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    7-Acetoxyhorminone from Salvia multicaulis Vahl. as Promising Inhibitor of 3-Hydroxy-3-methylglutaryl Coenzyme A (HMG-CoA) Reductase
    (MDPI, 2022) Yiğitkan, Serkan; Ertaş, Abdulselam; Salmas, Ramin Ekhteiari; Fırat, Mehmet; Orhan, İlkay Erdoğan
    3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase is a key enzyme involved in cholesterol biosynthesis and one of the most important targets for the treatment of hy-percholesterolemia. A limited number of studies on the HMG-CoA reductase inhibitory potential of natural products are available. Thus, in the current study, we aimed to test the HMG-CoA re-ductase inhibitory capacity of extracts from the roots and aerial parts of Salvia multicaulis Vahl., through activity-guided isolation. Our findings revealed that the root extract prepared with di-chloromethane–acetone (1:1) showed the highest inhibition (71.97 ± 0.37%) at 100 µg/mL. The extract was then initially fractionated by column chromatography and the obtained fractions were monitored by thin layer chromatography. Fractions which were similar to each other were combined and a total of 15 fractions were obtained. Further conventional chromatographic studies were carried out on the active fractions. Based on these fractions, 10 known compounds, compris-ing 9 terpenes and 1 steroid derivative in total, were isolated and their structures were verified by a combination of IT-TOF-MS, and 1D and 2D NMR techniques. According to the enzyme inhibition data of the identified compounds, 7-acetoxyhorminone exerted the highest inhibition (84.15 ± 0.10%, IC50 = 63.6 ± 1.21 µg/mL). The molecular docking experiments on 7-acetoxyhorminone and horminone indicated that both compounds strongly bind to the active site of the enzyme.
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    A comprehensive study on chemical and biological investigation of thymus brachychilus jalas: A rich source of ursolic and oleanolic acids
    (Taylor & Francis Inc, 2023) Akdeniz, Mehmet; Yiğitkan, Serkan; Yılmaz, Mustafa Abdullah; Yener, İsmail; Varhan Oral, Elif; Fırat, Mehmet; Orhan, İlkay Erdoğan
    The significance of Thymus species in the scientific community is growing steadily due to their extensive utilization in traditional medicine, food industry, and pharmaceutical sector, owing to their abundance in essential oil and phytochemical content, rendering them commercially significant species. The current work focuses on conducting a comprehensive analysis of the ethanol extract and essential oil derived from the root and aerial portions of Thymus brachychilus Jalas, an endemic species that has not been previously investigated. Additionally, a novel GC-MS (gas chromatography-mass spectrometry) technique was developed to quantify the levels of triterpenoids, which are frequently found in many plants, particularly those belonging to the Lamiaceae family. The approach was then used to assess the triterpenoid content of the species. While the phenolic content of the species was determined by LC-MS/MS (liquid chromatography-tandem mass spectrometry), the chemical composition of triterpenoid, essential oil and flavor (aroma) of the plant was determined by GC-MS. Eucalyptol was the primary ingredient in both the essential oil and the flavor, accounting for 11.05% and 12.35%, respectively. In the DPPH and ABTS radical scavenging techniques, the root ethanol extract exhibited the greatest antioxidant activity with IC50 values of 26.70 +/- 0.23 and 19.16 +/- 0.11 mu g/mL, respectively. There was a high level of urease (59.54 +/- 1.67% at 100 mu g/mL) inhibitory activity observed in the root ethanol extract in enzyme inhibition assays, as well as angiotensin (94.80 +/- 0.56%), elastase (40.19 +/- 0.39%), and collagenase (48.26 +/- 0.12%) inhibition in the aerial ethanol extract. Moreover, the MCF-7 cell line for breast cancer had a strong cytotoxic impact when exposed to the essential oil of the species (vitality%: 1.45 +/- 0.01 at 200 mu g/mL. The LC-MS/MS and GC-MS studies revealed that the roots had a significant concentration of rosmarinic acid (15,801 mu g analyte/g extract), but the aerial portions had a substantial quantity of ursolic acid (152,374 mu g analyte/g extract). The plant exhibits potential in the food, cosmetic, and pharmaceutical sectors on account of its elevated levels of rosmarinic and ursolic acid, superior antioxidant capacity, and angiotensin and urease inhibitory effect.
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    Öğe
    LAMIACEAE FAMİLYASINA AİT 37 TIBBİ BİTKİNİN HMG-KOA REDÜKTAZ İNHİBİTÖR AKTİVİTELERİ
    (Gazi Üniversitesi, 2020) Yiğitkan, Serkan; Ertaş, Abdulselam; Fırat, Mehmet; Yeşil, Yeter; Orhan, İlkay Erdoğan
    3-Hidroksi-3-metil-glutaril-koenzim A (HMG-KoA) redüktaz enzimi kolesterol biyosentezinde görev alan anahtar enzimdir. Dolayısıyla HMG-KoA redüktaz inhibisyonu hiperkolesterolemi tedavisi için en önemli hedeflerden biridir. Diğer yandan, yeni ilaç keşfi araştırmalarında tıbbi bitkiler ve bunlardan izole edilen moleküller önemli bir yer tutmaktadır. Bu çalışmada, Türkiye’de yetişen ve daha önce bu enzime yönelik olarak üzerinde araştırma yapılmamış olan Lamiaceae familyasına ait 37 bitki taksonunun etanol ekstrelerinin in vitro HMG-KoA redüktaz enzim inhibisyon aktiviteleri ELISA mikroplak yöntemi kullanılarak araştırılmıştır. Taramamız sonucunda Salvia inhibitör etkili bulunan ekstreler, Salvia multicaulis Vahl. (% 61,66 ± 1,52) ve Salvia blepharochlaena Hedge & Hub.Mor. (% 55,21 ± 1,12) olarak tespit edilmiştir.