JPS6327435A - Extracting method for extract with high baicalein content - Google Patents
Extracting method for extract with high baicalein contentInfo
- Publication number
- JPS6327435A JPS6327435A JP61170551A JP17055186A JPS6327435A JP S6327435 A JPS6327435 A JP S6327435A JP 61170551 A JP61170551 A JP 61170551A JP 17055186 A JP17055186 A JP 17055186A JP S6327435 A JPS6327435 A JP S6327435A
- Authority
- JP
- Japan
- Prior art keywords
- baicalein
- extract
- scutellariae
- powder
- serration
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- FXNFHKRTJBSTCS-UHFFFAOYSA-N Baicalein Natural products C=1C(=O)C=2C(O)=C(O)C(O)=CC=2OC=1C1=CC=CC=C1 FXNFHKRTJBSTCS-UHFFFAOYSA-N 0.000 title claims abstract description 49
- UDFLTIRFTXWNJO-UHFFFAOYSA-N baicalein Chemical compound O1C2=CC(=O)C(O)=C(O)C2=C(O)C=C1C1=CC=CC=C1 UDFLTIRFTXWNJO-UHFFFAOYSA-N 0.000 title claims abstract description 49
- 229940015301 baicalein Drugs 0.000 title claims abstract description 49
- 239000000284 extract Substances 0.000 title claims abstract description 30
- 238000000034 method Methods 0.000 title claims description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 10
- 238000010438 heat treatment Methods 0.000 claims abstract description 9
- 239000000843 powder Substances 0.000 abstract description 17
- 239000003814 drug Substances 0.000 abstract description 13
- 229940079593 drug Drugs 0.000 abstract description 9
- 239000002537 cosmetic Substances 0.000 abstract description 6
- 201000004624 Dermatitis Diseases 0.000 abstract description 4
- IPQKDIRUZHOIOM-UHFFFAOYSA-N Oroxin A Natural products OC1C(O)C(O)C(CO)OC1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 IPQKDIRUZHOIOM-UHFFFAOYSA-N 0.000 abstract description 4
- IKIIZLYTISPENI-ZFORQUDYSA-N baicalin Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 IKIIZLYTISPENI-ZFORQUDYSA-N 0.000 abstract description 4
- 229960003321 baicalin Drugs 0.000 abstract description 4
- AQHDANHUMGXSJZ-UHFFFAOYSA-N baicalin Natural products OC1C(O)C(C(O)CO)OC1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 AQHDANHUMGXSJZ-UHFFFAOYSA-N 0.000 abstract description 4
- 241000196324 Embryophyta Species 0.000 abstract description 3
- 238000002156 mixing Methods 0.000 abstract description 3
- 230000000144 pharmacologic effect Effects 0.000 abstract description 3
- 208000010668 atopic eczema Diseases 0.000 abstract description 2
- 240000004534 Scutellaria baicalensis Species 0.000 abstract 2
- 235000017089 Scutellaria baicalensis Nutrition 0.000 abstract 2
- 101000874322 Scutellaria baicalensis Baicalin-beta-D-glucuronidase Proteins 0.000 abstract 1
- -1 etc. Substances 0.000 abstract 1
- 241000411851 herbal medicine Species 0.000 abstract 1
- 238000000605 extraction Methods 0.000 description 17
- 239000000243 solution Substances 0.000 description 12
- 238000006243 chemical reaction Methods 0.000 description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 238000007654 immersion Methods 0.000 description 8
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- 241000207929 Scutellaria Species 0.000 description 6
- 238000011160 research Methods 0.000 description 5
- 238000007796 conventional method Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- TWCMVXMQHSVIOJ-UHFFFAOYSA-N Aglycone of yadanzioside D Natural products COC(=O)C12OCC34C(CC5C(=CC(O)C(O)C5(C)C3C(O)C1O)C)OC(=O)C(OC(=O)C)C24 TWCMVXMQHSVIOJ-UHFFFAOYSA-N 0.000 description 2
