scholarly journals Optimization of Triterpene Saponins Mixture with Antiproliferative Activity

2019 ◽  
Vol 9 (23) ◽  
pp. 5160
Author(s):  
Rodica Tatia ◽  
Christina Zalaru ◽  
Oana Craciunescu ◽  
Lucia Moldovan ◽  
Anca Oancea ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Antiproliferative Activity ◽  
In Vitro Tests ◽  
Antitumor Effects ◽  
Hedera Helix ◽  
Mtt Method ◽  
Tumor Cell Culture ◽  
Specialized Form

In this study, three of the saponins present in leaves of Hedera helix L., α-hederin, hederagenin, and hederacoside C were studied for their antiproliferative activity. The three saponins were analyzed in different concentrations by in vitro tests on normal fibroblasts cells and cervix ephitelial tumor cells. Determination of cytotoxicity and antitumor effects was performed using the MTT method. From the tested saponins, α-hederin was biocompatible in normal fibroblasts cells at concentrations between 2–10 μg/mL. Its antiproliferative activity was exerted in the concentration range of 10–400 μg/mL in cervix ephitelial tumor cells. Similarly, hederagenin presented antiproliferative activity at concentrations between 25–400 μg/mL. In turn, hederacoside C was shown to be noncytotoxic in normal fibroblasts and cervix ephitelial tumor cell culture at all the tested concentrations. The obtained experimental results were analyzed by “Mixture design”, a specialized form of the response surface method (RSM) provided by the Design Expert 11 software, and the optimal composition of obtained saponins mixture was selected and verified in vitro for antiproliferative activity. The results showed that an optimal saponins mixture has the potential to be used in pharmacological applications.

scholarly journals Synthesis and Evaluation of the Antitumor Activity of Novel 1-(4-Substituted phenyl)-2-ethyl Imidazole Apoptosis Inducers In Vitro

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4293
Author(s):  
Zhen-Wang Li ◽  
Chun-Yan Zhong ◽  
Xiao-Ran Wang ◽  
Shi-Nian Li ◽  
Chun-Yuan Pan ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Cells ◽  
Antiproliferative Activity ◽  
Antitumor Agent ◽  
Positive Control ◽  
Selectivity Index ◽  
Time Dependent ◽  
Potential Candidate ◽  
Dependent Manner

Novel imidazole derivatives were designed, prepared, and evaluated in vitro for antitumor activity. The majority of the tested derivatives showed improved antiproliferative activity compared to the positive control drugs 5-FU and MTX. Among them, compound 4f exhibited outstanding antiproliferative activity against three cancer cell lines and was considerably more potent than both 5-FU and MTX. In particular, the selectivity index indicated that the tolerance of normal L-02 cells to 4f was 23–46-fold higher than that of tumor cells. This selectivity was significantly higher than that exhibited by the positive control drugs. Furthermore, compound 4f induced cell apoptosis by increasing the protein expression levels of Bax and decreasing those of Bcl-2 in a time-dependent manner. Therefore, 4f could be a potential candidate for the development of a novel antitumor agent.

scholarly journals Antitumor Potential of Lippia citriodora Essential Oil in Breast Tumor-Bearing Mice

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 875
Author(s):  
Katerina Spyridopoulou ◽  
Tamara Aravidou ◽  
Evangeli Lampri ◽  
Eleni Effraimidou ◽  
Aglaia Pappa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antiproliferative Activity ◽  
Folk Medicine ◽  
Tumor Model ◽  
Flowering Plant ◽  
Antitumor Effects ◽  
Lippia Citriodora ◽  
Antitumor Potential ◽  
Apoptotic Marker

