Ahmed Sarfaraz, Al-Rehaily Adnan J, Alam Perwez, Alqahtani Ali S, Hidayatullah Syed, Rehman Md Tabish, Mothana Ramzi A, Abbas Syed Sadiq, Khan M U, Khalid Jamal M, Siddiqui Nasir A
Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Zoology, Shia P.G. College, Lucknow University, Lucknow, India.
Saudi Pharm J. 2019 Jul;27(5):655-663. doi: 10.1016/j.jsps.2019.03.008. Epub 2019 Mar 19.
The present study demonstrates the miquelianin or quercetin 3--glucuronide (compound ) isolated from aerial parts of exhibited significant results for antioxidant and antidiabetic potential. The compound along with kaempferol 3--glucuronide (compound ) and quercetin 3--rhamnoside (compound ) isolated from the same source were quantified by validated HPTLC method. Antioxidant activity was determined by chemical means in terms of ABTS radical cation and DPPH radical scavenging activity. Compound showed significant scavenging activity in both ABTS and DPPH assays as compared to standard BHA. In ABTS method IC values of compound and standard BHA is found to be 58.90 ± 3.40 µg/mL and 28.70 ± 5.20 µg/mL respectively while in DPPH assay IC values of Compound and standard BHA is 47.20 ± 4.90 µg/mL and 34.50 ± 6.20 µg/mL respectively. Antidiabetic effect was studied through α-amylase and α-glucosidase inhibitory activity. The mechanistic approach through molecular modelling also support the strong binding sites of compound which showed significant α-amylase and α-glucosidase inhibitory activities with IC values 128.34 ± 12.30 and 89.20 ± 9.20 µg/mL respectively as compared to acarbose 64.20 ± 5.60 and 52.40 ± 4.60 µg/mL respectively. The results of validated RP-HPTLC analyses revealed the concentration of compound found to be 16.39 µg/mg and for compound and compound as 3.92 and 14.98 µg/mg of dried extract, respectively.
本研究表明,从[植物名称]地上部分分离得到的槲皮苷或槲皮素3 - O - 葡萄糖醛酸苷(化合物[X])在抗氧化和抗糖尿病潜力方面显示出显著效果。通过经过验证的高效薄层色谱法(HPTLC)对从同一来源分离得到的化合物[X]以及山奈酚3 - O - 葡萄糖醛酸苷(化合物[Y])和槲皮素3 - O - 鼠李糖苷(化合物[Z])进行了定量分析。通过化学方法,以ABTS阳离子自由基和DPPH自由基清除活性来测定抗氧化活性。与标准丁基羟基茴香醚(BHA)相比,化合物[X]在ABTS和DPPH测定中均表现出显著的清除活性。在ABTS法中,化合物[X]和标准BHA的半数抑制浓度(IC)值分别为58.90 ± 3.40 μg/mL和28.70 ± 5.20 μg/mL;而在DPPH测定中,化合物[X]和标准BHA的IC值分别为47.20 ± 4.90 μg/mL和34.50 ± 6.20 μg/mL。通过α - 淀粉酶和α - 葡萄糖苷酶抑制活性研究了抗糖尿病作用。通过分子建模的机制研究方法也支持化合物[X]具有较强的结合位点,其表现出显著的α - 淀粉酶和α - 葡萄糖苷酶抑制活性,IC值分别为128.34 ± 12.30和89.20 ± 9.20 μg/mL,相比之下,阿卡波糖的IC值分别为64.20 ± 5.60和52.40 ± 4.60 μg/mL。经过验证的反相高效薄层色谱法(RP - HPTLC)分析结果显示,化合物[X]的浓度为16.39 μg/mg,化合物[Y]和化合物[Z]的浓度分别为3.92和14.98 μg/mg干提取物。