scholarly journals Evaluation of Various Biological Activities of Endemic Sideritis libanotica Extracts

2019 ◽  
Vol 11 (2) ◽  
pp. 210-217
Author(s):  
Mehmet ATAS ◽  
Nuraniye ERUYGUR ◽  
Fazli SOZMEN ◽  
Mustafa ERGUL ◽  
Merve ERGUL ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Biological Activities ◽  
Water Extract ◽  
In Vitro Cytotoxicity ◽  
Definitive Treatment ◽  
Inhibition Activity ◽  
Better Than

In recent years, using of plants to develop combine therapies for treatment of certain diseases such as cancer, Alzheimer's disease, and diabetes mellitus is extremely plausible approach. Perhaps, the definitive treatment of some of these diseases is hidden in the complex content of a plant in nature. Thus, in the present study, we decided to determine the biological activities of methanol and water extracts of the endemic Sideritis libanotica. To the best of our knowledge, the present study is the first investigation on antioxidant, enzyme inhibitory activity, antimicrobial activity, and in vitro cytotoxicity of S. libanotica. According to results, while the methanol extract shows better anti-cholinesterase, α-glucosidase, and α-amylase inhibition activity and cytotoxicity than the water extract, the tyrosinase inhibitory activity of the water extract was found to be better than the methanol extract. This study provides valuable information on how the biological activity of endemic S. libanotica changes in different solvent extractions such as water and methanol.

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Mannich Bases ◽  
In Vitro Cytotoxicity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

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 Phaseolus vulgaris L. var. Venanzio Grown in Tuscany: Chemical Composition and In Vitro Investigation of Potential Effects on Colorectal Cancer

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1181
Author(s):  
Federica Finetti ◽  
Marco Biagi ◽  
Jasmine Ercoli ◽  
Giulia Macrì ◽  
Elisabetta Miraldi ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Phaseolus Vulgaris ◽  
Unsaturated Fatty Acids ◽  
Biological Activities ◽  
Water Extract ◽  
Phaseolus Vulgaris L ◽  
Cellular Models ◽  
In Vitro Investigation ◽  
Promising Source

Phaseolus vulgaris L. (common bean) is a leguminous species that is an important dietary component due to its high content of proteins, unsaturated fatty acids, minerals, dietary fibers and vitamins. Due to the high content of polyphenols, several biological activities have been described for bean extracts, making it possible to include P. vulgaris among food with beneficial effects for human health. Moreover, more than 40,000 varieties of beans have been recognised with different nutraceutical properties, pointing out the importance of food biodiversity. In this work, we describe for the first time the chemical composition and biological activity of a newly recognized Italian variety of P. vulgaris grown in a restricted area of the Tuscany region and named “Fagiola di Venanzio”. Fagiola di Venanzio water extract is rich in proteins, sugars and polyphenols and displays antioxidant, anti-inflammatory and antiproliferative activities in in vitro assays on colon cancer cellular models. Our data indicate that this variety of P. vulgaris appears to be a promising source of bioactive compounds and encourage more in-depth studies to better elucidate the implications of its consumption for public health.

scholarly journals Machine Learning and In Vitro Chemical Screening of Potential α-Amylase and α-Glucosidase Inhibitors from Thai Indigenous Plants

Nutrients ◽  
2022 ◽  
Vol 14 (2) ◽  
pp. 267
Author(s):  
Tarapong Srisongkram ◽  
Sasisom Waithong ◽  
Thaweesak Thitimetharoch ◽  
Natthida Weerapreeyakul
Keyword(s):  
Diabetes Mellitus ◽  
Machine Learning ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Ethanolic Extract ◽  
Accuracy Score ◽  
Indigenous Plants ◽  
Predisposing Factor ◽  
Chemical Screening

Diabetes mellitus is a major predisposing factor for cardiovascular disease and mortality. α-Amylase and α-glucosidase enzymes are the rate-limiting steps for carbohydrate digestion. The inhibition of these two enzymes is clinically used for the treatment of diabetes mellitus. Here, in vitro study and machine learning models were employed for the chemical screening of inhibiting the activity of 31 plant samples on α-amylase and α-glucosidase enzymes. The results showed that the ethanolic twig extract of Pinus kesiya had the highest inhibitory activity against the α-amylase enzyme. The respective ethanolic extract of Croton oblongifolius stem, Parinari anamense twig, and Polyalthia evecta leaf showed high inhibitory activity against the α-glucosidase enzyme. The classification analysis revealed that the α-glucosidase inhibitory activity of Thai indigenous plants was more predictive based on phytochemical constituents, compared with the α-amylase inhibitory activity (1.00 versus 0.97 accuracy score). The correlation loading plot revealed that flavonoids and alkaloids contributed to the α-amylase inhibitory activity, while flavonoids, tannins, and reducing sugars contributed to the α-glucosidase inhibitory activity. In conclusion, the ethanolic extracts of P. kesiya, C. oblongifolius, P. anamense, and P. evecta have the potential for further chemical characterization and the development of anti-diabetic recipes.

