JP2022102811A - PDE5 inhibitor - Google Patents

PDE5 inhibitor Download PDF

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JP2022102811A
JP2022102811A JP2020217777A JP2020217777A JP2022102811A JP 2022102811 A JP2022102811 A JP 2022102811A JP 2020217777 A JP2020217777 A JP 2020217777A JP 2020217777 A JP2020217777 A JP 2020217777A JP 2022102811 A JP2022102811 A JP 2022102811A
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extract
pde5
powder
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spodoptera frugiperda
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志穂 齋藤
Shiho Saito
俊一郎 畑
Shunichiro Hata
直子 益子
Naoko MASUKO
裕美 石黒
Hiromi Ishiguro
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DKS Co Ltd
Biococoon Laboratories Inc
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Dai Ichi Kogyo Seiyaku Co Ltd
Biococoon Laboratories Inc
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Priority to TW110144616A priority patent/TW202233221A/en
Priority to PCT/JP2021/045727 priority patent/WO2022138258A1/en
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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Abstract

To provide a new substance having a PDE5 inhibitory effect.SOLUTION: The PDE5 inhibitor includes a powder of Paecilomyces tenuipes that parasitizes silkworms, or an extract thereof.SELECTED DRAWING: None

Description

ホスホジエステラーゼ(PDE:Phosphodiesterase)5阻害剤に関する技術が開示される。 Techniques for Phosphodiesterase (PDE) 5 inhibitors are disclosed.

PDE5阻害作用を有する物質は、尿路障害や肺動脈性肺高血圧症の予防ないし改善に有効であることが知られている(非特許文献1)。PDE5阻害作用を有する天然由来の物質も知られている(特許文献1及び2)。 A substance having a PDE5 inhibitory action is known to be effective in preventing or ameliorating urinary tract disorders and pulmonary arterial hypertension (Non-Patent Document 1). Naturally-derived substances having a PDE5 inhibitory effect are also known (Patent Documents 1 and 2).

特開2019-34920JP 2019-34920 特開2018-154610JP 2018-154610

日薬理誌、154、265-269、2019Japan Pharmacology Magazine, 154, 265-269, 2019

新たなPDE5阻害作用を有する物質を提供することが1つの課題である。 One challenge is to provide a substance with a new PDE5 inhibitory effect.

上記課題を解決すべく鋭意研究を重ねた結果、カイコハナサナギタケにPDE5阻害作用があることが見出された。斯かる知見に基づき更なる検討を重ね、下記に代表される発明が提供される。
項1
カイコハナサナギタケの粉末又は抽出物を含む、PDE5阻害剤。
項2
飲食品組成物の形態である、項1に記載のPDE5阻害剤。
項3
排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善用である、項1又は2に記載のPDE5阻害剤。
項4
PDE5阻害剤を製造するためのカイコハナサナギタケの粉末又は抽出物の使用。
項5
排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善用組成物を製造するための、カイコハナサナギタケの粉末又は抽出物の使用。
項6
PDE5阻害が必要な対象にカイコハナサナギタケの粉末又は抽出物を投与する方法。
項7
対象が排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善を必要とする、項6に記載の方法。
項8
PDE5阻害における使用のためのカイコハナサナギタケの粉末又は抽出物。
項9
排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善における使用のためのカイコハナサナギタケの粉末又は抽出物。
As a result of diligent research to solve the above problems, it was found that the silk moth, Spodoptera frugiperda, has a PDE5 inhibitory effect. Further studies will be conducted based on such findings, and the inventions represented by the following will be provided.
Item 1
A PDE5 inhibitor, including powder or extract of Spodoptera frugiperda.
Item 2
Item 2. The PDE5 inhibitor according to Item 1, which is a form of a food or drink composition.
Item 3
Item 2. The PDE5 inhibitor according to Item 1 or 2, which is used for preventing or ameliorating dysuria and / or pulmonary arterial hypertension.
Item 4
Use of silk moth powder or extract to produce PDE5 inhibitors.
Item 5
Use of silk moth powder or extract to produce compositions for the prevention or amelioration of dysuria and / or pulmonary arterial hypertension.
Item 6
A method of administering a powder or an extract of Spodoptera frugiperda to a subject in need of PDE5 inhibition.
Item 7
Item 6. The method according to Item 6, wherein the subject requires prevention or improvement of dysuria and / or pulmonary arterial hypertension.
Item 8
A powder or extract of Spodoptera frugiperda for use in PDE5 inhibition.
Item 9
Powder or extract of Spodoptera frugiperda for use in the prevention or amelioration of dysuria and / or pulmonary arterial hypertension.

