scholarly journals Preparation, COX-2 Inhibition and Anticancer Activity of Sclerotiorin Derivatives

Marine Drugs ◽  
2020 ◽  
Vol 19 (1) ◽  
pp. 12
Author(s):  
Tao Chen ◽  
Yun Huang ◽  
Junxian Hong ◽  
Xikang Wei ◽  
Fang Zeng ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Positive Control ◽  
Human Lung Cancer ◽  
Binding Modes ◽  
Ic50 Values ◽  
Cox 2 ◽  
Inhibitory Agents

The latest research has indicated that anti-tumor agents with COX-2 inhibitory activity may benefit their anti-tumor efficiency. A series of sclerotiorin derivatives have been synthesized and screened for their cytotoxic activity against human lung cancer cells A549, breast cancer cells MDA-MB-435 using the MTT method. Among them, compounds 3, 7, 12, 13, 15, 17 showed good cytotoxic activity with IC50 values of 6.39, 9.20, 9.76, 7.75, 9.08, and 8.18 μM, respectively. In addition, all compounds were tested in vitro the COX-2 inhibitory activity. The results disclosed compounds 7, 13, 25 and sclerotiorin showed moderate to good COX-2 inhibition with the inhibitory ratios of 58.7%, 51.1%, 66.1% and 56.1%, respectively. Notably, compound 3 displayed a comparable inhibition ratio (70.6%) to the positive control indomethacin (78.9%). Furthermore, molecular docking was used to rationalize the potential of the sclerotiorin derivatives as COX2 inhibitory agents by predicting their binding energy, binding modes and optimal orientation at the active site of the COX-2. Additionally, the structure-activity relationships (SARS) have been addressed.

scholarly journals Ingol and Ingenol-Type Diterpenes from Euphorbia trigona Miller with Keratinocyte Inhibitory Activity

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1206
Author(s):  
Reham Hammadi ◽  
Norbert Kúsz ◽  
Csilla Zsuzsanna Dávid ◽  
Zoltán Behány ◽  
László Papp ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
High Performance ◽  
Skin Condition ◽  
Positive Control ◽  
Active Species ◽  
The European Union ◽  
Ingenol Mebutate

Ingenol mebutate, isolated from Euphorbia peplus, is an ingenane-type diterpenoid, primarily used for the topical treatment of actinic keratosis, a premalignant skin condition. The aim of our work was to investigate other Euphorbia species to find structurally similar diterpenes that can be used as alternatives to ingenol mebutate. Pharmacological investigation of Euphorbia candelabrum, Euphorbia cotinifolia, Euphorbia ramipressa, and Euphorbia trigona revealed the potent keratinocyte (HPV-Ker cell line) inhibitory activity of these spurge species. From the methanolic extract of the aerial parts of Euphorbia trigona Miller, the most active species, five ingol (1–5) and four ingenane-type diterpenoids (6–9) were isolated by various chromatographic separation techniques, including open column chromatography, vacuum liquid chromatography, thin-layer chromatography, and high-performance liquid chromatography. The structures of the compounds were determined by NMR spectroscopic analysis and by comparison of the assignations with the literature data. The cytotoxic activity of the compounds against keratinocytes was tested in vitro by using ingenol mebutate as a positive control. Among the isolated compounds, two ingenane derivatives (6 and 7) exhibited remarkably stronger cytotoxic activity (IC50 values 0.39 μM and 0.32 μM, respectively) on keratinocytes than ingenol mebutate (IC50 value 0.84 μM). These compounds could serve as starting materials for further investigations to find alternatives to Picato® (with active substance ingenol mebutate), which was withdrawn from marketing authorization in the European Union.

scholarly journals Two new compounds from leaves of Bruguiera cylindrica (L.) Blume with the in vitro α-glucosidase inhibitory activity

2021 ◽  
Vol 23 (4) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Tung Thanh Bui ◽  
Phung Kim Phi Nguyen ◽  
Chi Minh Tran ◽  
Tu Dang Cam Phan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Ethyl Acetate Extract ◽  
Chemical Constituents ◽  
Positive Control ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Bruguiera Cylindrica ◽  
New Compounds ◽  
Better Than

Introduction: Bruguiera cylindrica is one of the mangrove plants belonging to Bruguiera genus. This genus is characterized by the presence of a large number of compounds, but the research on bioactivities has not been investigated so far. In the present research, the α-glucosidase inhibitory activity, as well as chemical constituents of the ethyl acetate extract of this plant, were studied. Methods: The chemical structures of two new compounds were elucidated by spectroscopic and computational methods. Results: Two new compounds, benzobrugierol (1) and bruguierine (2), were isolated from leaves of Bruguiera cylindrica (L.) Blume, together with nine known ones, including lupeol (3), betulin (4), chrysoeriol (5), glut-5-ene-3-ol (6), cholesta-4-ene-3-one (7), 3α-(Z)-coumaroyllupeol (8), 3α-(E)-coumaroyllupeol (9), 3β-hydroxycholesta-5-ene-7-one (10) and β-sitosterol 3-O-β-D-glucopyranoside (11). Extracts and some isolated compounds were evaluated for α-glucosidase inhibitory activities. Conclusion: The results showed that most of the extracts and tested compounds exhibited activities better than the positive control acarbose, especially two new compounds 1 and 2 with their IC50 values of 17.9 ± 0.4 and 34.6 ± 0.7 (mg/mL), respectively.