- PLMKQQMDOMTZGG-UHFFFAOYSA-N Astrantiagenin E-methylester Natural products CC12CCC(O)C(C)(CO)C1CCC1(C)C2CC=C2C3CC(C)(C)CCC3(C(=O)OC)CCC21C PLMKQQMDOMTZGG-UHFFFAOYSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 239000000706 filtrate Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- PFOARMALXZGCHY-UHFFFAOYSA-N homoegonol Natural products C1=C(OC)C(OC)=CC=C1C1=CC2=CC(CCCO)=CC(OC)=C2O1 PFOARMALXZGCHY-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000012827 research and development Methods 0.000 description 2
- TZJALUIVHRYQQB-UHFFFAOYSA-N Icarin Chemical compound C1=CC(OC)=CC=C1C1=C(OC2C(C(O)C(O)C(C)O2)O)C(=O)C2=C(O)C=C(OC3C(C(O)C(O)C(CO)O3)O)C(CC=C(C)C)=C2O1 TZJALUIVHRYQQB-UHFFFAOYSA-N 0.000 description 1
- 235000002597 Solanum melongena Nutrition 0.000 description 1
- 244000061458 Solanum melongena Species 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000035484 reaction time Effects 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 238000002791 soaking Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 235000021419 vinegar Nutrition 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9728—Fungi, e.g. yeasts
Abstract
Description
【発明の詳細な説明】
〔イ〕 発明の目的
本発明は、生薬植物の漢方名称（日周収載名称）オウゴ
ン（和名：フガネバナの根）から、効率良く、バイカレ
インを抽出する方法に関する。[Detailed Description of the Invention] [A] Object of the Invention The present invention relates to a method for efficiently extracting baicalein from the herbal medicinal plant name Scutellariae (Japanese name: Fuganebana root), which is a Chinese medicine name (name listed in the diurnal cycle).
（産業上の利用分野）
本発明による方法で得られた、バイカレイン高含有エキ
スは、医薬品、化粧品、医薬部外品等に用いることが出
来る。(Industrial Application Field) The baicalein-rich extract obtained by the method of the present invention can be used for pharmaceuticals, cosmetics, quasi-drugs, etc.
（従来の技術）
オウゴンは、漢方要薬の一つとして知られ、医薬品（内
服、外用）剤として利用きれ、皮膚炎、湿疹などに有効
とされている。(Prior Art) Scutellariae is known as one of the essential medicines of Chinese medicine, can be used as a pharmaceutical agent (internally and externally), and is said to be effective for treating dermatitis, eczema, etc.
その有効成分（薬理活性成分）としては、パイカリン又
はバイカレインが知られている。又、オウゴンから有効
成分を抽出し、その利用についての技術的文献としては
、例えば、第１表に示すごとくの公知刊行物がある。尚
、第１表中、×印を付したものは、本発明者らに係るも
のである。Picarin or baicalein is known as its active ingredient (pharmacologically active ingredient). Further, as technical documents regarding the extraction of effective ingredients from Scutellariae and its use, there are, for example, publicly known publications as shown in Table 1. In Table 1, the items marked with an x are those of the present inventors.
１第１表」 オウゴンに関する公知刊行物（発明が解決
しようとする問題点）
本発明者らは、すでに、特開昭６１−５０９２１号にお
いては、オウゴン中力）らバイカリンを得る方法、特開
昭６１−５０９１８号においては、パイカリン又はバイ
カレイン含有の化粧料について、研究開発を行なった。1 Table 1 Publications related to Scutellariae (Problems to be Solved by the Invention) The present inventors have already disclosed in JP-A-61-50921 a method for obtaining baicalin from Scutellariae In No. 61-50918, research and development was carried out on cosmetics containing picarin or baicalein.
そして、その後も引き続き、オウゴンに関する有効利用
の為の研究を行なってきた。Since then, we have continued to conduct research on the effective use of Scutellariae.
今回の研究開発のテーマは、オウゴン中から、バイカレ
インを、効率良く抽出する方法についてである。The theme of this research and development is a method for efficiently extracting baicalein from Scutellariae.
すなわち、オウゴン中には、パイカリン及びバイカレイ
ンなどが含まれる。しかし、その含有量は、平均的には
、オウゴン（乾燥）末１００ｇ中に、パイカリン５〜２
０ｇ（約１０％）、バイカレインは０．２〜５ ｇ （
約１％）と、パイカリンが断然多く含まれ、両物質の含
有比率は、約９０％以上がパイカリンとして存在してい
る。That is, Scutellariae contains picalin, baicalein, and the like. However, on average, the content is 5 to 2 picarin in 100 g of scutellariae powder (dried).