PDE5阻害作用を有する物質が提供される。一実施形態において、PDE5阻害作作用を利用した排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善の手段が提供される。 A substance having a PDE5 inhibitory action is provided. In one embodiment, a means for preventing or ameliorating dysuria and / or pulmonary arterial hypertension utilizing the PDE5 inhibitory action is provided.

カイコハナサナギタケについてPDE5阻害活性を測定した結果を示す。「Sample」はカイコハナサナギタケの熱水抽出物を示す。「Substrate」はcGMPを示す。The results of measuring the PDE5 inhibitory activity of the silk moth, Spodoptera frugiperda, are shown. "Sample" refers to a hot water extract of Spodoptera frugiperda. "Substrate" indicates cGMP.

PDE5阻害剤は、カイコハナサナギタケ又はその抽出物を含むことが好ましい。カイコハナサナギタケは、カイコに寄生して生育したハナサナギタケ(P.tenuipes、「冬虫夏草」とも称される。)である。カイコハナサナギタケは、市販されるもの及び栽培したもののいずれを使用することも可能である。カイコハナサナギタケの栽培方法は任意であり、例えば、カイコの幼虫やカイコの蛹を加熱滅菌処理した後、冬虫夏草の菌を植菌して育成する方法を挙げることができる。また、特開2005-237201に開示される方法を挙げることができる。具体的には、繭を形成する前のカイコの幼虫又はカイコの蛹を煮沸し、乾燥させ、このカイコ乾燥粉末50~90重量パーセント、残部が豆類、穀類、海藻類またはキノコ類の乾燥粉末の1種または2種以上からなる食物乾燥粉末を混合して、これに培養液を加えて混練し、これを育成箱の底部に敷き詰めて培地を作成し、この培地を、植菌袋に封入して加熱滅菌処理した後、培地に冬虫夏草の菌を接種して、育成することができる。 The PDE5 inhibitor preferably comprises Spodoptera frugiperda or an extract thereof. The silk moth Hanasanagitake is a silk moth that grows parasitic on the silk moth (P.tenuipes, also known as "Caterpillar fungus"). The silk moth, Spodoptera frugiperda, can be either commercially available or cultivated. The method for cultivating silk moths is arbitrary. For example, a method of heat-sterilizing silk moth larvae and silk moth pupae and then inoculating and growing Cordyceps sinensis can be mentioned. Further, the method disclosed in Japanese Patent Application Laid-Open No. 2005-237201 can be mentioned. Specifically, the silk moth larvae or silk moth frogs before forming the cocoons are boiled and dried, and the dry powder of the silk moth is 50 to 90% by weight, and the balance is the dry powder of beans, grains, seaweeds or mushrooms. Mix one or more kinds of dry food powder, add the culture solution to it, knead it, spread it on the bottom of the growing box to make a medium, and enclose this medium in a cocoon bag. After heat sterilization, the medium can be inoculated with the fungus of Cordyceps sinensis and grown.

一実施形態において、カイコハナサナギタケは粉末の形態であることが好ましい。カイコハナサナギタケの粉末は、カイコハナサナギタケを凍結乾燥させ、粉砕して得ることができる。カイコハナサナギタケの粉末は、ハナサナギタケの子実体のみを粉末化したものであってもよいが、子実体および宿主(例えば、カイコ)を粉末化したものであることが好ましい。 In one embodiment, the silk moth is preferably in the form of powder. The powder of Spodoptera frugiperda can be obtained by freeze-drying the Spodoptera frugiperda and pulverizing it. The silk moth powder may be a powder of only the fruiting body of the silk moth, but it is preferably a powder of the fruiting body and the host (for example, silk moth).

