TR2021021393A2 - INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF SALVIA TRILOBA LEAVES ON COX-1, COX-2 AND LOX ENZYMES - Google Patents

INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF SALVIA TRILOBA LEAVES ON COX-1, COX-2 AND LOX ENZYMES

Info

Publication number
TR2021021393A2
TR2021021393A2 TR2021/021393 TR2021021393A2 TR 2021021393 A2 TR2021021393 A2 TR 2021021393A2 TR 2021/021393 TR2021/021393 TR 2021/021393 TR 2021021393 A2 TR2021021393 A2 TR 2021021393A2
Authority
TR
Turkey
Prior art keywords
cox
leaves
extract
standardized
salvigenin
Prior art date
Application number
TR2021/021393
Other languages
Turkish (tr)
Inventor
E Esra Karada Ay
Nur Bi̇lteki̇n Kaleli̇ Sevde
Tosun Fatma
Original Assignee
İstanbul Medi̇pol Üni̇versi̇tesi̇
Filing date
Publication date
Application filed by İstanbul Medi̇pol Üni̇versi̇tesi̇ filed Critical İstanbul Medi̇pol Üni̇versi̇tesi̇
Priority to PCT/TR2022/051140 priority Critical patent/WO2023128990A1/en
Publication of TR2021021393A2 publication Critical patent/TR2021021393A2/en

Links

Abstract

Mevcut buluş, antienflamatuvar ajan olarak kullanım için Salvia triloba yapraklarının salvigenin üzerinden standardize ekstresi ile ilgilidir.The present invention relates to the standardized extract of Salvia triloba leaves based on salvigin for use as an anti-inflammatory agent.