0g (approx. 10%), baicalein 0.2-5g (
(approximately 1%), by far the largest amount of picarin, and the content ratio of both substances is approximately 90% or more as picarin.
〔口〕 発明の構成
本発明の主要部は、抽出における前処理にあり、その条
件が、４０〜６５°Ｃ（７）ｘＪ湿温下２時間以上、４
時間以内の浸漬を行なうことが特徴である。この抽出操
作によって、オウゴン中に含まれていた、パイカリンは
、パイ力すナーゼにより、バイカレインへと反応が進み
、最終的に得られる、そのエキス中には、バイカレイン
を高含有するエキスが、容烏に抽出されることとなる。[Example] Structure of the Invention The main part of the present invention is the pretreatment during extraction, and the conditions are: 40 to 65°C (7) x J humidity for 2 hours or more;
It is characterized by immersion within 1 hour. Through this extraction operation, the pycalin contained in Scutellariae undergoes a reaction to baicalein by pyelinase, and the extract that is finally obtained has a high baicalein content. It will be extracted by the crow.
（問題点を解決するための手段）
従来、オウゴンから得られた抽出エキスには、パイカリ
ンとバイカレインが共存した状態のエキスが多かった。(Means for Solving the Problems) Conventionally, many extracts obtained from Scutellariae include picalin and baicalein.
そして、従来の抽出エキスでは、パイカリンとバイカレ
インの含有比率は、パイカリンが８〜９に対して、バイ
カレインが１〜２の割合で含まれたものが多かった。In conventional extracts, the content ratio of picarin and baicalein was often 8 to 9 for picarin and 1 to 2 for baicalein.
このことは、パイカリンとバイカレインの構造上の特徴
にあり、パイカリンには、糖が結合し、バイカレインは
、糖が切り離きれた状態（アグリコン）にある、一般的
には、植物由来成分のアグリコンの状態になったもので
は、その薬理的作用は即効的、糖が結合したものでは遅
効的であるとされている。This is due to the structural characteristics of picalin and baicalein; picalin has a sugar attached to it, and baicalein has a separated sugar (aglycone), which is generally a plant-derived ingredient. The pharmacological action is said to be immediate in the case of sugar-bound drugs, and slow-acting in the case of sugar-bound drugs.
元来、オウゴン中に含まれていたパイカリンは、抽出工
程における各種の条件下で、糖が切断きれて、バイカレ
インに変化し、したがって、両物質が元のオウゴン中に
含まれている比率とは、異なった含有組成を、エキス中
で認めることとなる。Picalin, which was originally contained in Scutellariae, undergoes cleavage of the sugar and changes to baicalein under various conditions during the extraction process. Therefore, the ratio of both substances in the original Scutellariae is different. , different content compositions are recognized in the extract.
そこで、本発明者らは、オウゴン中に含まれるパイカリ
ンが、抽出工程中で反応し、バイカレインに分解される
ことに興味をいだき、抽出条件をフントロールすれば、
あるいは、−気に、オウゴン中に含まれるパイカリンを
、すべて、バイカレインに分解反応させ得ることが出来
るのではないかと考え、その追求に当った。Therefore, the present inventors became interested in the fact that picalin contained in Scutellariae reacts during the extraction process and is decomposed into baicalein, and by adjusting the extraction conditions,
Alternatively, I thought that it might be possible to decompose all the picalin contained in Scutellariae into baicalein, and set out to pursue this idea.
すなわち、本発明の目的であるバイカレインを、効率良
く抽出するための条件を見出せば、これによって、オウ
ゴン中から即、パイカリンを含まない、バイカレインを
高含有したエキスが得られるものと推定し、その研究に
当った。In other words, it is estimated that if conditions for efficiently extracting baicalein, which is the object of the present invention, are found, an extract containing high baicalein and free of picalin can be obtained immediately from Scutellaria scutellariae. I did research.