一実施形態において、カイコハナサナギタケは、抽出物の形態であることが好ましい。抽出物を得るために用いられる方法及び条件は、任意である。例えば、カイコハナサナギタケをそのまま、裁断、粉砕及び/又は乾燥し、搾取又は適当な溶媒を用いて抽出することができる。溶媒の種類は特に制限されず、例えば、水、メタノール、エタノール、イソプロパノール等の低級アルコール、プロピレングリコール、1,3-ブチレングリコール等の多価アルコール;アセトン等のケトン類、ジエチルエーテル、ジオキサン、アセトニトリル、酢酸エチルエステル等のエステル類、ジメチルスルホキシド、キシレン、ベンゼン、クロロホルム等が挙げられる。一実施形態において好ましい溶媒は、水であり、好ましくは熱水(60℃以上、70℃以上、80℃以上、又は90℃以上)である。 In one embodiment, the silk moth is preferably in the form of an extract. The methods and conditions used to obtain the extract are arbitrary. For example, the silk moth, Spodoptera frugiperda, can be cut, crushed and / or dried as it is, exploited or extracted using a suitable solvent. The type of solvent is not particularly limited, and is, for example, lower alcohols such as water, methanol, ethanol and isopropanol, polyhydric alcohols such as propylene glycol and 1,3-butylene glycol; ketones such as acetone, diethyl ethers, dioxane and acetonitrile. , Esters such as ethyl acetate esters, dimethylsulfoxide, xylene, benzene, chloroform and the like. The preferred solvent in one embodiment is water, preferably hot water (60 ° C. or higher, 70 ° C. or higher, 80 ° C. or higher, or 90 ° C. or higher).

一実施形態において、カイコハナサナギタケの抽出物は次の方法で得られたものであることが好ましい。即ち、カイコハナサナギタケの乾燥粉末に熱水を加え、60℃以上80℃以下の温度で所定の時間(例えば、1時間以上5時間以下)撹拌し、濾過して得られた濾液を乾燥して抽出物を得ることが好ましい。乾燥粉末と熱水との混合比率は任意であるが、例えば、乾燥粉末1重量部に対して5~20重量部、又は7~15重量部とすることができる。 In one embodiment, the extract of Spirogyra spp. Is preferably obtained by the following method. That is, hot water is added to the dry powder of Spodoptera frugiperda, stirred at a temperature of 60 ° C. or higher and 80 ° C. or lower for a predetermined time (for example, 1 hour or more and 5 hours or less), and the filtrate obtained by filtration is dried and extracted. It is preferable to obtain a product. The mixing ratio of the dry powder and the hot water is arbitrary, but may be, for example, 5 to 20 parts by weight or 7 to 15 parts by weight with respect to 1 part by weight of the dry powder.

カイコハナサナギタケの粉末又は抽出物の水分含量は特に制限されないが、例えば、20重量%以下、10重量%以下、8重量%以下、又は5重量%以下とすることができる。 The water content of the silk moth powder or extract is not particularly limited, but may be, for example, 20% by weight or less, 10% by weight or less, 8% by weight or less, or 5% by weight or less.

PDE5阻害剤は、カイコハナサナギタケの粉末又はその抽出物のみから成るものであっても、更に任意の他の成分を含むものであってもよい。他の成分としては、例えば、賦形剤、結合剤、崩壊剤、滑沢剤、湿潤剤、流動化剤、保存剤、界面活性剤、安定剤、希釈剤、溶解剤、等張化剤、殺菌剤、防腐剤、矯味剤、矯臭剤、着色剤、香料等を挙げることができる他の成分として、他のPDE5阻害活性を有する成分や他の生理活性成分を選択することもできる。PDE5阻害剤の形態は任意であり、例えば、粉末状、顆粒状、錠剤状、カプセル状、又は液体状とすることができる。 The PDE5 inhibitor may consist only of powdered silk moth, Spodoptera frugiperda, or an extract thereof, or may further contain any other component. Other ingredients include, for example, excipients, binders, disintegrants, lubricants, wetting agents, fluidizing agents, preservatives, surfactants, stabilizers, diluents, solubilizers, isotonic agents, etc. As other components such as bactericides, preservatives, flavoring agents, odorants, coloring agents, and fragrances, other components having PDE5 inhibitory activity and other physiologically active components can also be selected. The form of the PDE5 inhibitor is arbitrary and can be, for example, powder, granule, tablet, capsule or liquid.

