scholarly journals Antioxidant, Anti-Inflammatory, and Antidiabetic Activities of Bioactive Compounds from the Fruits of Livistona chinensis Based on Network Pharmacology Prediction

2021 ◽  
Vol 2021 ◽  
pp. 1-21
Author(s):  
Yuwei Wang ◽  
Jianxiu Zhai ◽  
Dan Yang ◽  
Na Han ◽  
Zhe Liu ◽  
...  

In this study, a chemical investigation on the fruits of Livistona chinensis (FLC) led to the isolation and identification of 45 polyphenols and 5 alkaloids, including two new compounds (Livischinol (1) and Livischinine A (46)), an undescribed compound (47) and 47 known compounds. FLC was predicted with novel potential antidiabetic function by collecting and analyzing the potential targets of the ingredients. Compound 32 exhibited significant α-glucosidase inhibitory activity ( I C 50 = 5.71  μM) and 1, 6, and 44 showed the PTP1B inhibitory activity with IC50 values of 9.41-22.19 μM, while that of oleanolic acid was 28.58 μM. The competitive inhibitors of PTP1B (compounds 1 and 44) formed strong binding affinity, with catalytic active sites, proved by kinetic analysis, fluorescence spectra measurements, and computational simulations, and stimulated glucose uptake in the insulin-resistant HepG2 cells at the dose of 50 μM. In addition, FLC was rich in antioxidant and anti-inflammatory bioactive compounds so that they could be developed as nutraceuticals against diabetes.

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.


2021 ◽  
Vol 4 (1) ◽  
pp. 108
Author(s):  
Devi Ayu Septiani ◽  
Aliefman Hakim ◽  
Lalu Raftha Patech ◽  
Zulhalifah Zulhalifah ◽  
Siswadi Siswadi

Sambiloto plant (Andrographis paniculata Ness) is a plant that has been used as medicine from generation to generation. Bioactive compounds in Sambiloto have pharmacological effects such as immunostimulants (increase immunity), antibiotic diuretics (facilitate urine), antipyretics, anti-inflammatory (anti-inflammatory), hepatoprotective, hypotensive, hypoglycemic, antibacterial, anti-inflammatory, respiratory tract, and heart and lung meridians - lungs. The bioactive compound in Sambiloto which is mostly found in the leaves is Andrographolide. In this study, the isolation of Andrographolide from the leaves of the sambiloto plant (Andrographis paniculata Ness) was carried out using purification and crystallization methods aimed at obtaining pure Andrographolide isolates more efficiently and identifying the results of Andrographolide isolates. The results showed that the isolates obtained using the purification and crystallization methods obtained a yield of 0.47%. In the qualitative test of Andrographolide isolates using eluent and acetate: n-hexane (3: 2), the Rf value was 0.38. The results obtained from Andrographolide isolates using infrared spectroscopy (FT-IR) were identical to the literature on Andrographolide. The absorption peaks at the wavenumbers obtained includes 3400,41 cm-1, 1979,68 cm-1, 1959,46 cm-1, 2928,22 cm-1, 1727,56 cm-1, 1646,98 cm-1, and 907,53 cm-1.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Naiqiang Zhu ◽  
Jingyi Hou

AbstractInflammation, a protective response against infection and injury, involves a variety of biological processes. Sophorae Flavescentis (Kushen) is a promising Traditional Chinese Medicine (TCM) for treating inflammation, but the pharmacological mechanism of Kushen’s anti-inflammatory effect has not been fully elucidated. The bioactive compounds, predicted targets, and inflammation-related targets of Kushen were obtained from open source databases. The “Component-Target” network and protein–protein interaction (PPI) network were constructed, and hub genes were screened out by topological analysis. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed on genes in the PPI network. Furthermore, nitric oxide (NO) production analysis, RT-PCR, and western blot were performed to detect the mRNA and protein expression of hub genes in LPS-induced RAW264.7 cells. An immunofluorescence assay found that NF-κB p65 is translocated. A total of 24 bioactive compounds, 465 predicted targets, and 433 inflammation-related targets were identified and used to construct “Component-Targets” and PPI networks. Then, the five hub genes with the highest values-IL-6, IL-1β, VEGFA, TNF-α, and PTGS2 (COX-2)- were screened out. Enrichment analysis results suggested mainly involved in the NF-κB signaling pathway. Moreover, experiments were performed to verify the predicted results. Kushen may mediate inflammation mainly through the IL-6, IL-1β, VEGFA, TNF-α, and PTGS2 (COX-2), and the NF-κB signaling pathways. This finding will provide clinical guidance for further research on the use of Kushen to treat inflammation.


Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3750
Author(s):  
Xiao-Yan Liu ◽  
You-Bo Zhang ◽  
Xiu-Wei Yang ◽  
Yan-Fang Yang ◽  
Wei Xu ◽  
...  

The dried vine stems of Spatholobus suberectus are commonly used in traditional Chinese medicine for treating gynecological and cardiovascular diseases. In this study, five new compounds named spasuberol A (2), homovanillyl-4-oxo-nonanoate (5), spasuberol C (6), spasuberoside A (14), and spasuberoside B (15), together with ten known compounds (1, 3, 4, 7–13), were isolated from the dried vine stems of S. suberectus. Their chemical structures were analyzed using spectroscopic assays. This is the first study interpreting the detailed structural information of 4. The anti-inflammatory activity of these compounds was evaluated by reducing nitric oxide overproduction in RAW264.7 macrophages stimulated by lipopolysaccharide. Compounds 1 and 8–10 showed strong inhibitory activity with half maximal inhibitory concentration (IC50) values of 5.69, 16.34, 16.87, and 6.78 μM, respectively, exhibiting higher activity than the positive drug l-N6-(1-iminoethyl)-lysine (l-NIL) with an IC50 value of 19.08 μM. The IC50 values of inhibitory activity of compounds 2 and 4–6 were 46.26, 40.05, 45.87, and 28.29 μM respectively, which were lower than l-NIL, but better than that of positive drug indomethacin with an IC50 value of 55.44 μM. Quantitative real-time polymerase chain reaction analysis revealed that assayed compounds with good anti-inflammatory activity, such as 1, 6, 9, and 10 at different concentrations, can reduce the messenger RNA (mRNA) expression of some pro-inflammatory cytokines such as tumor necrosis factor α (TNF-α), nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX-2). The anti-inflammatory activity and the possible mechanism of the compounds mentioned in this paper were studied preliminarily.


Author(s):  
Alina K. Sebastian ◽  
P. V. Anto

Sclerotium stipitatum Berk. et. Curr., locally known as ‘nilamanga’ is a rare macro fungus, traditionally used to treat numerous diseases like arthritis, earache, jaundice etc. The present study aims to evaluate the anti-inflammatory activity of ethanol extract of S. stipitatum and identify the bioactive compounds present in them. Phytochemical screening of extracts obtained using different solvents like petroleum ether, chloroform, ethanol and water were done. The best extract was chosen for the acute carrageenan-induced and chronic formalin-induced anti-inflammatory studies. Diclofenac was used as the standard drug. Ethanol extract showed significant inhibition of inflammation induced by carrageenan and formalin-induced paw edema models compared to the control. GC-MS analysis shows certain bioactive compounds. The significant inhibitory effect on paw edema proves that S. stipitatum possesses remarkable anti-inflammatory activity, and isolation and identification of bioactive compounds can be used for new drug formulations.


Author(s):  
Saad R. Atta-Allah ◽  
Ibrahim F. Nassar ◽  
Wael A. El-Sayed

Background & Objectives: New N-substituted 5-(oxoindolinyl)-2-thioxo- thiazolidinone derivatives were synthesized. Methods: The C2 -substituted thiazolidinone derivatives with piperidinyl and morpholinyl moieties in addition to the tetracyclic [(oxindolo)pyrazino]thiazolidine, the chloro- and amino- derivatives of the (indolyl)thiazolidinone ring system were also prepared. Results: The COX-2 inhibition activity of the synthesized compounds was investigated by studying their ability to inhibit the conversion of arachidonic acid to prostaglandin H2 (PGH2). Five of the tested candidates, substituted (oxonidolyl)thiazolidine derivatives (3a, 6f, 8b, 10 and 12) showed significant COX-2 inhibitory activity exhibiting IC50 values better than or close to the reference celecoxib. The anti-inflammatory activity was studied revealing that a number of compounds have shown good activities and compound 10 produced no significant mucosal injury. Conclusion: Molecular docking study was implemented to interpret the variable inhibitory activity of the newly synthesized compounds against COX enzyme.The results suggested that some of these derivatives could be active COX inhibitors possessing a high preference for COX-2.


Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3210 ◽  
Author(s):  
Qosay A. Al-Balas ◽  
Mousa L. Al-Smadi ◽  
Mohammad A. Hassan ◽  
Ghazi A. Al Jabal ◽  
Ammar M. Almaaytah ◽  
...  

Glyoxalase-I (Glo-I) enzyme was established to be a valid target for anticancer drug design. It performs the essential detoxification step of harmful byproducts, especially methylglyoxal. A robust computer-aided drug design approach was used to design and validate a series of compounds with selenium or sulfur based heterorings. A series of in-house multi-armed 1,2,3-selenadiazole and 1,2,3-thiadiazole benzene derivatives were tested for their Glo-I inhibitory activity. Results showed that these compounds bind Glo-I active sites competitively with strong potential to inhibit this enzyme with IC50 values in micro-molar concentration. Docking poses revealed that these compounds interact with the zinc atom at the bottom of the active site, which plays an essential role in its viability.


2021 ◽  
Vol 33 (2) ◽  
pp. 423-438
Author(s):  
Rita M. Borik ◽  
Mohammed A. Hussein

In this work, a new derivative of ethyl 5-chloro-2-(3-(4-hydroxyphenyl)propanamido)benzoate (1) was synthesized by reacting the amino group of 3-(4-hydroxyphenyl)propanoic acid (0.01 mol) and methyl 2-amino-5-chlorobenzoate in presence of PCl3. Cyclcondensation of 1 with hydrazine hydrate afforded the corresponding 2-(4-hydroxyphenethyl)-3-amino-6-chloroquinazolin-4(3H)-one (2). Also, new Schiff base 3 was prepared via reaction of 2-(4-hydroxyphenethyl)-3-amino-6-chloroquinazolin- 4(3H)-one (2) with 4-hydroxy-3-methoxybenzaldehyde. The synthesized compounds were characterized by elemental analysis, IR, 1H NMR and mass spectral data. Also, the median lethal doses (LD50s) of compounds 1-3 in rats were 1125, 835 and 1785 mg/kg b.w., respectively. IC50 values of compounds (1, 3) as measured by DPPH• method was 136.47 and 73.54 μg/mL, respectively. IC50 values of compounds (1-3) as measured by ABTS•+ radical method was 0.8, 0.92 and 0.08 mg/mL, respectively. Antiulcerogenic activity at dose 1/20 LD50 in albino rats was 47.94, 24.60 and 56.45%, respectively. However, the anti-inflammatory effect at dose 1/20 LD50 of compounds (1-3) induced edema model after 120 min were 74.19, 69.93 and 59.03%, respectively. The synthesized compounds also possess hepatocytes and gastric mucosa protective activity against ibuprofen induced ulceration and LPS-induced liver toxicity, respectively in rats via normalization of oxidative stress biomarkers and inflammatory mediators (Na+/K+-ATPase, ALT, AST, LDH, TNF-α, NO, TBARS, GPx, CAT and SOD). Also, TNF-α, NO, PGE2 and COX-2 were inhibited in peritoneal macrophage cells at a concentration of 100 μg/L. Molecular docking suggested that the most active compounds 1 and 2 can be positioned within the active sites of COX-2 at Arg121 & Tyr356 similarly to ibuprofen (Arg-120, Glu-524 and Tyr-355). The compound 3–COX-2 complex generated by docking, revealed intricate interactions with a COX-2 channel, including hydrogen bonds with key residues Arg121 and phe519. These findings suggest that compounds 1-3 exhibited good antioxidant, antiulcer, anti-inflammatory activity and safe on liver enzymes in rats.


2019 ◽  
Author(s):  
Chem Int

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.


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