研究に当って、本発明者らの発想は、才ウゴン中に含ま
れるパイカリンとバイカレインとの関係から、パイカリ
ンの構造上に結合した糖の部分を切断する酵素に着目し
たのである。つまり、オウコ゛ン中には、パイカリンと
共に、パイ力すナーゼが共存していることが知られてい
るので、本発明者らの研究は、このオウゴン中の、パイ
力すナーゼの活性化の為の条件を、オウゴンエキスの抽
出工程に採用出来れば、あるいは、これによって、特別
な薬剤を用いた加水分解等の手段を用いないでも、抽出
工程において、バイカレインに反応が進み、最終的には
、目的となすバイカレインのみを、高含有したエキスが
抽出可能と考えてみたのである。In conducting the research, the inventors focused on an enzyme that cleaves the sugar moiety bonded to the structure of picalin, based on the relationship between picalin and baicalein contained in baicalein. In other words, it is known that picarinase and picarinase coexist in Scutellaria scutellariae, so the present inventors' research focused on the activation of pilinase in Scutellariae. If these conditions can be adopted in the extraction process of Scutellariae extract, or by doing so, the reaction to baicalein will proceed in the extraction process without using any means such as hydrolysis using special chemicals, and ultimately the desired purpose will be achieved. We thought that it would be possible to extract an extract with a high content of only the eggplant baicalein.
その結果、前記したごとく、４０〜６５°Ｃ（最適温度
５０〜６０°Ｃ）で、２時間から４時間以内の加温条件
は、これによって、オウゴン中の７＜イカリンは、その
ほとんどがバイカレインとなることを見出した。As a result, as mentioned above, under heating conditions of 40 to 65°C (optimal temperature 50 to 60°C) for 2 to 4 hours, most of the 7<icarin in Scutellariae is baicalein. I found that.
以下に、その研究成果をもとに、２〜３の実施例を開示
して、さらに詳記する。Below, based on the research results, two to three examples will be disclosed and described in further detail.
「実施例−１」
オウゴン の末又はキザミ（粉末の方
が収量及び反応性が良好、又、加温における時間も、粉
末の方が、短縮され、微粉末になると１第２表」の結果
より、１時間以上反応が短縮される）に対して、水を加
え（オウゴン末１０ｇに水８０謔を添加）、室温から７
０’Ｃの加温下で、浸漬時間との関係をみながら、その
浸漬（反応）させた後の、浸漬溶液に対して、メタノー
ルを加えて加温した後、妨らにメタノールを加え、全量
をｓ ｏ ｏｕＱとする。"Example-1" Results of Scutellaria scutellariae (Table 1, Table 2) (the reaction time is shortened by more than 1 hour), add water (add 80 g of water to 10 g of scutellariae powder), and heat from room temperature to 7 oz.
After immersion (reaction) under heating at 0'C, while looking at the relationship with the immersion time, methanol was added to the immersion solution, heated, and then methanol was added to the immersion solution. Let the total amount be s o ouQ.
次表１第２表」は、上記の実施例１によって得られた、
オウゴンの末（粉末：１６〜４８メツシユ）から得られ
た抽出溶液に含すれる、パイカリンとバイカレインの量
について、高速液体クロマトを用いて求めた、その含有
比率である。The following Table 1, Table 2 was obtained by the above Example 1,
This is the content ratio of picalin and baicalein contained in an extracted solution obtained from scutellariae powder (powder: 16 to 48 mesh) using high performance liquid chromatography.
１第２表」 バイ力レイン含有比率（％）前記の実施例
１（第２表）に示すごとく、オウゴンを出発原料となし
、抽出工程において、その前処理操作にあっては、水中
の加温条件が４０〜６５℃附近で、２〜４時間の処理に
よれば、容易に、オウゴン中のパイカリンは、バイカレ
インに移行されることである。1 Table 2" Bi-rhein content ratio (%) As shown in Example 1 (Table 2) above, Scutellariae was used as the starting material, and in the extraction process, the pretreatment operation involved adding water When the temperature is around 40 to 65°C and the treatment is carried out for 2 to 4 hours, picalin in Scutellariae is easily converted to baicalein.