PDE5阻害剤に含まれる、カイコハナサナギタケ又はその抽出物の量は任意であるが、例えば、乾燥重量換算で、0.1%以上100%以下の範囲で設定することができる。含有量の下限は、例えば、1%以上、2%以上、5%以上、10%以上、15%以上、20%以上、30%以上、40%以上、50%以上、60%以上または70%以上とすることができ、上限は99%以下、95%以下、90%以下、80%以下、70%以下、又は60%以下とすることができる。これらの下限及び上限は任意に組み合わせられる。 The amount of Spodoptera frugiperda or its extract contained in the PDE5 inhibitor is arbitrary, but can be set in the range of 0.1% or more and 100% or less in terms of dry weight, for example. The lower limit of the content is, for example, 1% or more, 2% or more, 5% or more, 10% or more, 15% or more, 20% or more, 30% or more, 40% or more, 50% or more, 60% or more or 70%. The upper limit can be 99% or less, 95% or less, 90% or less, 80% or less, 70% or less, or 60% or less. These lower and upper limits can be combined arbitrarily.

一実施形態において、PDE5阻害剤は飲食品の形態であることが好ましい。飲食品には、一般食品だけでなく、保健機能食品(具体的には、特定保健用食品、栄養機能食品、機能性表示食品)、病者用食品、サプリメント等が含まれる。 In one embodiment, the PDE5 inhibitor is preferably in the form of food and drink. Food and drink includes not only general foods but also foods with health claims (specifically, foods for specified health use, foods with nutritional claims, foods with functional claims), foods for the sick, supplements and the like.

一実施形態において、PDE5阻害剤の形態は、液剤、乳剤、懸濁剤、シロップ剤等の液状形態、散剤、顆粒剤、細粒剤、錠剤、丸剤、カプセル剤(ハードカプセル、ソフトカプセルを含む)、トローチ、チュアブル、ゲル状、クリーム状、ペースト状、ムース状、シート状等の半固形または固形形態であり得る。 In one embodiment, the PDE5 inhibitor forms include liquid forms such as liquids, emulsions, suspensions, syrups, powders, granules, fine granules, tablets, rounds, capsules (including hard capsules, soft capsules). , Troches, chewables, gels, creams, pastes, mousses, sheets and the like, in semi-solid or solid form.

一般食品は特に制限されないが、例えば、飲料類(例えば、果汁飲料、野菜ジュース、清涼飲料、アルコール飲料、炭酸飲料、スポーツドリンク、滋養強壮ドリンク、栄養ドリンク等)、菓子類(例えば、スナック菓子、米菓、チョコレート、グミ、キャンディー、ゼリー、プリン、和菓子、洋菓子等)、調味料類(例えば、醤油、味噌、みりん風調味料、ミックススパイス、たれ、つゆ、ソース、ケチャップ等)、ドレッシング類、麺類(例えば、うどん、そば、スパゲッティ等)、畜肉魚肉加工食品類(例えば、ソーセージ、ウインナー、ハム、ハンバーグ等)、乳製品類(ヨーグルト、牛乳、チーズ、クリーム、バター等)等を挙げることができる。 General foods are not particularly limited, but for example, beverages (for example, fruit juice beverages, vegetable juices, soft beverages, alcoholic beverages, carbonated beverages, sports drinks, nourishing tonic drinks, nutritional drinks, etc.), confectionery (eg, snack confectionery, rice). Confectionery, chocolate, gummy, candy, jelly, pudding, Japanese confectionery, Western confectionery, etc.), seasonings (for example, soy sauce, miso, mirin-style seasoning, mixed spices, sauce, soup, sauce, ketchup, etc.), dressings, noodles (For example, udon, buckwheat, spaghetti, etc.), processed meat and fish foods (for example, sausage, wiener, ham, hamburger, etc.), dairy products (yogurt, milk, cheese, cream, butter, etc.), etc. can be mentioned. ..

一実施形態において、上述のPDE5阻害剤は、PDE5の活性を阻害することによって、排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善する用途で用いることができる。尿路障害の原因、種別は問わないが、下部尿路症状を伴う尿路障害を挙げることができる。 In one embodiment, the PDE5 inhibitor described above can be used for the prevention or amelioration of dysuria and / or pulmonary arterial hypertension by inhibiting the activity of PDE5. The cause and type of urinary tract disorder are not limited, but urinary tract disorders accompanied by lower urinary tract symptoms can be mentioned.

