scholarly journals Tyrosinase Inhibitory Effect, Antioxidant and Anticancer Activities of Bioactive Compounds in Ripe Hog Plum (Spondias Pinnata) Fruit Extracts

2019 ◽  
Vol 35 (3) ◽  
pp. 916-926
Author(s):  
Supawadee Patathananone ◽  
Jureerut Daduang ◽  
Amonrat Koraneekij ◽  
Chia-Ying Li
Keyword(s):  
High Performance ◽  
Antioxidant Property ◽  
Inhibitory Effect ◽  
Tyrosinase Activity ◽  
Normal Fibroblast ◽  
Anticancer Activities ◽  
Ic50 Value ◽  
Bioactive Agents ◽  
Hog Plum

The usage of ripe hog plum fruit (Spondias pinnata) extracts in cosmetics and food products, including cancer therapeutic agents, have a few studies. Herein, the strong anti-tyrosinase activity found in the extracted part of isopropanol is reported. This extract was separated by liquid/liquid extraction using hexane: methanol+H2O. The hydrophilic layer (6A*) exhibited the anti-tyrosinase, antioxidant, and anticancer activities in vitro. The IC50 value of each bioactivity was presented as approximately 0.18, 0.04, and 1.40 mg/ml, respectively. In addition, 6A* fraction showed a very low cytotoxic effect in normal fibroblast cells (NHDF cells). The bioactive agents in 6A* were purified by C18 reverse-phase High-Performance Liquid Column Chromatography (HPLC). The 12 purified peaks were shown in the chromatogram profile. All peaks (excepted 6A-06 and 6A-09) displayed anti-tyrosinase activity, whereas the antioxidant property was not found in 6A-01, 6A-06, and 6A-08 but was represented in other peaks. Most purified peaks were indicated to be the aromatic alcohol or derivative phenol compounds.

Matrix metalloproteinase-2 inhibition activity of Plukenetia volubilis L. leaves extract for anti-aging application

Food Research ◽  
2021 ◽  
Vol 5 (4) ◽  
pp. 120-126
Author(s):  
N. Wuttisin ◽  
T. Nararatwanchai ◽  
A. Sarikaphuti
Keyword(s):  
High Performance ◽  
Antioxidant Property ◽  
In Vitro Cytotoxicity ◽  
Hot Water ◽  
Matrix Metalloproteinase 2 ◽  
Human Skin Fibroblast ◽  
Inhibition Activity ◽  
Hot Air ◽  
Plukenetia Volubilis

Plukenetia volubilis L. leaves were part of the traditional diets in many countries. P. volubilis leaves were used to make tea and sold as local products in Thailand. There is less information on the composition of P. volubilis leaves. Previous study revealed that roasted leaves extract with hot water showed the highest antioxidant activity and the antioxidant property might be due to the presence of flavonoid. The present study was carried out to determine the quercetin content in P. volubilis leaves extract and evaluate the anti-aging potential activities including MMP-2 inhibition activity and telomerase stimulation activity. P. volubilis leaves were roasted in hot air oven and extracted with hot water. The extract was investigated for quercetin content by high-performance liquid chromatography (HPLC). In vitro cytotoxicity, MMP-2 inhibition activity and telomerase stimulation activity were determined for anti-aging properties. The results revealed that P. volubilis leaves contained quercetin 50.50±4.78 mg/g DW. The extract showed no cytotoxicity on human skin fibroblast with cell viability of 96.76-120.83%. It demonstrated the potential of MMP-2 inhibition (8.74±2.84%) activity but lower than ascorbic acid. P. volubilis leave extract did not have telomerase stimulation activity on the human Hela cell line. However, the results from this study have indicated the possibility of anti-aging potential of P. volubilis leaves extract.

scholarly journals Potential Effect of Pomegranate Peels Extract (Punica Granatum.) against Covid-19 Virus .