Description

TARIFNAME SAL VIA TRILOBA YAPRAKLARININ STANDARDIZE EKSTRELERININ COX-l, COX-Z VE LOX ENZIMLERINI INHIBE EDICI ETKILERI Teknik Alan Mevcut bulus, antienflamatuvar ajan olarak kullanim için Salvia triloba yapraklarinin salvigenin üzerinden standardize ekstresi ile ilgilidir. Teknigin Bilinen Durumu Enilamasyon kaynakli rahatsizliklar siklikla karsimiza çikmaktadir. Vücudun farkli bölgelerinde farkli nedenlerle meydana gelen enflamasyonlarin tedavisi çesitli konvansiyonel ilaçlarla saglanmaya çalisilmaktadir. Ancak kullanilan bu ajanlarla tedavi zaman zaman yetersiz kalmakla beraber yeni ve dogal antienflamatuar aj anlarin kesfi büyük Önem tasimaktadir. Dogal kaynakli terapötik ajanlarin ticari kullaniminda en çok karsilasilan problemlerden biri dogal ürünlerden elde edilen ekstrelerin içerisindeki farmasötik etkiye sahip madde miktarinin sabit olmamasidir. Bitkinin toplandigi bölgeye veya toplandigi döneme göre degisiklik gösterebilen burn iktar degisikligi, bitkisel kökenli ekstreler kullanilarak etkinligi tekrar edilebilir ve standardize edilebilir formülasyonlar gelistirilmesini engellemektedir. Teknigin bilinen durumu göz önüne alindiginda hem bitkisel veya dogal kaynaklardan elde edilen hem de içerisinde bulunan farmasötik etkinlik gösteren madde miktari yönünden standardize edilebilen, farma kalitede antienflamatuar ajanlara ihtiyaç oldugu görülmektedir. Bulusun Amaci Bulus sahipleri, bitkisel veya dogal kaynaklardan elde edilen ve içerisinde bulunan farmasötik etkinlik gösteren madde miktari yönünden standardize edilebilen antienilamatuar ajanlar gelistirmeyi amaçlamaktadir. Bulusun Kisa Açiklamasi Mevcut bulus antienflamatuvar ajan olarak kullanim için Salvia triloba yapraklarinin salvigenin üzerinden standardize ekstresine veya herhangi bir oranda örnegin %1 - %99 oraninda salvigenin içeren bilesiklere, tercihen "01 - %99 oraninda isalvigenin içeren bitki eskirelerine, özellikle tercihen %1 ile %95 oraninda salvigeni'n içeren Salvia trilaba yapraklarinin ekstresine, örnegin Bulusta salvigenin açisindan standardize ekstreler kullanildigi için yapilan çalisma sonuçlarinin tekrarlanabilirligi ve tartisilabilirligi mevcuttur. Ayrica, COX ve LOX enzimlerini selektif olarak inhibe eden çok fazla ajan olmamasi nedeniyle, bulusa uygun antientlamatuvar ajan olarak kullanim için Salvi'a trilaba yapraklarinin salvigenin üzerinden standardize ekstresi ile hastalara dogal bir antienflamatuar ajan saglanmaktadir. Bulusun Detayli Anlatimi Mevcut bulus antienflamatuvar ajan olarak kullanim için Salvia triloba yapraklarinin salvigenin üzerinden standardize ekstresine yöneliktir. Bulusun bir diger uygulamasi antienflamatuvar ajan olarak kullanim için Salvia iriloba yapraklarinin en az % l, tercihen %1-5 araliginda salvigenin içeren standardize ekstresine yöneliktir. Bulus kapsaminda bahsedilen % salvigenin miktari, standardize ekstrenin Türk Farmakopesi-II monogratlar (Avrupa farmakopesi adaptasyonu) - 2016 isimli kaynakta (TC. Saglik Bakanligi, Türkiye Ilaç ve Tibbi cihaz kurumu, 1. Baski, 2016) Salvia triloba yapraklarinin ekstresinde salvigenin tayininde kullanilan herhangi bir analiz yöntemi örnegin HPLC ve/veya HPTLC cihazi analizleri ile belirlenmektedir. Burada kullanilan antientlamatuar ajan ifadesi, COX-l ve/veya COK-2 ve/veya LOX inhibitörü etkisi gösteren aj anlari da kapsamaktadir. Bu bulus kapsaminda bahsi geçen % orani relatif bir oran olup, analize tabi tutulan Sal via triloba yapraklarinin ekstresi numunesindeki toplam madde miktarina kiyasla salvigenin miktarini ifade etmektedir. Örnegin, bir Salvi'a triloba yapraklarinin ekstresi numunesinin HPLC analizinde elde edilen tüm pik alani 100 ile ifade edilecek olursa, bulusa uygun bir Salvia triloba yapraklarinin numunesinde salvigenin'e karsilik gelen pikin alani en az 1 olmalidir. Bulus bir diger açidan, antienflamatuvar ajan olarak kullanima uygun Salvi'a triloba yapraklarinin en az % 1, tercihen %1-5 araliginda salvigenin içeren standardize ekstresini içeren farmasötik bilesimlere iliskindir. Bulusun bir diger unsuru, etken madde olarak Salvia triloba yapraklarinin en az % 1, tercihen %1- araliginda salvigenin içeren standardize ekstresini içeren farmasötik bilesimlerde bahsi geçen bu etken maddeye ilave olarak bir diger antienflamatuar ajan kullanilmasidir. Bulusun bir uygulamasinda bahsi geçen ilave antienflamatuar ajan ibuprofen veya diklofenak olabilir. Bulusa uygun kombinasyonlar, ayni dozaj formunda veya farkli dozaj formlarinda formüle edilebilir. Bulusa uygun kombinasyon forrnülasyonlarinin farkli dozaj formlarinda formüle edilmesi durumunda bahsi geçen formülasyonlar farkli zamanlarda veya ayni anda veya sirali olarak kullanilabilir. Bulusa uygun formülasyonlar oral veya topikal kullanima uygun bir dozaj formunda formüle edilebilir. Oral formülasyonlar, tablet, kapsül, uzun salinimli kapsül, geciktirilmis salinimli kapsül, surup, emülsiyon, süspansiyon, kaplamali tablet, katmanli tablet, agizda dagilan tablet, efervesan tablet, sase, dil alti tablet formlarindan herhangi birinde olabilir. Topikal formülasyonlar, merhem, krem, jel, hidrojel, losyon formlarindan herhangi birinde olabilir. Bulusa uygun formülasyonlar içerisinde Salvi'a tri'loba yapraklarinin en az % l salvigenin içeren ekstresine ek olarak farmasötik olarak kabul edilebilir en az bir yardimci madde olabilir. Bahsi geçen yardimci madde, herhangi bir terapötik etkisi olmayip, fonnülasyonun hazirlanmasi veya korunmasi veya kullanimi esnasinda ortaya çikan bir gereksinimi karsilamak için kullanilabilir. Endüstriye Uygulanabilirlik Bulus sayesinde antientlamatuar ajan olarak kullanima uygun dogal kökenli ajanlar gelistirilmistir. Bu yönüyle bulus hem saglik sektöründeki son kullanicilari hem de ilaç gelistiricilerini il gilendirmektedir. Örnekler Örnek 1: Bulusa uygun Salvia triloba yapraklarinin ekstresinin COX-l ve COK-2 inhibisyonu için Asagida sonuçlari verilen çalismada kullanilan Salvia triloba yapraklarinin ekstresi içerisinde % 3,7 salvigenin bulunmaktadir. Madde No. ICso (ug/mL) SI Salvia triloba yapraklari Örnek 1"de yer alan sonuçlar degerlendirildiginde bulusa uygun Salvi'a rriloba yapraklarinin salvigenin üzerinden standardize ekstresinin dogal bir ekstre olmasina ragmen ticari olarak uzun sürelerdir kullanilan antienflamatuvar ajanlardan daha iyi veya anlamli derecede yakin antienflamatuar etki gösterdigi görülmektedir. Burada bahsi geçen antienIlamatuar etki COX-l ve/veya COK-2 inhibisyonu üzerinden gösterilmektedir. Özellikle ilaç piyasasinda uzun yillardir siklikla kullanilan antientlamatuar ajanlardan olan ibuprofen ve diklofenak etken maddelerine kiyasla daha iyi COX-l ve COX-Z inhibisyonunun görülmesi bu dogal kaynakli standardize ekstrelerin Önemli antietlamatuar ajanlar olabilecegini ortaya koymaktadir. Ayrica, bulusa uygun Salvi'a tri'loba yapraklarinin salvigenin üzerinden standardize ekstresinin her iki aj ana kiyasla COX-Z üzerinde daha etkin oldugu yukarida verilen tablodan görülmektedir, bu özelligi ile bulusa uygun bu ekstrenin bazi antientlamatuar aj anlarda siklikla görülen mide tahris edici etkiye sahip olmadigi da tespit edilmistir. Bu yönüyle de bulusa uygun standardize ekstreler bilinen teknikte var olan ajanlardan daha üstün etki göstermektedir. TR TR TR DESCRIPTION INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF SAL VIA TRILOBA LEAVES ON COX-1, COX-Z