一実施形態において、PDE5阻害剤は医薬の形態とすることができる。PDE5阻害剤を含む医薬は、カイコハナサナギタケの粉末又は抽出物に必要に応じて薬学的に許容可能な賦形剤を組み合わせて調製することができる。 In one embodiment, the PDE5 inhibitor can be in the form of a pharmaceutical. Pharmaceuticals containing PDE5 inhibitors can be prepared by combining the powder or extract of Spodoptera litura with a pharmaceutically acceptable excipient as required.

PDE5阻害剤の摂取(投与)量は、目的とする効果が奏される限り特に限定されず、対象者(対象動物)の体格、年齢、症状、適用形態、使用目的等に応じて適宜設定すすることができる。例えば、1日当たりの摂取(投与)量は、体重60kgの成人を基準として、カイコハナサナギタケ又はその抽出物の乾燥重量換算として、0.001~8000mg、0.01~5000mg等の範囲で設定することができる。摂取(投与)回数は任意であり、例えば、1日あたり単回摂取(投与)であってもよく複数回摂取(投与)であってもよい。 The intake (administration) amount of the PDE5 inhibitor is not particularly limited as long as the desired effect is achieved, and is appropriately set according to the physique, age, symptom, application form, purpose of use, etc. of the subject (target animal). can do. For example, the daily intake (administration) amount should be set in the range of 0.001 to 8000 mg, 0.01 to 5000 mg, etc. in terms of dry weight of silk moth, Spodoptera frugiperda or its extract, based on an adult weighing 60 kg. Can be done. The number of ingestions (administrations) is arbitrary, and may be, for example, a single ingestion (administration) or a plurality of ingestions (administrations) per day.

上述のとおり、カイコハナサナギタケ又はその抽出物はPDE5阻害作用を有するため、カイコハナサナギタケの粉末又は抽出物をPDE5阻害剤を製造するために使用できる。また、排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善用組成物を製造するために、カイコハナサナギタケの粉末又は抽出物を使用こともできる。 As described above, since the silk moth bamboo shoot or its extract has a PDE5 inhibitory effect, the powder or extract of the silk moth spinach bamboo can be used for producing a PDE5 inhibitor. In addition, powder or extract of Spodoptera frugiperda can also be used to produce a composition for preventing or ameliorating dysuria and / or pulmonary arterial hypertension.

上述のとおり、カイコハナサナギタケ又はその抽出物はPDE5阻害作用を有するため、PDE5阻害が必要な対象にカイコハナサナギタケの粉末又は抽出物を投与し、PDE5阻害作用を提供することができる。また、PDE5阻害によって、排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善が可能となるため、排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善を必要とする対象にカイコハナサナギタケの粉末又は抽出物を投与することにより、当該予防若しくは改善を行うことができる。 As described above, since the silk moth Spodoptera frugiperda or its extract has a PDE5 inhibitory action, it is possible to administer the powder or the extract of the Spodoptera litura to a subject in need of PDE5 inhibition to provide the PDE5 inhibitory action. In addition, since PDE5 inhibition enables prevention or amelioration of dysuria and / or pulmonary arterial hypertension, powder of Kaikohanasanagitake is targeted for subjects who require prevention or improvement of dysuria and / or pulmonary arterial hypertension. Alternatively, the prevention or improvement can be performed by administering the extract.

以下、実施例により本発明についてさらに詳細に説明するが、本発明はこれらに制限されるものではない。 Hereinafter, the present invention will be described in more detail by way of examples, but the present invention is not limited thereto.

1.カイコハナサナギタケ熱水抽出物
カイコ蛹を宿主として得られるハナサナギタケ(カイコハナサナギタケ)を凍結乾燥し、ミキサーで粉砕することによりカイコハナサナギタケ粉末を得た。反応容器に、得られた粉末(42g)および超純水420mLを入れ、70℃で3時間攪拌した後、ろ過を行うことにより残渣を取り除いて溶液を得た。続いて、溶液が30mLになるまで濃縮した後、スプレー乾燥を行うことによりカイコハナサナギタケ熱水抽出物を得た。
1. 1. Spirogyra chinensis hot water extract The silk moth pupa obtained as a host was lyophilized and pulverized with a mixer to obtain silk moth pupa powder. The obtained powder (42 g) and 420 mL of ultrapure water were placed in a reaction vessel, stirred at 70 ° C. for 3 hours, and then filtered to remove the residue to obtain a solution. Subsequently, the solution was concentrated to 30 mL and then spray-dried to obtain a hot water extract of Spirogyra vulgaris.

