Jatrophainolides A–C, new cembrane-type diterpenoids with PTP1B inhibitory activity from the root bark of Jatropha integerrima

2020 ◽  
Vol 36 ◽  
pp. 166-170
Author(s):  
Dong-Bo Zhang ◽  
Zheng Wang ◽  
Yan-Ni Liang ◽  
Jin-Gao Yu ◽  
Zhen Zhang ◽  
...  
2017 ◽  
Vol 33 (10) ◽  
pp. 1436-1441 ◽  
Author(s):  
Poomraphie Nuntawong ◽  
Virunh Kongkatitham ◽  
Kittisak Likhitwitayawuid ◽  
Wanwimon Mekboonsonglarp ◽  
Suchada Sukrong ◽  
...  

ChemInform ◽  
2008 ◽  
Vol 39 (28) ◽  
Author(s):  
JunPil Jang ◽  
MinKyun Na ◽  
Phuong Thien Thuong ◽  
Dieudonne Njamen ◽  
Joseph Tanyi Mbafor ◽  
...  

2020 ◽  
Vol 83 (4) ◽  
pp. 1229-1237 ◽  
Author(s):  
Yifan Fu ◽  
Xiaoyu Ding ◽  
Xianglei Zhang ◽  
Xingcheng Shao ◽  
Jihui Zhao ◽  
...  

2021 ◽  
Author(s):  
Po-Chun Chen ◽  
Bongani Sicelo Dlamini ◽  
Chiy-Rong Chen ◽  
Yueh-Hsiung Kuo ◽  
Wen-Ling Shih ◽  
...  

Abstract In the continuous search for α-glucosidase inhibitors, eleven phenolic compounds (1-11) were isolated from the root bark of Paeonia suffruticosa. Their α-glucosidase inhibitory activity and inhibition mechanism were investigated using an in vitro inhibition assay and molecular docking studies. Compounds 2, 5, 6, and 8-11 (IC50 between 290 and 431 µM) inhibited α-glucosidase more effectively than the reference compound acarbose (IC50=1463 ± 29.5 µM). Among them, compound 10 exhibited the highest α-glucosidase inhibitory effect with an IC50 value of 290.4 ± 9.6 µM. Compounds 2, 5, 9 10 and 11 were found to be competitive inhibitors, while compounds 6 and 8 were noncompetitive inhibitors of α-glucosidase. Computational analyses showed that the main binding forces between the compounds and the main residues were hydrogen bonds. The results indicated that these compounds had considerable α-glucosidase inhibitory activity.


Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2893 ◽  
Author(s):  
Srijan Shrestha ◽  
Su Hui Seong ◽  
Seul Gi Park ◽  
Byung Sun Min ◽  
Hyun Ah Jung ◽  
...  

Protein tyrosine phosphatase 1B (PTP1B) plays a specific role as a negative regulator of insulin signaling pathways and is a validated therapeutic target for Type 2 diabetes. Previously, arylbenzofurans were reported to have inhibitory activity against PTP1B. However, detailed investigation regarding their structure activity relationship (SAR) has not been elucidated. The main aim of this work was to investigate the PTP1B inhibitory activity of 2-arylbenzofuran analogs (sanggenofuran A (SA), mulberrofuran D2 (MD2), mulberrofuran D (MD), morusalfuran B (MB), mulberrofuran H (MH)) isolated from the root bark of Morus alba. All compounds demonstrated potent inhibitory activity with IC50 values ranging from 3.11 to 53.47 µM. Among the tested compounds, MD2 showed the strongest activity (IC50, 3.11 µM), followed by MD and MB, while SA and MH demonstrated the lowest activity. Lineweaver-Burk and Dixon plots were used for the determination of inhibition type whereas ligand and receptor interactions were investigated in modeled complexes via molecular docking. Our study clearly supports 2-arylbenzofuran analogs as a promising class of PTP1B inhibitors and illustrates the key positions responsible for the inhibitory activity, their correlation, the effect of prenyl/geranyl groups, and the influence of resorcinol scaffold, which can be further explored in-depth to develop therapeutic agents against T2DM.


2019 ◽  
Vol 25 (3) ◽  
pp. 268
Author(s):  
Young-Su Chang ◽  
Hong-Guang Jin ◽  
Hwan Lee ◽  
Dong-Sung Lee ◽  
Eun-Rhan Woo

2008 ◽  
Vol 56 (1) ◽  
pp. 85-88 ◽  
Author(s):  
JunPil Jang ◽  
MinKyun Na ◽  
Phuong Thien Thuong ◽  
Dieudonné Njamen ◽  
Joseph Tanyi Mbafor ◽  
...  

RSC Advances ◽  
2017 ◽  
Vol 7 (2) ◽  
pp. 805-812 ◽  
Author(s):  
Ya-Nan Yang ◽  
Ya-Wen An ◽  
Zhi-Lai Zhan ◽  
Jing Xie ◽  
Jian-Shuang Jiang ◽  
...  

Lycium chinense Mill. is a deciduous shrub in the Solanaceae family that is known for its fruits (Lycii fructus) and root bark (Lycii cortex).


2016 ◽  
Vol 26 (12) ◽  
pp. 2788-2794 ◽  
Author(s):  
Manh Tuan Ha ◽  
Manh Hung Tran ◽  
Kim Jeong Ah ◽  
Kyung-Jin Jo ◽  
Jaewang Kim ◽  
...  

Author(s):  
Pınar Ercan ◽  
Sedef Nehir El

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.


Sign in / Sign up

Export Citation Format

Share Document