一方、常温下でも、オウゴン（末）中のパイカリンは、
水の存在下にあって、バイカレインへの移行（反応）が
進行され、８時間の経過は、これによって、オウゴン中
に含まれていたパイカリンを、１００％容易に、バイカ
レインに移行出来ることがわかった。又、その際、４８
〜２００メツシユの微粉末を用いるときでは、３時間の
経過で１００％バイカレインに移行することもわかった
。しかし、７０℃以上の反応では、パイカリンの状態が
保持され、バイカレインへの分解反応は認められなかっ
た。On the other hand, even at room temperature, the picarin in Scutellariae
In the presence of water, the transfer (reaction) to baicalein proceeded, and after 8 hours, it was found that the picalin contained in Scutellaria scutella can be transferred to baicalein 100% easily. Ta. Also, in that case, 48
It was also found that when a fine powder of ~200 mesh was used, the transition to 100% baicalein occurred after 3 hours. However, in the reaction at 70°C or higher, the state of picalin was maintained, and no decomposition reaction to baicalein was observed.
次に、分取したバイカレインの溶解性については、前処
理（浸漬）条件の違いは、異なった溶解性を示す様にな
る。このことについては、パイカレインの、エタノール
７ジ％含有水溶液に対する溶解量（％）を求めてみると
、第３表に示すごとくとなり、５０〜６０℃における３
時間の加温下で処理されたものでは、０．３％強が可溶
であるのに対し、それ以下の温度で処理したものでは、
０．２〜０．３％程度の範囲内にとどまった。Next, regarding the solubility of the fractionated baicalein, different pretreatment (soaking) conditions result in different solubility. Regarding this, when calculating the dissolution amount (%) of picalein in an aqueous solution containing 7% ethanol, it is as shown in Table 3.
In those treated under heating for hours, just over 0.3% is soluble, while in those treated at lower temperatures,
It remained within the range of about 0.2 to 0.3%.
したがって、化粧料等の配合用、あるいは、それらにＭ
領した外用剤等に用いる、バイカレイン含有溶液のｉ＊
ａ、あるいは、内服剤等に用いるための原料として供給
するためには、４０℃では４時間、５０〜６０℃では、
３時間から３時間中の加温下で前処理きれた後、得られ
たものの方が有利と言える。Therefore, it can be used for blending cosmetics, etc., or M
i* of baicalein-containing solutions used in external preparations etc.
a. Alternatively, in order to supply it as a raw material for use in internal medicines, etc., at 40 ° C. for 4 hours, at 50 to 60 ° C.
It can be said that the product obtained after the pretreatment is completed under heating for 3 to 3 hours is more advantageous.
すなわち、従来、オウゴン中から得られたパイカリンや
バイカレインは、水に難溶であり、通常、両物質は水に
対しては、はとんど不溶であったことからしてみれば、
末法による前処理条件下で抽出すれば、その溶解性が向
上し、製剤化上も望ましいものとなる。In other words, picarin and baicalein conventionally obtained from Scutellariae were sparingly soluble in water;
If extracted under pretreatment conditions using a powder method, its solubility will be improved and it will be desirable from the viewpoint of formulation.
「第３表ノ溶解性及びその溶解液の安定性「実施例２゜
ここでは、バイカレインを主体とする化粧料、外用、そ
の他、内服用に利用されやすい溶液又ハ、ソの濃縮エキ
スについて示ス。"Table 3 Solubility and stability of its solution" Example 2 Here, we will show solutions and concentrated extracts of baicalein that are easily used for cosmetics, external use, and internal use. vinegar.
抽出条件の基本的な操作は、前記の実施例１と同様にし
て行なう。The basic operation of extraction conditions is performed in the same manner as in Example 1 above.