scholarly journals Preliminary in vitro study of anti-oxidant activity and anti-diabetic potential of plant extracts from 4 herbal substances not traditionally used for treatment of diabetes mellitus

Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 755-762
Author(s):  
Dora Trifonova ◽  
Anna Gavrilova ◽  
Galina Dyakova ◽  
Genadi Gavrilov ◽  
Maya Yotova ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Biologically Active ◽  
Total Phenolic ◽  
Water Extracts ◽  
Sambucus Ebulus ◽  
Anti Oxidant ◽  
Treatment Of Diabetes

The focus of the presented study is the in vitro anti-oxidant activity and anti-diabetic potential of water extracts from the following four herbal substances, not traditionally used for treatment of diabetes mellitus – leaves of Sambucus ebulus L. and Prunus mahaleb L., and flowering stems of Cichorium intybus L. and Satureja kitaibelii Wierzb. ex Heuff. The water extracts are obtained through ultrasonication. The extract of S. kitaibelii stands out due to its highest values in all studied indicators – total phenolic content, scavenging potential (DPPH, ABTS) and α-glucosidase inhibitory activity which was six times higher than acarbose. The extract of C. intybus also showed significant α-glucosidase inhibitory activity compared to acarbose. The flowering stems of both species are promising sources of biologically active substances for blood sugar control in diabetes mellitus.

scholarly journals Phytochemical evaluation and in vitro antidiabetic efficiency of isopropanolic leaf extract of pimenta racemosa

2020 ◽  
Vol 7 (2) ◽  
pp. 50-55
Author(s):  
Anitha T A ◽  
Pakutharivu T ◽  
Nirubama K ◽  
Akshaya V
Keyword(s):  
Diabetes Mellitus ◽  
Glucose Uptake ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Yeast Cells ◽  
Antidiabetic Activity ◽  
Leaf Extracts ◽  
Pimenta Racemosa

The traditional herbal medicines are mainly obtained from plants are used in the management of Diabetes mellitus. The main objective of this work was to assess the presence of phytochemical compounds and to evaluate the in vitro antidiabetic activity of isopropanolic extracts of Pimenta racemosa leaves by studying their α-amylase inhibitory activity and glucose transport across yeast cells. Screening of phytochemicals showed positive results for alkaloids, steroids, cardiac glycosides, terpenoids, reducing sugars, anthraquinones, and results of in vitro α-amylase inhibitory studies demonstrated there was a dose-dependent increase in percentage inhibitory activity by the isopropanolic leaf extracts of Pimenta racemosa. At a concentration of 1 mg/ml, the extract showed a percentage inhibition 33.6 and for 5 mg/ml it was 91.2. The glucose uptake study was also studied through yeast cells by analyzing theamount of glucose remaining in the medium after a specific time intervals. It serves as an indicator for the capability of isopropanolic leaf extracts of Pimenta racemosa to transport the glucose into yeast cells. As a result, we found that the isopropanolic leaf extract of Pimenta racemosa have inhibitory activity against αamylase and also, which is efficient in glucose uptake. This therapeutic potentiality of Pimenta racemosa could be exploited in the treatment of Type 2 Diabetes mellitus. Further studies are also required to elucidate whether the plant have antidiabetic potential by in vivo for corroborating the traditional claim of the plant.

scholarly journals In vitro antioxidant and pancreatic α-amylase inhibitory activity of isolated fractions from water extract of Qingzhuan tea

2013 ◽  
Vol 52 (2) ◽  
pp. 928-935 ◽  
Author(s):  
Qian Cheng ◽  
Shengbao Cai ◽  
Dejiang Ni ◽  
Ruojun Wang ◽  
Feng Zhou ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Water Extract

scholarly journals DNA Topoisomerase I Inhibitory Activity of Quinochalcone C-glycosides from the Florets of Carthamus tinctorius

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Shi-Jun Yue ◽  
Wen-Xiao Wang ◽  
Cheng Qu ◽  
Lan-Ting Xin ◽  
Yu-Ping Tang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Dna Cleavage ◽  
Topoisomerase I ◽  
Docking Study ◽  
Carthamus Tinctorius ◽  
In Vitro Cytotoxicity ◽  
Molecular Docking Study ◽  
Dna Topoisomerase ◽  
Cleavage Complex

The DNA topoisomerase (Topo) I inhibitory activity of six quinochalcone C-glycosides (QCGs) isolated from the florets of Carthamus tinctorius were evaluated in vitro. Among them, anhydrosafflor yellow B (AHSYB, 4) and carthorquinoside B (6) could inhibit DNA Topo I at concentrations as low as 100 μM. Molecular docking study revealed that both of them have the capacity to stabilize Topo I-DNA cleavage complex in silico interacting with the essential binding sites, such as Arg364, Thr718 and TGP11. Besides, both compounds 4 and 6 exhibited no antitumor activity by in vitro cytotoxicity assays.

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