PSU Knowledge Bank Community:http://kb.psu.ac.th:80/psukb/handle/2553/35802024-03-28T16:58:23Z2024-03-28T16:58:23Zชาสมุนไพรสำหรับลดระดับน้ำตาลในเลือดผ่านการยับยั้งเอนไซม์แอลฟากลูโคซิเดสสุกัญญา เดชอดิศัยhttp://kb.psu.ac.th:80/psukb/handle/2016/181392023-05-11T03:18:58Z2566-01-01T00:00:00ZTitle: ชาสมุนไพรสำหรับลดระดับน้ำตาลในเลือดผ่านการยับยั้งเอนไซม์แอลฟากลูโคซิเดส
Authors: สุกัญญา เดชอดิศัย2566-01-01T00:00:00Zการพัฒนาอนุพันธ์ Mitragynine ที่คาดว่ามีฤทธิ์ยับยั้งเอนไซม์ Acetylcholinesteraseลือลักษณ์ ล้อมลิ้มวรมย์ญลิน ทิพย์มณีจุไรทิพย์ หวังสินทวีกุลhttp://kb.psu.ac.th:80/psukb/handle/2016/181362023-05-11T02:31:47Z2566-01-01T00:00:00ZTitle: การพัฒนาอนุพันธ์ Mitragynine ที่คาดว่ามีฤทธิ์ยับยั้งเอนไซม์ Acetylcholinesterase
Authors: ลือลักษณ์ ล้อมลิ้ม; วรมย์ญลิน ทิพย์มณี; จุไรทิพย์ หวังสินทวีกุล2566-01-01T00:00:00ZStudy on α-Glucosidase Inhibitors from Solanum stramonifolium Jacq. Inflorescence and Neuropeltis racemosa Wall. StemOraphan Sakulkeohttp://kb.psu.ac.th:80/psukb/handle/2016/180012023-04-19T08:15:42Z2022-01-01T00:00:00ZTitle: Study on α-Glucosidase Inhibitors from Solanum stramonifolium Jacq. Inflorescence and Neuropeltis racemosa Wall. Stem
Authors: Oraphan Sakulkeo
Abstract: This research was the first report, which studied on the phytochemical investigation and potential anti-diabetic effect of two plants from order Solanales, Solanum stramonifolium Jacq. inflorescence and Neuropeltis racemosa Wall. stem. The plant extracts were evaluated the α-glucosidase inhibitory activity. The ethyl acetate extract of S. stramonifolium (SSEA) inflorescence and the ethanol extract of N. racemosa (NREO) stem showed better inhibitory activity than other solvent extracts with IC50 215.92 and 39.65 μg/ml, respectively. Both of these extracts performed mixed-type inhibition. The combination study of extracts with acarbose standard suggested that SSEA and NREO extracts promoted the activity of acarbose to inhibit the α-glucosidase enzyme. The isolation used the α-glucosidase inhibitory activity guided fractionation. Ten compounds and one mixture compound were obtained. The five compounds and a mixture compound from S. stramonifolium were identified as flavonoid compounds that were myricetin 3, 4, 5, 7-tetramethyl ether (SS1), combretol (SS2), kaempferol (SS3), kaempferol-7-O--glucopyranoside (SS4), 5-hydroxy3, 7, 4, 5 -tetramethoxyflavone-3-O-glucopyranoside (SS5), and a mixture (SS6) of isorhamnetin-3-O-glucopyranoside (SS6-1) and kaempferol-3-O-glucopyranoside (SS6-2). Other five compounds from N. racemosa were defined as scopoletin (NR1), syringic acid (NR2), methyl 3-methyl-2-butenonoate (NR3), trans-N-feruloyltyramine (NR4) and trans-N-coumaroyltyramine (NR5). From previous survey, the compound of SS5 has not been reported before. The isolated flavonoid compounds of S. stramonifolium were obtained small amount. So, they were preformed the α-glucosidase inhibitory activity as the percent of inhibition. Kaempferol and kaempferol-3-O-glucopyranoside (astragalin) were used as the representative compounds for the study on mechanism of action and enzyme inhibition of the combination with acarbose. Both of kaempferol and astragalin performed mixed-type inhibition with α-glucosidase. Additionally, α-glucosidase inhibitory acitvity of acarbose was decreased when combined with kaempferol or astragalin. The compound NR1, NR2, NR3, NR4 and NR5 of N. racemosa showed α-glucosidase inhibitory acitvity with IC50 as 577.46, >2,523.09, >4,380.59, 95.34 and 3.25 μM, respectively, whereas the acarbose presented IC50 as 424.40 μM. The mechanism of action