AND LOX ENZYMES Technical Field The present invention relates to the standardized extract of Salvia triloba leaves via salvigen for use as an anti-inflammatory agent. Known Status of the Technique Disorders caused by enlargement occur frequently. Inflammations that occur in different parts of the body for different reasons are tried to be treated with various conventional drugs. However, although treatment with these agents is sometimes insufficient, the discovery of new and natural anti-inflammatory agents is of great importance. One of the most encountered problems in the commercial use of naturally derived therapeutic agents is that the amount of substances with pharmaceutical effects in the extracts obtained from natural products is not constant. Variation in nose quantity, which may vary depending on the region where the plant is collected or the period in which it is collected, prevents the development of reproducible and standardizable formulations using plant-derived extracts. Considering the known state of the art, it appears that there is a need for pharmaceutical quality anti-inflammatory agents that are obtained from herbal or natural sources and can be standardized in terms of the amount of pharmaceutically active substances they contain. Purpose of the Invention The inventors aim to develop anti-inflammatory agents that are obtained from herbal or natural sources and can be standardized in terms of the amount of pharmaceutically active substances they contain. Brief Description of the Invention The present invention is based on the standardized extract of Salvia triloba leaves over salvigenin for use as an anti-inflammatory agent or compounds containing salvigenin in any ratio, for example 1% to 99%, preferably plant extracts containing 01% to 99% isalvigenin, especially preferably 1% to 99%. Since standardized extracts were used in the invention, for example, the extract of Salvia trilaba leaves containing 95% salvigenin, the results of the study are reproducible and questionable. Moreover, since there are not many agents that selectively inhibit COX and LOX enzymes, it can be used as an anti-inflammatory agent in accordance with the invention. With the standardized extract of Salvia trilaba leaves over salvigen, a natural anti-inflammatory agent is provided to patients. Detailed Description of the Invention The present invention is directed to the standardized extract of Salvia triloba leaves over salvige for use as an anti-inflammatory agent. Another application of the invention is directed to the standardized extract of Salvia iriloba leaves containing at least 1%, preferably 1-5% salvigenin, for use as an anti-inflammatory agent. The amount of % salvigene mentioned within the scope of the invention is determined by the standardized extract in the Turkish Pharmacopoeia-II monogrades (European pharmacopoeia adaptation) - 2016 (Turkish Ministry of Health, Turkish Medicines and Medical Devices Agency, 1st Edition, 2016) as any data used in the determination of salvigene in the extract of Salvia triloba leaves. An analysis method is determined by, for example, HPLC and/or HPTLC device analysis. The term anti-inflammatory agent used here also includes agents that have COX-1 and/or COK-2 and/or LOX inhibitory effects. Within the scope of this invention, the percentage mentioned is a relative ratio and expresses the amount of salvigen compared to the total amount of substance in the extract sample of Sal via triloba leaves subjected to analysis. For example, if the entire peak area obtained in the HPLC analysis of a sample of Salvia triloba leaves extract is expressed as 100, the area of the peak corresponding to salvigenin in a sample of Salvia triloba leaves according to the invention must be at least 1. In another aspect, the invention relates to pharmaceutical compositions containing the standardized extract of Salvi'a triloba leaves containing at least 1%, preferably 1-5% salvigenin, suitable for use as an anti-inflammatory agent. Another element of the invention is the use of another anti-inflammatory agent in addition to the said active ingredient in pharmaceutical compositions containing the standardized extract of Salvia triloba leaves containing at least 1%, preferably 1% salvigenin, as the active ingredient. In one embodiment of the invention, said additional anti-inflammatory agent may be ibuprofen or diclofenac. The combinations according to the invention can be formulated in the same dosage form or in different dosage forms. If the combination formulations according to the invention are formulated in different dosage forms, said formulations can be used at different times or simultaneously or sequentially. The formulations according to the invention can be formulated in a dosage form suitable for oral or topical use. Oral formulations can be in any of the forms of tablets, capsules, extended-release capsules, delayed-release capsules, syrups, emulsions, suspensions, coated tablets, layered tablets, orodispersible tablets, effervescent tablets, sachets, and sublingual tablets. Topical formulations can be in any of the forms of ointment, cream, gel, hydrogel or lotion. Formulations according to the invention may contain at least one pharmaceutically acceptable excipient in addition to the extract of Salvi'a tri'loba leaves containing at least 1% salvigenin. Said excipient does not have any therapeutic effect and can be used for the preparation or maintenance of the formulation or to meet a need arising during its use. Industrial Applicability Thanks to the invention, natural origin agents suitable for use as anti-inflammatory agents have been developed. In this respect, the invention interests both end users in the healthcare sector and drug developers. Examples Example 1: For COX-1 and COK-2 inhibition of the extract of Salvia triloba leaves according to the invention. The extract of Salvia triloba leaves used in the study whose results are given below contains 3.7% salvigenin. Item No. ICso (ug/mL) SI Salvia triloba leaves When the results in Example 1 are evaluated, it can be seen that the standardized extract of Salvia triloba leaves according to the invention over salvigen has a better or significantly closer anti-inflammatory effect than the anti-inflammatory agents that have been used commercially for a long time, despite being a natural extract. The anti-inflammatory effect mentioned here is shown through COX-1 and/or COK-2 inhibition. This natural source shows better COX-1 and COX-Z inhibition compared to the active ingredients ibuprofen and diclofenac, which are anti-inflammatory agents that have been frequently used in the pharmaceutical market for many years. It reveals that standardized extracts can be important anti-inflammatory agents. Moreover, it can be seen from the table given above that the standardized extract of Salvi'a tri'loba leaves over salvigen according to the invention is more effective on COX-Z compared to both the main ones, with this feature, this extract according to the invention has some anti-inflammatory properties. It has also been determined that it does not have the stomach irritating effect that is often seen in other drugs. In this respect, the standardized extracts in accordance with the invention have a superior effect than the agents available in the known art. TR TR TR