2.PDE5阻害活性の測定
PDE5阻害活性は、PDE-Glo(商標)Phosphodiesterase Aassay(Promega社製)を用いて行った。カイコハナサナギタケ熱水抽出物を終濃度が33μg/ml、11μg/g、3.7μg/ml、1.2μg/mlとなるように超純水に希釈したものをサンプルとして用いた。酵素は、ホスホジエステラーゼ5A1ヒト(Sigma-Aldrich製)を用いた。3100U/μlのPDE1μと反応バッファー205.7μlを混合し、PDE溶液を調製した。PDE溶液15μlと各サンプル10μlを混合し、2分間スピンダウンし、室温で5分間振盪した。この混合液25μlに20μMのcGMPを25μlを添加して混合し、PCRチューブに8μlずつ分注した。これをシェーカーに載せ、室温、400rpmで反応させた。各チューブに検出バッファーを4μl添加し、スピンダウン後に室温で20分間振盪した。これとKinase-Glo試薬を10μlを384ウェルプレート(Thermo Fisher製)の各ウェルに10μlずつ分注し、室温で振盪し、反応させた。カイコハナサナギタケ熱水抽出物を添加しないサンプルを用いた試験例を0%コントロール、PDEを添加しない試験例を100%コントロールとして、カイコハナサナギタケ熱水抽出物による相対的な阻害率を測定した。測定は4回繰り返した。結果を図1に示す。
2. 2. Measurement of PDE5 Inhibitory Activity PDE5 inhibitory activity was performed using PDE-Glo ™ Phosphodiesterase Assay (manufactured by Promega). A sample obtained by diluting the hot water extract of Kaikohanasanagitake with ultrapure water so that the final concentrations were 33 μg / ml, 11 μg / g, 3.7 μg / ml, and 1.2 μg / ml was used as a sample. As the enzyme, phosphodiesterase 5A1 human (manufactured by Sigma-Aldrich) was used. 1μ of PDE of 3100 U / μl and 205.7 μl of reaction buffer were mixed to prepare a PDE solution. 15 μl of PDE solution and 10 μl of each sample were mixed, spun down for 2 minutes and shaken at room temperature for 5 minutes. To 25 μl of this mixed solution, 25 μl of 20 μM cGMP was added and mixed, and 8 μl each was dispensed into a PCR tube. This was placed on a shaker and reacted at room temperature at 400 rpm. 4 μl of detection buffer was added to each tube, and after spin-down, the mixture was shaken at room temperature for 20 minutes. 10 μl of this and 10 μl of Kinase-Glo reagent was dispensed into each well of a 384-well plate (manufactured by Thermo Fisher), shaken at room temperature, and reacted. The relative inhibition rate by the silk moth hot water extract was measured with 0% control of the test example using the sample without the addition of the hot water extract of the silk moth, and 100% control of the test example without the addition of PDE. The measurement was repeated 4 times. The results are shown in FIG.

図1の結果から、カイコハナサナギタケ熱水抽出物にはPDE5阻害活性が存在し、その活性が濃度依存的に上昇することが確認された。この結果から、カイコハナサナギタケは、肺動脈性肺高血圧症及び排尿障害等の疾患の治療無いし予防に有効と考えられる。 From the results shown in FIG. 1, it was confirmed that the Spodoptera frugiperda hot water extract has a PDE5 inhibitory activity, and the activity increases in a concentration-dependent manner. From this result, it is considered that Spodoptera frugiperda is effective for the prevention without treatment of diseases such as pulmonary arterial hypertension and dysuria.

Claims (3)

カイコハナサナギタケの粉末又は抽出物を含む、PDE5阻害剤。 A PDE5 inhibitor, including powder or extract of Spodoptera frugiperda. 飲食品組成物の形態である、請求項1に記載のPDE5阻害剤。 The PDE5 inhibitor according to claim 1, which is in the form of a food and drink composition. 排尿障害及び/又は肺動脈性肺高血圧症の予防若しくは改善用である、請求項1又は2に記載のPDE5阻害剤。 The PDE5 inhibitor according to claim 1 or 2, which is used for preventing or ameliorating dysuria and / or pulmonary arterial hypertension.
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