scholarly journals SYNTHESIS, CHARACTERIZATION AND CYTOTOXIC ACTIVITY OF Pt(II)COMPLEX OF CAMPHOR 4-METHYL THIOSEMICARBAZONE

2018 ◽  
Vol 56 (2A) ◽  
pp. 75-80
Author(s):  
Phan Thi Hong Tuyet
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
1H Nmr ◽  
Biomedical Application ◽  
Molecular Formula ◽  
Hep G2 ◽  
Anti Cancer ◽  
Ic50 Values ◽  
Cancer Activity

The new complex of Pt(II) with camphor 4-methyl thiosemicarbazone was synthesized and characterized by means of MS, 1H-NMR and IR spectroscopes. Results show that, the molecular formula of new Pt(II) complex is [Pt(C12H20N3S))2]. The Pt(II) complex is of four coordinate. The result of in vitro anti-cancer activity of the complex has shown that the complex of Pt(II) with camphor 4-methyl thiosemicarbazone exhibit inhibitor on Hep-G2 and RD cancer cells with IC50 values of 7.74 and 7.61 µg.mL-1. These results indicated a potential of new Pt(II)complex in biomedical application.

scholarly journals Methoxy-Substituted Tyramine Derivatives Synthesis, Computational Studies and Tyrosinase Inhibitory Kinetics

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2477
Author(s):  
Yasir Nazir ◽  
Hummera Rafique ◽  
Naghmana Kausar ◽  
Qamar Abbas ◽  
Zaman Ashraf ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Competitive Inhibition ◽  
Kojic Acid ◽  
Positive Control ◽  
Potential Candidate ◽  
Binding Modes ◽  
Mushroom Tyrosinase ◽  
In Silico Docking ◽  
Human Tyrosinase

Targeting tyrosinase for melanogenesis disorders is an established strategy. Hydroxyl-substituted benzoic and cinnamic acid scaffolds were incorporated into new chemotypes that displayed in vitro inhibitory effects against mushroom and human tyrosinase for the purpose of identifying anti-melanogenic ingredients. The most active compound 2-((4-methoxyphenethyl)amino)-2-oxoethyl (E)-3-(2,4-dihydroxyphenyl) acrylate (Ph9), inhibited mushroom tyrosinase with an IC50 of 0.059 nM, while 2-((4-methoxyphenethyl)amino)-2-oxoethyl cinnamate (Ph6) had an IC50 of 2.1 nM compared to the positive control, kojic acid IC50 16700 nM. Results of human tyrosinase inhibitory activity in A375 human melanoma cells showed that compound (Ph9) and Ph6 exhibited 94.6% and 92.2% inhibitory activity respectively while the positive control kojic acid showed 72.9% inhibition. Enzyme kinetics reflected a mixed type of inhibition for inhibitor Ph9 (Ki 0.093 nM) and non-competitive inhibition for Ph6 (Ki 2.3 nM) revealed from Lineweaver–Burk plots. In silico docking studies with mushroom tyrosinase (PDB ID:2Y9X) predicted possible binding modes in the catalytic site for these active compounds. Ph9 displayed no PAINS (pan-assay interference compounds) alerts. Our results showed that compound Ph9 is a potential candidate for further development of tyrosinase inhibitors.

scholarly journals HYPOGLYCEMIC ACTIVITY OF FRUITING BODY EXTRACTS FROM Pycnoporus sanguineus (L.: Fr.) Murr. MUSHROOM

2018 ◽  
Vol 40 (3) ◽  
Author(s):  
Tran Duc Tuong ◽  
Duong Xuan Chu ◽  
Bui Thi Minh Dieu
Keyword(s):  
Fruiting Body ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Positive Control ◽  
Hypoglycemic Activity ◽  
Alpha Amylase ◽  
Moderate Activity ◽  
Pycnoporus Sanguineus ◽  
Ic50 Values