オウゴン末１００ｇに精製水６０ （Ｉｌｌ（４００〜
１．０００ｔｌｌの範囲内なら良好）を加えた後、５０
℃で３時間（５０〜６０℃であるときは３時間程度が最
良、１５°Ｃ以上、６５℃以下であれば良い、又、時間
は、その際の温度に対応させて、３〜１０時間以内で良
い）の前処理浸漬を行なう、この操作を終了した後、こ
の浸漬液に対して、１．４００−のエタノール（ここで
は、エタノールは、浸漬溶液が、７０％エタノール含有
濃度となるように１１１１したが、これにこだわる必要
はなく、０〜９０％の濃度でも良い）を加え、室温で１
６時間（６０〜９０℃加熱のときでは、１〜３時間、３
０〜６０℃では、３〜８時間）の浸漬抽出を行なうた後
、その濾液を取る。この濾液は、パイカリンは、はとん
ど含まれていないが、バイカレインを、０．３〜０．５
％含有し、黄褐色澄明な液体として得られる。100g of Scutellariae powder and 60g of purified water (Ill (400~
(Good if within the range of 1.000tll) After adding 50
℃ for 3 hours (when the temperature is 50 to 60℃, about 3 hours is best, 15℃ or higher and 65℃ or lower is fine, and the time depends on the temperature at that time, 3 to 10 hours) After completing this operation, the immersion solution is immersed in 1.400% ethanol (here, ethanol is used so that the immersion solution has a concentration of 70% ethanol). 1111, but there is no need to be particular about this, and a concentration of 0 to 90% is fine), and 1111 at room temperature.
6 hours (1 to 3 hours, 3 hours when heating at 60 to 90℃)
After performing immersion extraction for 3 to 8 hours at 0 to 60°C, the filtrate is taken. This filtrate contains almost no picalin, but contains 0.3 to 0.5 baicalein.
% and is obtained as a yellow-brown clear liquid.
この液体は、そのまま化粧料、医薬品等に配合して用い
ることが出来る。又、減圧下で濃縮して乾燥を行ない、
粉体エキスとしてもちいることが出来る。This liquid can be used as it is by blending it into cosmetics, medicines, etc. Also, concentrate and dry under reduced pressure,
It can be used as a powder extract.
〔ハ〕 発明の効果
本発明による抽出法は、オウゴン自体に含まれる酵素：
バイ力すナーゼの反応を利用して、オウゴン中に含まれ
るパイカリンを、その抽出工程の系中で、バイカレイン
に変換させることによる、オウゴンエキスの抽出法にあ
る。[C] Effects of the invention The extraction method according to the present invention extracts enzymes contained in Scutellariae itself:
The present invention is a method for extracting Scutellariae extract by converting picalin contained in Scutellariae into baicalein in the system of the extraction process using the reaction of scutellariae.
末法によれば、前処理における反応条件として、水中で
２０℃前後から７０℃以下の加温下で行なうことであり
、前記第１表で示される公知エキスの、そのいずれに比
較しても、操作性が簡単であり、しかも、確実に、バイ
カレインとなしたエキスが得られることである。According to the powder method, the reaction conditions in the pretreatment are to carry out the reaction in water under heating from around 20°C to 70°C or less, and compared to any of the known extracts shown in Table 1 above, It is easy to operate and moreover, it is possible to reliably obtain an extract containing baicalein.
又、末法によって得られたエキスは、従来のオウゴンエ
キスに比べ、薬理的活性も強く示きれるようになるが、
これは、主体成分がパイカリンのアグリコンとなした、
バイカレインであることに起因することのみならず、溶
解性が向上しているためである。In addition, the extract obtained by the powder method has stronger pharmacological activity than conventional Scutellaria scutellariae extract, but
The main component is an aglycone of picarin.
This is not only due to the fact that it is baicalein, but also because its solubility is improved.
すなわち、末法によるエキスは、製剤化上からも、従来
のエキスに比べ、溶解性が良く、少量でよく効果を示す
ようになる。That is, from the viewpoint of formulation, the powder-formed extract has better solubility than conventional extracts, and is effective even in small amounts.
又、本発明による抽出法は、従来法に比べ、抽出法が簡
易であり、大量生産が容易となる。又、この方法によっ
て得られたエキスを用いれば＋バイ力レインの精製化も
容易となる。Furthermore, the extraction method according to the present invention is simpler than conventional methods, and mass production is facilitated. Furthermore, if the extract obtained by this method is used, it will be easy to purify +biryokurein.
