Chemical Constituents with Proprotein Convertase Subtilisin/Kexin Type 9 mRNA Expression Inhibitory Activity from Dried ImmatureMorus albaFruits

2017 ◽  
Vol 65 (26) ◽  
pp. 5316-5321 ◽  
Author(s):  
Pisey Pel ◽  
Hee-Sung Chae ◽  
Piseth Nhoek ◽  
Young-Mi Kim ◽  
Young-Won Chin
Keyword(s):  
Mrna Expression ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Proprotein Convertase

scholarly journals Chemical Constituents with Inhibitory Activities on Proprotein Convertase Subtilisin/kexin Type 9 Expression from the Aerial Parts of Penthorum chinense

2020 ◽  
Author(s):  
Pisey Pel ◽  
Hee-Sung Chae ◽  
Jinwoo Cho ◽  
Young-Mi Kim ◽  
Jungmoo Huh ◽  
...  
Keyword(s):  
Mrna Expression ◽  
Chemical Constituents ◽  
Density Lipoprotein ◽  
Infectious Hepatitis ◽  
Enzyme Linked Immunosorbent Assay ◽  
Methyl Gallate ◽  
Proprotein Convertase ◽  
Active Constituents ◽  
Inhibitory Activities ◽  
Penthorum Chinense

Abstract Background: Penthorum chinense has been used in East Asia for the treatment of cholecystitis, infectious hepatitis, and jaundice. So far there is no report regarding proprotein convertase subtilisin/kexin type 9 inhibitory constituents from this plant. The aim of the present study was to discover new active constituents with PCSK9 expression inhibitory activities from P. chinenseMethods: All structures were established by interpreting NMR spectroscopic data and MS data. Further experimental and calculated ECD data were used to determine the absolute configuration of the two new neolignans. To monitor the inhibitory activity on proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA expression and PCSK9-low density lipoprotein receptor (LDLR) interaction, quantitative real time-PCR, Western blot analysis, and an enzyme-linked immunosorbent assay (ELISA) method by a PCSK9-biotinylated-LDLR binding assay were performed.Results: 39 compounds were isolated and identified including two new oxepine-type neolignans, penthorinols A (1) and B (2) and a naturally occurring chalcone, 6'-hydroxy-2'-methoxychalcone-4'-O-β-D-glucopyranoside (20). Of all tested compounds, penthorin A (4) and methyl gallate (25) were found to suppress PCSK9 mRNA expression with IC50 values of 15.56 and 11.66 µM, respectively. Furthermore, penthorin A (4) and methyl gallate (25) downregulated PCSK9 protein expression. However, all compounds seemed to be inactive in PCSK9-LDLR interaction.Conclusion: In the present study, two new compounds was discovered from this plant and active constituents with PCSK9 expression inhibitory activities were suggested.

scholarly journals Antiglycation potential of Indigoferin a, Indigoferin B and Indigoferin C natural products from Indigofera heterantha Brandis

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Ayesha Khan ◽  
Ajmal Khan ◽  
Manzoor Ahmad ◽  
Mumtaz Ali ◽  
Umar Farooq ◽  
...  
Keyword(s):  
Natural Products ◽  
Diabetic Complications ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Intramolecular Hydrogen Bonding ◽  
Glycation End Products ◽  
End Products ◽  
Serious Disease ◽  
Intramolecular Hydrogen

Abstract Background Diabetes is a long-lasting and serious disease that effect in worldwide individual lives, families, and societies. Hyperglycemia of diabetes mellitus produced Advance Glycation End Products that are associated with diabetic complications like neuropathy, nephropathy, retinopathy, and cardiovascular diseases. Methods In this study, the natural products isolated from of Indigofera heterantha Brandis, Indigoferin A (S1), Indigoferin B (S2) and Indigoferin C (S3) were evaluated for their in vitro antiglycation activity. Results The compounds exhibited a significant inhibitory activity against the formation of Advanced Glycation End-Products with IC50 values of 674.25 ± 3.2 μM, 407.03 ± 4.7 μM and 726.41 ± 2.1 μM, respectively. Here, important structure-activity relationship was observed, when the intramolecular hydrogen bonding interactions suppressed the antiglycation activity of compound S3. Thus, the study clearly demonstrates that the number and the position of substituents act as an assisting factor and directly influence the inhibitory activity of the natural product by altering the sugar or protein binding affinity. Conclusions This study explain first time the antiglycation inhibitory ability of chemical constituents isolated from I. heterantha and can be used for above late diabetic complications.