2021 ◽  
Author(s):  
Ashraf fawzy mosa ◽  
Mostafa abo Elhoda Mohamed
Keyword(s):  
Tissue Culture ◽  
Water Extract ◽  
Punica Granatum ◽  
Inhibitory Effect ◽  
Potential Effect ◽  
Laboratory Methods ◽  
Global Epidemic ◽  
Ic50 Value ◽  
The World

Abstract Background: Covid-19 Virus infection poses significant global health challenges and considered a global epidemic sweeping all countries of the world Which prompted scientists around the world to search for a quick or safe treatment to preserve people's lives .So far, options for controlling and treating the disease have not been revealed. The current study was conducted to evaluate the effectiveness of pomegranate peels extract against the Covid-19 virus in the laboratory. Methods: In this research, tow methods of extraction are carried out ethyl alcohol and distal water extract of pomegranate peels . activity of the extract assessed using 50% Tissue Culture Infectious Doses (TCID50) method in Vero E6 cells. Results: Pomegranate peels extract had the highest inhibitory effect against Covid -19 virus with IC50 value of 0.125, 0.0625 and 0.031256 μl in Vero E6 cells. Conclusion: Based on our results, the aqueous extract of pomegranate peels can inhibit Covid-19 virus replication in vitro.

In vitro inhibitory effects of glucosamine, chondroitin and diacerein on human hepatic CYP2D6

2021 ◽  
Vol 36 (4) ◽  
pp. 259-270
Author(s):  
Boon Hooi Tan ◽  
Nafees Ahemad ◽  
Yan Pan ◽  
Uma Devi Palanisamy ◽  
Iekhsan Othman ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
High Performance ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Time Curve ◽  
Clinical Drugs ◽  
Inhibition Potencies ◽  
P450 2D6

Abstract Objectives Glucosamine, chondroitin and diacerein are natural compounds commonly used in treating osteoarthritis. Their concomitant intake may trigger drug–natural product interactions. Cytochrome P450 (CYP) has been implicated in such interactions. Cytochrome P450 2D6 (CYP2D6) is a major hepatic CYP involved in metabolism of 25% of the clinical drugs. This study aimed to investigate the inhibitory effect of these antiarthritic compounds on CYP2D6. Methods CYP2D6 was heterologously expressed in Escherichia coli. CYP2D6–antiarthritic compound interactions were studied using in vitro enzyme kinetics assay and molecular docking. Results The high-performance liquid chromatography (HPLC)-based dextromethorphan O-demethylase assay was established as CYP2D6 marker. All glucosamines and chondroitins weakly inhibited CYP2D6 (IC50 values >300 µM). Diacerein exhibited moderate inhibition with IC50 and K i values of 34.99 and 38.27 µM, respectively. Its major metabolite, rhein displayed stronger inhibition potencies (IC50=26.22 μM and K i =32.27 μM). Both compounds exhibited mixed-mode of inhibition. In silico molecular dockings further supported data from the in vitro study. From in vitro–in vivo extrapolation, rhein presented an area under the plasma concentration-time curve (AUC) ratio of 1.5, indicating low potential to cause in vivo inhibition. Conclusions Glucosamine, chondroitin and diacerein unlikely cause clinical interaction with the drug substrates of CYP2D6. Rhein, exhibits only low potential to cause in vivo inhibition.

scholarly journals Inhibitory effect of the glucosinolate–myrosinase system on Phytophthora cinnamomi and Pythium spiculum

2019 ◽  
Vol 55 (No. 2) ◽  
pp. 93-101 ◽  
Author(s):  
Francisco Teodoro Arroyo Cordero ◽  
Rocío Rodríguez-Arcos ◽  
Ana Jiménez-Araujo ◽  
Rafael Guillén-Bejarano ◽  
María José Basallote ◽  
...  
Keyword(s):  
Mycelial Growth ◽  
High Performance ◽  
Phytophthora Cinnamomi ◽  
Inhibitory Effect ◽  
Reversed Phase ◽  
Field Application ◽  
Additional Information ◽  
Array Detection ◽  
Important Additional Information

Glucosinolate extracts from sprouts of common Brassica nigra, B. juncea cv. Scala, B. carinata cv. Eleven, and Sinapis alba cv. Ludique were analysed by reversed phase high-performance liquid chromatography-diode array detection-mass spectrometry. The effect of the glucosinolate–myrosinase system on in vitro mycelial growth of Phytophthora cinnamomi Rands and Pythium spiculum B. Paul was assessed. Likewise, sinigrin and sinalbin monohydrate commercial standards were also tested. The extracts from B. carinata, which contained 159 mmol/g plant DW equivalent (85% sinigrin, 5% gluconapin, and 3% glucotropaeolin), were the most effective against Phytophthora and Pythium isolates used in this study. However, the extract from S. alba, which contained 1 180 mmol/g (100% sinalbin), did not inhibit the mycelial growth of the isolates tested. The use of the glucosinolate-myrosinase system provides important additional information to advance in the implementation of field application of brassicaceous amendments for the control of soil-borne pathogens.