Claims (1)

1.STEMLER Antienflamatuvar ajan olarak kullanim için Salvi'a triloba yapraklarinin en az % 1 oraninda salvigenin içeren standardize ekstresi, . Istem 1 ”e göre COX-l ve/veya COK-2 ve/veya LOX enzimi inhibitörü olarak kullanim için Salvi'a tri'loba yapraklarinin en az % 1 oraninda salvigenin içeren standardize ekstresi. . Istem 1 veya 2°ye göre bir ekstre olup %1-5 araliginda salvigenin içerir. . AntienIlamatuvar ajan olarak kullanima uygun, etken madde olarak Salvi'a tri'loba yapraklarinin en az % 1 oraninda salvi genin içeren standardize ekstresini içeren fannasötik bilesimler. . Istem 4,e göre bir farmasötik bilesim olup ilave olarak bir diger antienflamatuar ajan içerir. . Istem 5”e göre bir farmasötik bilesim olup ilave antienflamatuar ajan diklofenak veya iboprofendir. . Istem 4-6”dan herhangi birine göre bir farmasötik bilesim olup, oral veya topikal kullanima uygun bir dozaj formunda formüle edilmistir. TR TR TR1.CLAIM: Standardized extract of Salvi'a triloba leaves containing at least 1% salvigenin for use as an anti-inflammatory agent. Standardized extract of Salvi'a tri'loba leaves containing at least 1% salvigenin for use as inhibitor of COX-1 and/or COK-2 and/or LOX enzyme according to claim 1. . It is an extract according to claim 1 or 2 and contains 1-5% salvigenin. . Pharmaceutical compositions suitable for use as anti-inflammatory agents, containing as the active ingredient the standardized extract of Salvi'a tri'loba leaves containing at least 1% of salvi gene. . A pharmaceutical composition according to claim 4 further comprising another anti-inflammatory agent. . A pharmaceutical composition according to claim 5, wherein the additional anti-inflammatory agent is diclofenac or iboprofen. . A pharmaceutical composition according to any one of claims 4-6, formulated in a dosage form suitable for oral or topical use. TR TR TR
TR2021/021393 2021-12-28 2021-12-28 INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF SALVIA TRILOBA LEAVES ON COX-1, COX-2 AND LOX ENZYMES TR2021021393A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/TR2022/051140 WO2023128990A1 (en) 2021-12-28 2022-10-17 Inhibitory effects of standardized extracts of salvia triloba leaves on cox-1, cox-2 and lox enzymes

