Nanyangshansu extract can effectively reduce the increase in liver function index caused by carbon tetrachloride (Groups A2 and A3).
(B)南洋山蘇水萃物對壞死之肝細胞的影響 (B) Effect of Nanyang Mountain Soda 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天以腹腔注射四氯化碳(溶於橄欖油中，濃度為20%)，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~2d圖所示。 In this test, male Wistar rats were also selected. The rats of each group were continuously orally administered with the water extract of Nanyang Mountain as shown in Table 2 for 4 days (once a day). Carbon chloride (dissolved in olive oil at a concentration of 20%). Rats in each group were sacrificed at 24 hours. After the liver was collected, the sections were sliced and hematoxylin and eosin stain (H & E stain) were obtained. 2a ~ 2d.
請參照第2b圖所示，經四氯化碳處理之第B1組大鼠之肝臟的中央靜脈(Central Venous，簡稱CV)附近肝細胞壞死，整體組織結構紊亂；而預先經口灌食濃度為2~6mL/kg的南洋山蘇水萃物之第B2、B3組大鼠之中央靜脈附近肝細胞壞死的現象則有減緩的狀況，顯示本發明之南洋山蘇水萃物可以有效減緩四氯化碳所造成之肝細胞壞死的現象。 Please refer to Figure 2b. Hepatocytes in the vicinity of the central vein (CV) of the liver of group B1 rats treated with carbon tetrachloride are necrotic and the overall tissue structure is disordered; The phenomenon of hepatocyte necrosis near the central vein of rats in groups B2 and B3 of Nanyangshan Sushui extract of 2 ~ 6mL / kg has been reduced, indicating that the Nanyangshan Sushui extract of the present invention can effectively slow down Necrosis of liver cells caused by carbonization.
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，可以降低四氯化碳所造成之肝功能指數升高的現象及減緩四氯化碳所造成之肝細胞壞死的現象，因而可以應用於製備防治化學性肝損傷的藥物，為本發明之功效。 To sum up, the use of the water extract of Nanyang Mountain Perilla in the present invention is to reduce the increase in liver function index caused by carbon tetrachloride and slow down the cause of carbon tetrachloride by extracting the active ingredients from Nanyang Mountain Perilla. The phenomenon of hepatocyte necrosis can be applied to the preparation of drugs for preventing and treating chemical liver injury, which is the efficacy 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。 Although the present invention has been disclosed using the above-mentioned preferred embodiments, it is not intended to limit the present invention. Anyone skilled in the art can make various changes and modifications to the above embodiments without departing from the spirit and scope of the present invention. The technical scope protected by the invention, so the scope of protection of the present invention shall be determined by the scope of the appended patent application.
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| TW106118700A TWI612967B (en) | 2017-06-06 | 2017-06-06 | A use of an extract of asplenium australasicum (j. sm.) hook. |
| PCT/US2018/034874 WO2018226450A1 (en) | 2017-06-06 | 2018-05-29 | Method for protecting against chemical-induced hepatotoxicity |
| CN201880037389.3A CN110869087A (en) | 2017-06-06 | 2018-05-29 | Method for preventing and treating chemical liver injury |
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| Lih-Shiuh Lai et al,"Chemical compositions and some physical properties of the water and alkali-extracted mucilage from the young fronds of Asplenium australasicum (J. Sm.) Hook", Food Hydrocolloids, 2012, 26(2): 344-349. * |
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