scholarly journals Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 437
Author(s):  
Shu-Qin Qin ◽  
Lian-Chun Li ◽  
Jing-Ru Song ◽  
Hai-Yun Li ◽  
Dian-Peng Li
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
A549 Cells ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Diphenyl Tetrazolium Bromide ◽  
Conjugated Compounds

A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.

scholarly journals Validation of an HPLC Method for the Simultaneous Quantification of Metabolic Reaction Products Catalysed by CYP2C11 Enzymes in Rat Liver Microsomes: In Vitro Inhibitory Effect of Salicylic Acid on CYP2C11 Enzyme

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4294 ◽  
Author(s):  
Salhab ◽  
Naughton ◽  
Barker
Keyword(s):  
High Performance Liquid Chromatography ◽  
Enzyme Activity ◽  
Salicylic Acid ◽  
Liquid Chromatography ◽  
Rat Liver ◽  
High Performance ◽  
Inhibitory Effect ◽  
Metabolic Reaction ◽  
Rat Liver Microsomes

The inhibitory effect of new chemical entities on rat liver P450 marker activities was investigated in a functional approach towards drug development. Treatment of colorectal cancer (CRC) and chemoprevention using salicylic acid has gained a lot of attention, mainly in the prevention of the onset of colon cancer. Thus, an in vitro inhibitory effect of salicylic acid on rat CYP2C11 activity was examined by using high performance liquid chromatography (HPLC). High performance liquid chromatography analysis of a CYP2C11 assay was developed on a reversed phase C18 column (SUPELCO 25 cm × 4.6 mm × 5 µm) at 243 nm using 32% phosphate buffer (pH 3.36) and 68% methanol as a mobile phase. The CYP2C11 assay showed good linearity for all components (R2 > 0.999). Substrates and metabolites were found to be stable for up to 72 hours. Additionally, the method demonstrated good reproducibility, intra- and inter-day precision (<15%), acceptable recovery and accuracy (80%–120%), and low detection (1.3501 µM and 3.2757 µM) and quantitation limit values (4.914 µM and 9.927 µM) for 16α-hydroxytestosterone and testosterone, respectively. Salicylic acid acts reversibly as a noncompetitive (weak) inhibitor with Ki = 84.582 ± 2.67 µM (concentration of inhibitor to cause 50% inhibition of original enzyme activity (IC50) = 82.70 ± 2.67 µM) for CYP2C11 enzyme activity. This indicates a low potential to cause toxicity and drug–drug interactions.

scholarly journals Chenopodium album L. and Sisymbrium officinale (L.) Scop.: Phytochemical Content and In Vitro Antioxidant and Anti-Inflammatory Potential

Plants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 505
Author(s):  
Valentina Amodeo ◽  
Mariangela Marrelli ◽  
Veronica Pontieri ◽  
Roberta Cassano ◽  
Sonia Trombino ◽  
...  
Keyword(s):  
High Performance ◽  
Chenopodium Album ◽  
Antioxidant Properties ◽  
New Drugs ◽  
Herbal Remedies ◽  
Raw 264.7 Cells ◽  
Phytochemical Content ◽  
Ic50 Value ◽  
Anti Inflammatory

Spontaneous edible plants have an old history of use in popular traditions all around the world, and the rediscovery of these species could also be useful for the search of new drugs. Chenopodium album L. (Amaranthaceae) and Sisymbrium officinale (L.) Scop. (Brassicaceae) are two annual plants traditionally used both as food and herbal remedies against inflammatory disorders. In this work, the potential anti-inflammatory and anti-arthritic activities of these plant species have been investigated, together with their antioxidant potential. The phytochemical composition was assessed as well by means of gas chromatography coupled to mass spectrometry (GC-MS) and high performance thin layer chromatography (HPTLC). The antioxidant properties were assessed using the DPPH and β-carotene bleaching test. The ability of extracts to protect against lipid peroxidation was also examined in rat-liver microsomal membranes. All the samples showed a preservation of antioxidant activity up to 60 min. A significant inhibitory activity on the production of the pro-inflammatory mediator nitric oxide was induced in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by the dichloromethane fraction of C. album extract, with an IC50 value equal to 81.7 ± 0.9 μg/mL. The same sample showed also a concentration-dependent anti-denaturation effect on heat-treated bovine serum albumin (IC50 = 975.6 ± 5.5 μg/mL), even if the best in vitro anti-arthritic activity was observed for the dichloromethane fraction of S. officinale extract, with an IC50 value of 680.9 ± 13.2 μg/mL.