Publications (1)

Publication Number Publication Date
TR2021021393A2 true TR2021021393A2 (en) 2023-07-21

Family

ID=

Similar Documents

Publication Publication Date Title
US8142819B2 (en) Synergistic compositions that treat or inhibit pathological conditions associated with inflammatory response
US7270835B2 (en) Compositions that treat or inhibit pathological conditions associated with inflammatory response
US8557306B2 (en) Compositions that treat or inhibit pathological conditions associated with inflammatory response
CA2503196C (en) Compositions that treat or inhibit pathological conditions associated with inflammatory response
Peng et al. Berberine produces antidepressant-like effects in the forced swim test and in the tail suspension test in mice
Hwang et al. Cycloastragenol can negate constitutive STAT3 activation and promote paclitaxel-induced apoptosis in human gastric cancer cells
Toselli et al. Echinacea metabolism and drug interactions: the case for standardization of a complementary medicine
Li et al. Interactions of the active components of Punica granatum (pomegranate) with the essential renal and hepatic human Solute Carrier transporters
Kwan et al. Vascular effects of Siberian ginseng (Eleutherococcus senticosus): endothelium-dependent NO-and EDHF-mediated relaxation depending on vessel size
Dziwenka et al. Ginkgo biloba
Zhai et al. The protective effect of hypericin on postpartum depression rat model by inhibiting the NLRP3 inflammasome activation and regulating glucocorticoid metabolism
CN101444139A (en) Compositions exhibiting inhibition of cyclooxygenase-2
Müller et al. Interactions between phytochemical components of Sutherlandia frutescens and the antiretroviral, atazanavir in vitro: implications for absorption and metabolism
Rajan et al. Anti-diabetic effect of hesperidin on palmitate (PA)-treated HepG2 cells and high fat diet-induced obese mice
Ishaq et al. COMPARATIVE STUDY OF ETHANOLIC AND AQUEOUS EXTRACTS OF APIUM GRAVEOLENS L. ROOT WITH FUROSEMIDE FOR ITS DIURETIC ACTIVITY & EXCRETION OF URINARY METABOLITES IN WISTAR RATS.
TR2021021393A2 (en) INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF SALVIA TRILOBA LEAVES ON COX-1, COX-2 AND LOX ENZYMES
TR2021021378A1 (en) INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF MALVA SYLVESTRIS L. FLOWERS ON COX-1, COX-2 AND LOX ENZYMES
Allam et al. Experimental study of the possible protective effect of alpha-lipoic acid on paracetamol induced oxidative stress and hepatic toxicity in albino rats
TR2021021375A2 (en) INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF ALLIUM SATIVUM L. ONIONS ON COX-1, COX-2 AND LOX ENZYMES
TR2021021391A2 (en) INHIBITORY EFFECTS OF STANDARDIZED EXTRACTS OF ROSMARINUS OFFICINALIS L. LEAVES ON COX-1, COX-2 AND LOX ENZYMES
TR2021021394A1 (en) INHIBITORY EFFECTS OF SALVIGENIN ON COX-1, COX-2 AND LOX ENZYMES
Alabdallat In-vivo antioxidant effects of the orally administered paracetamol, aqueous extracts of saliva triloba, and origanum syriacum
TR2021021374A1 (en) INHIBITORY EFFECTS OF ALLICIN ON COX-1, COX-2 AND LOX ENZYMES
TR2021021396A1 (en) INHIBITORY EFFECTS OF CHLOROGENIC ACID ON COX-1, COX-2 AND LOX ENZYMES
TR2021021389A1 (en) INHIBITORY EFFECTS OF ROSMARINIC ACID ON COX-1, COX-2 AND LOX ENZYMES