ABSTRACT Alpha-amylase and α-glucosidase are two main enzymes involved in carbohydrate metabolism. Inhibition of α-amylase and α-glucosidase can be said as an effective treatment for delaying the absorption of glucose after meals in people with diabetes mellitus. The objective of the present study is to provide an in vitro evidence for the potential hypoglycemic activity via inhibitory activity of the ethanolic and aqueous extracts from fruiting bodies of Pycnoporus sanguineus mushroom on α-amylase and α-glucosidase enzymes. Alpha-amylase and α-glucosidase inhibitory activities of aqueous and ethanolic extracts of P. sanguineus fruiting body were examined in a dose-response manner. Acarbose was used as a positive control. The results showed that the ethanolic extract of P. sanguineus possessed strong inhibitory activity on α-amylase and α-glucosidase with IC50 values of 97.08 and 92.60 μg/mL, respectively. The aqueous extract also exhibited moderate activity against α-amylase and α-glucosidase with IC50 values of 150.15 and 102.29 μg/mL, respectively. Which was significantly lower than that of acarbose with IC50 values of 85.12 and 68.36 μg/mL, respectively. The degree of α-amylase and α-glucosidase inhibition was correlated with the dose of inhibitors. From these results Pycnoporus sanguineus (Trametes sanguinea) possesses high potential in lowering blood glucose level, reduced insulin resistance and the risk of diabetic-related complications.

Extracts from Viscum and Crataegus are Cytotoxic against Larynx Cancer Cells

1997 ◽  
Vol 52 (1-2) ◽  
pp. 42-44 ◽  
Author(s):  
M. T. Sáenz ◽  
M. C. Ahumada ◽  
M. D. García
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Positive Control ◽  
Complete Inhibition ◽  
Vitro Activity ◽  
Larynx Cancer ◽  
In Vitro Activity ◽  
Similar Activity ◽  
Crataegus Monogyna

Abstract The effects of hexanoic extracts of Viscum cruciatum Sieber parasitic on Crataegus mono­gyna Jacq. (I), Crataegus monogyna Jacq. parasitized with Viscum cruciatum Sieber (II), and Crataegus monogyna Jacq. non-parasitized (III), and of a triterpenes enriched fractions isolated from I, II and III (CFI, CFII, CFIII respectively), on the growth of HEp-2 cells have been evaluated. All the samples demonstrated significant cytotoxic activity against cultured HEp-2 cells, and all of them showed a stronger in vitro activity than 6-mercaptopurine solution used as a positive control. With the hexanoic extracts I, II and III almost similar activity was obtained, but the hexanoic extract I showed comparably better results. Almost complete inhibition was observed with triterpenes-enriched fractions CFI, CFII and CFIII, at the dose 6 μg/ml, after 72 h of treatment. The most intense response was obtained with the triterpenesenriched fraction CFIII (from Crataegus monogyna non-parasitized), where the inhibition was 93%, but the fraction CFI and CFII showed similar inhibition (92% and 83%).

scholarly journals In vitro α-glucosidase inhibitory activity of compounds isolated from mangrove Lumnitzera littorea leaves

2019 ◽  
Vol 22 (1) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Thuy Thi Pham ◽  
Poul Erik Hansen ◽  
Phung Kim Phi Nguyen
Keyword(s):  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Mangrove Forest ◽  
2D Nmr ◽  
Positive Control ◽  
Spectroscopic Methods ◽  
Corosolic Acid ◽  
Ic50 Values ◽  
Alpha Glucosidase

Introduction: Lumnitzera littorea grown at CanGio Mangrove Forest has been investigated. The present study reports the isolation, characterization and evaluation of the alpha-glucosidase inhibitory activity of isolated compounds from Lumnitzera littorea leaves. Methods: Their structures were elucidated by spectroscopic methods (including MS, 1D and 2D–NMR) and comparison with values from the literature. From the n-hexane extract, nine compounds including lupeol (1), betulin (2), betulinic acid (3), oleanolic acid (4), corosolic acid (5), -sitosterol (6), beta-sitosterol 3-O- beta-D-glucopyranoside (7), stigmast-5-ene-3beta-O-(6-O-hexadecanoyl-beta-D-glucopyranoside) (8), and stigmast-4-ene-3-one (9) were isolated and identified. Results: The results of the alpha-glucosidase inhibitory activity showed thatcorosolic acid (5) and oleanolic acid (4) were the most potent, with IC50 values of 17.86 +/- 0.42 and 18.82 +/- 0.59 ug/mL, respectively. Five of the other seven compounds exhibited inhibitory activity with IC50 values below 100 ug/mL, and higher than the positive control acarbose (127.64 +/- 0.64 ug/mL).  

Inhibitory effects of bioaccessible anthocyanins and procyanidins from apple, red grape, cinnamon on α-amylase, α-glucosidase and lipase

2020 ◽  
pp. 1-9
Author(s):  
Pınar Ercan ◽  
Sedef Nehir El
Keyword(s):  
Inhibitory Activity ◽  
Digestive Enzymes ◽  
Positive Control ◽  
Anthocyanin Content ◽  
Inhibitory Effects ◽  
Total Anthocyanin ◽  
Total Anthocyanin Content ◽  
Before And After ◽  
Red Grape

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.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

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