scholarly journals Screening and Application of Chitin Synthase Inhibitors

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1029
Author(s):  
Xiaozai Shi ◽  
Shuo Qiu ◽  
Yingling Bao ◽  
Hanchi Chen ◽  
Yuele Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Chitin Synthase ◽  
Fungal Cell ◽  
Ic50 Value ◽  
Further Development ◽  
Fungicide Target ◽  
Better Than

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

scholarly journals α-Glucosidase Inhibitory, Anti-Oxidant, and Anti-Hyperglycemic Effects of Euphorbia nivulia–Ham. in STZ-Induced Diabetic Rats

Dose-Response ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 155932582093942
Author(s):  
Muhammad Younus ◽  
Muhammad Mohtasheem ul Hasan ◽  
Khalil Ahmad ◽  
Ali Sharif ◽  
Hafiz Muhammad Asif ◽  
...  
Keyword(s):  
High Performance ◽  
Wistar Rat ◽  
Inhibitory Effect ◽  
Diabetic Rats ◽  
In Vivo Studies ◽  
Control Group ◽  
Control Drug ◽  
Antidiabetic Effects

In this study, we aimed to investigate the antidiabetic effects of Euphorbia nivulia (En), native to Cholistan Desert area of Bahawalpur, Pakistan. First, we performed high-performance liquid chromatography analysis and found that this plant contains ferulic acid, gallic acid, quercetin, benzoic acid, polyphenols, and flavonoids. Then, we performed in vitro and in vivo studies to assess its effects on diabetic Wistar rat model. The experiments were performed and compared with control drug glibenclamide. The 70% hydroalcoholic extract of En exhibited 97.8% in vitro α-glucosidase inhibitory effect at a dose of 1.0 mg/mL. We orally administered the extract of En and control drug to the streptozotocin (STZ)-induced diabetic rats and analyzed its antidiabetic effects. We found that the extract of En with a dose of 500 mg/kg/body weight exhibited significant effect to reduce blood glucose in STZ-induced rats as compared with the control group ( P < .001). Our histological data also showed that the extract significantly improved the histopathology of pancreas. Collectively, both in vitro and in vivo studies revealed that En possesses α-glucosidase inhibitory, antioxidant, and anti-hyperglycemic effect in STZ-induced diabetic rats.

scholarly journals Optimization of Flavonoid Extraction in Dendrobium officinale Leaves and Their Inhibitory Effects on Tyrosinase Activity

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Haixia Lu ◽  
Ke Yang ◽  
Lianghui Zhan ◽  
Tingting Lu ◽  
Xue Chen ◽  
...  
Keyword(s):  
Ethanol Concentration ◽  
Inhibitory Effect ◽  
Tyrosinase Activity ◽  
Dendrobium Officinale ◽  
Key Factors ◽  
Extraction Technology ◽  
Steepest Ascent ◽  
Burman Design ◽  
Solid Liquid

In order to establish the extraction technology of flavonoids from Dendrobium officinale leaves, a method combining Plackett–Burman design (PBD), steepest ascent design, and central composite design was developed to optimize the extraction of flavonoids. In addition, the tyrosinase activity inhibition of flavonoids was further tested in vitro. PBD results showed that ethanol concentration and number of extractions were key factors. Response surface methodology (RSM) indicated that the optimal extraction conditions were 78% ethanol concentration, six extraction times, 2 h, and 1:50 solid-liquid ratio. Under these conditions, the total flavonoid content could reach 35 mg/50 mL. In vitro tyrosinase experiment, the extracted total flavonoids had better inhibitory effect on tyrosinase activity than β-arbutin, and its inhibition rate for monophenolase and diphenolase exceeded 100% and 70%, respectively. These results indicate that RSM can effectively improve the extraction of flavonoids from Dendrobium officinale leaves and the flavonoids have the prospect of being applied to foods and cosmetics.

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