すなわち、従来法によりバイカレインをオウゴンエキス
中から抽出精製しようとすれば、そのエキス中には、パ
イカリンとバイカレインが共存し、しかも、パイカリン
の含有量の方が多く、シたがって、その少ないバイカレ
インを分取していたわけであり、当然その収量は、きら
に少なくなっていた。これに対して、末法によるエキス
であれば、パイカリンは、抽出工程中で、そのすべてが
、バイカレインに変換きれており、容易にして、大量の
バイカレインが得られるようになる。In other words, when trying to extract and purify baicalein from Scutellaria scutella extract using the conventional method, picalin and baicalein coexist in the extract, and the content of picalin is higher, so it is necessary to extract and purify baicalein from scutellariae extract. Since it was being fractionated, the yield was naturally much lower. On the other hand, in the case of an extract obtained by the powder method, all of the picalin is converted to baicalein during the extraction process, making it easy to obtain a large amount of baicalein.
第１図から、第４図は、第２表（備考欄）中で示した、
高速液体クロマトによる条件で、得られたチャートであ
る。尚、第１図から第４図中、ａはパイカリン、ｂはバ
イカレインを示す。
第１図は、従来法によるオウゴンエキス又は、７０℃以
上の加熱下で、約１時間以上の抽出によって得られた抽
出溶液が示すチャート。尚、第１図中では、ｂ：バイ力
レインのピークは確認しに＜＜、表示していない。
第２図は、末法による５０°Ｃ１３０分間の前処理（反
応）を行なって得られた溶液のチャート。
第３１！Ｉは、末法による５０℃、１時間の前処理（反
応）を行なって得られた溶液のチャート。
第４図は、末法による５０℃、３時間の前処理（反応）
を行なって得られた溶液のチャート。
尚、第４図中では、ａ：バイカリンのピークは確認され
ないため、表示していない。Figures 1 to 4 are as shown in Table 2 (remarks column).
This is a chart obtained under the conditions of high performance liquid chromatography. In addition, in FIGS. 1 to 4, a represents picarin and b represents baicalein. FIG. 1 is a chart showing scutellariae extract obtained by a conventional method or an extraction solution obtained by extraction for about 1 hour or more under heating at 70° C. or more. In addition, in FIG. 1, the peak of b: bi-force rain is not shown for confirmation. FIG. 2 is a chart of a solution obtained by pretreatment (reaction) at 50° C. for 130 minutes using the powder method. 31st! I is a chart of a solution obtained by pretreatment (reaction) at 50° C. for 1 hour using the powder method. Figure 4 shows pretreatment (reaction) at 50°C for 3 hours using the powder method.
A chart of the solution obtained by doing this. In addition, in FIG. 4, the peak of a: baicalin is not confirmed, so it is not displayed.
Claims (1)
２時間から４時間、４０〜６５℃の加温下で前処理する
ことを特徴とする、バイカレイン高含有エキスの抽出法
。(1) After adding water to the end of Scutellariae or Kizami,
A method for extracting a baicalein-rich extract, which is characterized by pretreatment under heating at 40 to 65°C for 2 to 4 hours.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61170551A JPS6327435A (en) | 1986-07-18 | 1986-07-18 | Extracting method for extract with high baicalein content |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61170551A JPS6327435A (en) | 1986-07-18 | 1986-07-18 | Extracting method for extract with high baicalein content |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6327435A true JPS6327435A (en) | 1988-02-05 |
| JPH0470286B2 JPH0470286B2 (en) | 1992-11-10 |
Family
ID=15906968
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP61170551A Granted JPS6327435A (en) | 1986-07-18 | 1986-07-18 | Extracting method for extract with high baicalein content |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6327435A (en) |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0236125A (en) * | 1988-07-26 | 1990-02-06 | Ichimaru Pharcos Co Ltd | Testosterone 5alpha-reductase inhibitor |
| US6641846B2 (en) * | 2000-11-08 | 2003-11-04 | Tianjin Yanling Health Food Co. | Pharmaceutical composition against type I allergy and the preparation thereof |
| WO2005045051A1 (en) * | 2003-11-05 | 2005-05-19 | Novozymes A/S | Baicalin de-glycosylation |
| EP2108370A1 (en) | 2002-04-30 | 2009-10-14 | Unigen Pharmaceuticals, Inc. | Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent |
| US8197861B2 (en) * | 2008-10-02 | 2012-06-12 | George Zabrecky | Methods and formulations for treating chronic liver disease |
| US8771761B2 (en) | 2006-10-12 | 2014-07-08 | Unigen, Inc. | Composition for treating atopic dermatitis comprising extracts of bamboo and scutellaria |
| US8945518B2 (en) | 2002-04-30 | 2015-02-03 | Unigen, Inc. | Formulation of dual eicosanoid system and cytokine system inhibitors for use in the prevention and treatment of oral diseases and conditions |
| US9061039B2 (en) | 2002-03-01 | 2015-06-23 | Unigen, Inc. | Identification of Free-B-Ring flavonoids as potent COX-2 inhibitors |
| CN104991029A (en) * | 2015-05-07 | 2015-10-21 | 北京东方运嘉科技发展有限公司 | Quality detection method of children's cough-relieving medicine |
| US9168242B2 (en) | 2002-03-22 | 2015-10-27 | Unigen, Inc. | Isolation of a dual COX-2 and 5-lipdxygenase inhibitor from Acacia |
| US9622964B2 (en) | 2003-04-04 | 2017-04-18 | Unigen, Inc. | Formulation of dual cycloxygenase (COX) and lipoxygenase (LOX) inhibitors for mammal skin care |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103961661A (en) * | 2014-04-10 | 2014-08-06 | 李红 | Liquid medicine for treating psoriasis for external use and preparation method for liquid medicine |
| CN104530161A (en) * | 2014-12-03 | 2015-04-22 | 安徽海神寿春药业有限公司 | Production process of baikal skullcap root extract |
-
1986
- 1986-07-18 JP JP61170551A patent/JPS6327435A/en active Granted
Non-Patent Citations (1)
| Title |
|---|
| ACTA PHYTOCHIMICA=1935 * |
Cited By (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0236125A (en) * | 1988-07-26 | 1990-02-06 | Ichimaru Pharcos Co Ltd | Testosterone 5alpha-reductase inhibitor |
| US6641846B2 (en) * | 2000-11-08 | 2003-11-04 | Tianjin Yanling Health Food Co. | Pharmaceutical composition against type I allergy and the preparation thereof |
| US9061039B2 (en) | 2002-03-01 | 2015-06-23 | Unigen, Inc. | Identification of Free-B-Ring flavonoids as potent COX-2 inhibitors |
| US9168242B2 (en) | 2002-03-22 | 2015-10-27 | Unigen, Inc. | Isolation of a dual COX-2 and 5-lipdxygenase inhibitor from Acacia |
| EP2108370A1 (en) | 2002-04-30 | 2009-10-14 | Unigen Pharmaceuticals, Inc. | Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent |
| US8945518B2 (en) | 2002-04-30 | 2015-02-03 | Unigen, Inc. | Formulation of dual eicosanoid system and cytokine system inhibitors for use in the prevention and treatment of oral diseases and conditions |
| US9370544B2 (en) | 2002-04-30 | 2016-06-21 | Unigen, Inc. | Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent |
| US9655940B2 (en) | 2002-04-30 | 2017-05-23 | Unigen, Inc. | Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent |
| US9849152B2 (en) | 2002-04-30 | 2017-12-26 | Unigen, Inc. | Formulation of a mixture of Free-B-ring flavonoids and flavans as a therapeutic agent |
| US9622964B2 (en) | 2003-04-04 | 2017-04-18 | Unigen, Inc. | Formulation of dual cycloxygenase (COX) and lipoxygenase (LOX) inhibitors for mammal skin care |
| WO2005045051A1 (en) * | 2003-11-05 | 2005-05-19 | Novozymes A/S | Baicalin de-glycosylation |
| US8771761B2 (en) | 2006-10-12 | 2014-07-08 | Unigen, Inc. | Composition for treating atopic dermatitis comprising extracts of bamboo and scutellaria |
| US9623068B2 (en) | 2006-10-12 | 2017-04-18 | Unigen, Inc. | Composition for treating atopic dermatitis comprising extracts of bamboo and scutellaria |
| US8197861B2 (en) * | 2008-10-02 | 2012-06-12 | George Zabrecky | Methods and formulations for treating chronic liver disease |
| CN104991029A (en) * | 2015-05-07 | 2015-10-21 | 北京东方运嘉科技发展有限公司 | Quality detection method of children's cough-relieving medicine |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0470286B2 (en) | 1992-11-10 |
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