analysis exhibited that NR1 displayed mixed-type inhibition manner, while NR4 and NR5 exhibited uncompetitive inhibition manner with Ki 51.81 and 1.99 μM, respectively. Moreover, the molecular docking study provided the understanding to α-glucosidase inhibition of isolated compounds. For the flavonoid compounds from S. stramonifolium, the non-glycosylated flavonoids (SS2 and SS3) showed lower binding energy than their glycosylated flavonoid derivatives (SS4, SS5 and SS6-2). The binding energy of SS2 showed -3.53 Kcal/mol, while SS5 was 63.78 Kcal/mol. SS3 exhibited the binding energy as -3.02 Kcal/mol, while SS4 and SS6-2 were -1.29 and 55.47 Kcal/mol, respectively. So, non-glycosylated flavonoids exhibited better α-glucosidase inhibitory activity than glycosylated flavonoid derivatives. For the isolated tyramine-derived amides from N. racemosa, the binding energy of NR4 and NR5 were -5.42 and -5.15 Kcal/mol, respectively. Both of NR4 and NR5 demonstraded the potential to α-glucosidase inhibition. Fortunately, these findings could be used to relate the accordance between the laboratory and the computer experiments. These results will be the beneficial informations for the furture drug discovery.
Description: Doctor of Philosophy (Pharmaceutical Sciences), 20222022-01-01T00:00:00Zฤทธิ์ต้านเบาหวานของอนุพันธ์อินเตอร์รับตินที่สกัดจากเฟิร์นไซโคลซอรัส เทอร์มิแนนส์สิรีวรรณ แก้วสุวรรณhttp://kb.psu.ac.th:80/psukb/handle/2016/176442022-11-21T04:04:17Z2562-01-01T00:00:00ZTitle: ฤทธิ์ต้านเบาหวานของอนุพันธ์อินเตอร์รับตินที่สกัดจากเฟิร์นไซโคลซอรัส เทอร์มิแนนส์
Authors: สิรีวรรณ แก้วสุวรรณ
Abstract: The fern Cyclosorus terminans has long been consumed as a vegetable in northern Thailand. It has been reported as the source of coumarin derivatives, interruptins A and B. In this study, they were found to exhibit in vitro antidiabetic property by enhancing the glucose consumption into hepatocytes and skeletal muscle cells through PPAR-Y pathway. Likewise, both interruptins A and B also increased glycogen accumulation in heptaocytes, while only interruptin B could encourage glycogen content in muscle cells. Interestingly, prepared interruptin-rich extract (IRE) demonstrated not only no cytotoxicity toward hepatocytes and skeletal muscle cells, but also activated glucose uptake into both cells. Furthermore, acute toxicity study Wistar rats revealed no mortality or signs of toxicity after a single oral of 2,000 mg/kg IRE administration and indicated the LDso as 2,000-5,000 mg/kg body weight. Moreover, interruptin B displayed potent anti-inflammation through NO radical scavenging and NO production inhibition in macrophage RAW264.7 cells with ICso of 67.68 and 0.81 JM followed by interruptin A with JCso of 90.07 and 12.18 |uM, respectively. These compounds also down-regulated iNOS and up-regulated PPAR-Y mRNA expression in a dose-dependent manner. Additionally, the appropriate HPLC method for analysis the corresponding interruptins content in C. terminans extract was successfully validated according to ICH requirement. To the best of our knowledge, this is the first study describing anti-diabetic activity in liver and muscle cells and anti-inflammatory activity in macrophage cells of isolated interruptins A and B. These actions may be due to an induction of PPAR-Y. These results are very promising to find that C. terminans extract with
active interruptin derivatives might be a potential natural material for anti-diabetic application. Nevertheless, more research is still required to address questions surrounding in vivo anti-diabetes.2562-01-01T00:00:00Z