Dammarane-type saponins with proprotein convertase subtilisin/kexin type 9 inhibitory activity from Gynostemma pentaphyllum

2022 ◽  
Vol 194 ◽  
pp. 113005
Author(s):  
Ya-Ping Huang ◽  
Yun-Shan Wang ◽  
Bi-Wen Liu ◽  
Zhe Song ◽  
Xiao-Shuang Liang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Proprotein Convertase ◽  
Gynostemma Pentaphyllum

Glutathione S-Transferase, Acetylcholinesterase Inhibitory and Antibacterial Activities of Chemical Constituents of Barleria prionitis

2007 ◽  
Vol 62 (4) ◽  
pp. 580-586 ◽  
Author(s):  
Kalhari S. Kosmulalage ◽  
Shamsulhaq Zahid ◽  
Chibuike C. Udenigwe ◽  
Sarfraz Akhtar ◽  
Athar Ata ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Spectroscopic Studies ◽  
Sri Lankan ◽  
Glutathione S Transferase ◽  
Ache Inhibitory Activity ◽  
Phytochemical Studies ◽  
Derivatives Of

Phytochemical studies on the ethanolic extract of Barleria prionitis of Sri Lankan origin have resulted in the isolation of a new compound, balarenone (1), along with three known compounds, pipataline (2), lupeol (3) and 13,14-seco-stigmasta-5,14-diene-3-α-ol (4). The structures of 1 - 4 were elucidated with the aid of extensive NMR spectroscopic studies. Compounds 1 - 4 showed moderate inhibitory activity against glutathione S-transferase (GST) and acetylcholinesterase (AChE). Compounds 1, 2 and 4 also exhibited antibacterial activity against Bacillus cereus and Pseudomonas aeruginosa (25 μg/disk). Three different derivatives of compound (2), 7,8-epoxypipataline (5), 8- amino-7-hydroxypipataline (6) and 7,8-dibromopipataline (7) were synthesized to evaluate them for GST and AChE inhibitory activities. Household microwave radiations were used to synthesize compound (6). Among all tested compounds, 8-amino-7-hydroxypipataline (6) exhibited a significant AChE inhibitory activity with an IC50 value of 36.8 μM.

scholarly journals Rotenoid Derivatives from Derris Trifoliata with Nitric Oxide Production Inhibitory Activity

2012 ◽  
Vol 7 (11) ◽  
pp. 1934578X1200701
Author(s):  
Chihiro Ito ◽  
Tomiyasu Murata ◽  
Hugh T.-W. Tan ◽  
Norio Kaneda ◽  
Hiroshi Furukawa ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Interferon Γ ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Nitric Oxide Production ◽  
Murine Macrophage ◽  
Isolation And Identification ◽  
Oxide Production

Study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) collected in Singapore led to the isolation and identification of three known and two new rotenoid derivatives. The new derivatives, named derrisfolin A (1) and B (2), inhibited nitric oxide production in murine macrophage-like RAW 264.7 cells stimulated with interferon-γ and lipopolysaccharide.

scholarly journals Anti-acne vulgaris effect including skin barrier improvement and 5α-reductase inhibition by tellimagrandin I from Carpinus tschonoskii

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Jun Yin ◽  
In Hyoek Hwang ◽  
Min Won Lee
Keyword(s):  
Mrna Expression ◽  
Inhibitory Activity ◽  
Acne Vulgaris ◽  
Skin Barrier ◽  
Positive Control ◽  
Skin Barrier Function ◽  
Rat Liver Microsomes ◽  
Dependent Manner ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Abstract Background Carpinus tschonoskii (CT) has been previously studied for various activities in the improvement of skin diseases. In the present study, we examined the in vitro anti-acne vulgaris (AV) effect of CT leaves (CTL) and tellimagrandin I (TI), one of the main ellagitannins from CT, including skin barrier improvement and 5α-reductase inhibitory activity. Methods To test the anti-AV activities of CTL and TI, firstly, anti-oxidative and anti-inflammatory activities including DPPH radical scavenging activity, nitric oxide (NO) inhibitory activity, and cytokines [interleukin (IL)-6 and IL-8] were tested. Skin barrier improvement experiments were tested using developing cornified envelope (CE) formation, and filaggrin mRNA expression level was determined by RT-PCR. The 5α-reductase inhibitory activity was determined by measuring the testosterone levels in rat liver microsomes. Results CTL and TI showed potent anti-oxidative activity and anti-inflammatory activities. Especially, the cytokine production inhibitory activities of TI were found to be similar to the positive control, epigallocatechin gallate (EGCG). CTL and TI enhanced the CE formation and filaggrin mRNA expression levels and showed potent activities compared to that in the positive control, 1.5 mM Ca2+. In additionally, CTL and TI showed 5α-reductase inhibitory activities in a dose-dependent manner. Conclusion The results showed that CTL and TI inhibit AV endogenous factors such as 5α-reductase and inflammatory cytokines and affect exogenous factors such as developing skin barrier function (CE and filaggrin levels). Therefore, CTL and TI may be plant-derived agent, promising in the treatment of acne vulgaris.

scholarly journals Chemical constituents and ACE inhibitory activity of desert plant Suaeda physophora Pall.

2013 ◽  
Vol 3 (5) ◽  
pp. 328-332 ◽  
Author(s):  
Ruizhi Men ◽  
Ning Li ◽  
Yachao Xing ◽  
Yingzhan Tang ◽  
Chengyu Tan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Desert Plant ◽  
Ace Inhibitory Activity ◽  
Ace Inhibitory ◽  
Suaeda Physophora
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