Tuğba Günbatan1, İlhan Gürbüz2, Erdal Bedir3, Ayşe Mine Gençler Özkan4, Özge Özçınar5. 1. Gazi University, Faculty of Pharmacy, Department of Pharmacognosy, Etiler, 06330, Ankara, Turkey. Electronic address: tugbagunbatan86@yahoo.com. 2. Gazi University, Faculty of Pharmacy, Department of Pharmacognosy, Etiler, 06330, Ankara, Turkey. Electronic address: igurbuz@gazi.edu.tr. 3. Izmir Institute of Technology, Department of Bioengineering, Urla, 35430, Izmir, Turkey. Electronic address: erdalbedir@iyte.edu.tr. 4. Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Botany, Tandoğan, 06100, Ankara, Turkey. Electronic address: gencler_65@yahoo.com. 5. Ege University, Faculty of Pharmacy, Department of Pharmacognosy, Bornova, 35040, Izmir, Turkey. Electronic address: ozge.ozcinar7@gmail.com.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Sideritis caesarea H. Duman, Aytaç & Başer are used for complaints such as stomach-aches, and intestinal spasms as traditional medicine in Kayseri, Turkey. AIM OF STUDY: To investigate the anti-ulcerogenic activity by using bioassay guided fractionation technique (BAGF) and to identify the compound(s) that are responsible for anti-ulcerogenic activity through ethanol-induced anti-ulcerogenic activity model in vivo. MATERIALS AND METHODS: Liquid-liquid partition and then different chromatographic techniques were utilized for the BAGF of the ethanol (80%) extract of the aerial parts of Sideritis caesarea. Ethanol-induced gastric ulcer method on rats was employed for the determination of the anti-ulcerogenic activity, and the ulcer index was also calculated for anti-ulcerogenic activity detection. RESULTS: The ethanol (80%) extract of S. caesarea showed statistically potent anti-ulcerogenic activity (95.9% ulcer inhibition, p < 0.001). Among the liquid-liquid fractions, strongest anti-ulcerogenic activity was observed with the ethyl acetate fraction (91.4% inhibition, p < 0.001) and therefore BAGF studies were proceeded with the ethyl acetate fraction. Two anti-ulcerogenic flavonoids {4'-O-methylhypolaetin-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-6″-O-acetyl-β-D-glucopyranoside and isoscutellarein-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-6″-O-acetyl-β-D-glucopyranoside} were isolated from this fraction together with a sesquiterpene glycoside [(2E,6E)-2,6,10-trimethyl-2,6,11-dodecatriene-1,10-diol-1-O-β-D-glucopyranoside] and two additional flavonoids {4'-O-methylhypolaetin-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-β-D-glucopyranoside and isoscutellarein-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-β-D-glucopyranoside}. CONCLUSIONS: Traditional use of S. caesarea in the treatment of stomach-aches was supported by this study and four flavonoids were isolated by using BAGF method and two of them were determined to have significant anti-ulcerogenic activity. Additionally, (2E,6E)-2,6,10-trimethyl-2,6,11-dodecatriene-1,10-diol-1-O-β-D-glucopyranoside was obtained from a Sideritis genus for the first time.
ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Sideritis caesarea H. Duman, Aytaç & Başer are used for complaints such as stomach-aches, and intestinal spasms as traditional medicine in Kayseri, Turkey. AIM OF STUDY: To investigate the anti-ulcerogenic activity by using bioassay guided fractionation technique (BAGF) and to identify the compound(s) that are responsible for anti-ulcerogenic activity through ethanol-induced anti-ulcerogenic activity model in vivo. MATERIALS AND METHODS: Liquid-liquid partition and then different chromatographic techniques were utilized for the BAGF of the ethanol (80%) extract of the aerial parts of Sideritis caesarea. Ethanol-induced gastric ulcer method on rats was employed for the determination of the anti-ulcerogenic activity, and the ulcer index was also calculated for anti-ulcerogenic activity detection. RESULTS: The ethanol (80%) extract of S. caesarea showed statistically potent anti-ulcerogenic activity (95.9% ulcer inhibition, p < 0.001). Among the liquid-liquid fractions, strongest anti-ulcerogenic activity was observed with the ethyl acetate fraction (91.4% inhibition, p < 0.001) and therefore BAGF studies were proceeded with the ethyl acetate fraction. Two anti-ulcerogenic flavonoids {4'-O-methylhypolaetin-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-6″-O-acetyl-β-D-glucopyranoside and isoscutellarein-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-6″-O-acetyl-β-D-glucopyranoside} were isolated from this fraction together with a sesquiterpene glycoside [(2E,6E)-2,6,10-trimethyl-2,6,11-dodecatriene-1,10-diol-1-O-β-D-glucopyranoside] and two additional flavonoids {4'-O-methylhypolaetin-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-β-D-glucopyranoside and isoscutellarein-7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-β-D-glucopyranoside}. CONCLUSIONS: Traditional use of S. caesarea in the treatment of stomach-aches was supported by this study and four flavonoids were isolated by using BAGF method and two of them were determined to have significant anti-ulcerogenic activity. Additionally, (2E,6E)-2,6,10-trimethyl-2,6,11-dodecatriene-1,10-diol-1-O-β-D-glucopyranoside was obtained from a Sideritis genus for the first time.