Lippia citriodora is a flowering plant cultivated for its lemon-scented leaves and used in folk medicine for the preparation of tea for the alleviation of symptoms of gastrointestinal disorders, cold, and asthma. The oil extracted from the plant leaves was shown to possess antioxidant potential and to exert antiproliferative activity against breast cancer. The aim of this study was to further investigate potential antitumor effects of L. citriodora oil (LCO) on breast cancer. The in vitro antiproliferative activity of LCO was examined against murine DA3 breast cancer cells by the sulforhodamine B assay. We further explored the LCO’s pro-apoptotic potential with the Annexin-PI method. The LCO’s anti-migratory effect was assessed by the wound-healing assay. LCO was found to inhibit the growth of DA3 cells in vitro, attenuate their migration, and induce apoptosis. Finally, oral administration of LCO for 14 days in mice inhibited by 55% the size of developing tumors in the DA3 murine tumor model. Noteworthy, in the tumor tissue of LCO-treated mice the apoptotic marker cleaved caspase-3 was elevated, while a reduced protein expression of survivin was observed. These results indicate that LCO, as a source of bioactive compounds, has a very interesting nutraceutical potential.

Ajugalide-B (ATMA) is an anoikis-inducing agent from Ajuga taiwanensis with antiproliferative activity against tumor cells in vitro

2012 ◽  
Vol 80 ◽  
pp. 64-69 ◽  
Author(s):  
Chun-Tang Chiou ◽  
Yao-Haur Kuo ◽  
Yu-Yi Chan ◽  
Shin-Hun Juang ◽  
Hsiu-Hui Chan ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Antiproliferative Activity

scholarly journals Comparative Characteristics of Determination of Antioxidant Activity of Sea Buckthorn Fruits by Various Methods

2019 ◽  
Vol 8 (4) ◽  
pp. 48-52
Author(s):  
O. V. Trineeva
Keyword(s):  
Antioxidant Activity ◽  
Medicinal Plant ◽  
Plant Material ◽  
Natural Antioxidants ◽  
Sea Buckthorn ◽  
In Vitro Tests ◽  
Medicinal Plant Material

Introduction. Recently, much attention has been paid to the primary assessment of the pharmacological effect of various drugs using in vivo and in vitro tests. It is known that such a medicinal plant as sea buckthorn, in its phytochemical composition is rich in natural antioxidants: carotenoids, tocopherols, flavonoids, ascorbic acid, etc. In some publications there is information about the antioxidant activity of sea buckthorn and fatty oil based on them. However, information on the comparative characteristics of the use of various methods for determining the antioxidant activity of this type of medicinal plant material and the results obtained are not found in the scientific literature.Aim. The aim of this work was a comparative determination of the antioxidant activity of medicinal plant material of buckthorn fruits of various species of buckthorn.Materials and methods. The total antioxidant activity of water and water-alcohol extracts from the fruits of sea buckthorn fruits was determined using various techniques recommended in the literature. The antioxidant activity of the extracts was determined by permanganometric titration, in vitro inhibition of adrenaline autooxidation, and also in a biological model, Parametium caudatum cell culture.Results and discussion. The effect of the extractant polarity on the value of antioxidant activity was studied. It was found that the highest content of antioxidants in the extraction is observed when using 96 % ethanol as an extractant.Conclusion. Using three methods, the prospects of using sea buckthorn fruits and preparations based on them as a source of antioxidants are shown. 

scholarly journals Hydroxychloroquine Synergizes With The PI3K Inhibitor BKM120 to Exhibit Antitumor Efficacy Independent of Autophagy

2021 ◽  
Author(s):  
Xin Peng ◽  
Shaolu Zhang ◽  
Wenhui Jiao ◽  
Zhenxing Zhong ◽  
Yuqi Yang ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Cell Biology ◽  
Molecular Mechanisms ◽  
Critical Role ◽  
Single Agent ◽  
Antitumor Efficacy ◽  
Antitumor Effects ◽  
Autophagy Inhibitor

Abstract Background: The critical role of phosphoinositide 3-kinase (PI3K) activation in tumor cell biology has prompted massive efforts to develop PI3K inhibitors (PI3Kis) for cancer therapy. However, recent results from clinical trials have shown only a modest therapeutic efficacy of single-agent PI3Kis in solid tumors. Targeting autophagy has controversial context-dependent effects in cancer treatment. As a FDA-approved lysosomotropic agent, hydroxychloroquine (HCQ) has been well tested as an autophagy inhibitor in preclinical models. Here, we elucidated the novel mechanism of HCQ alone or in combination with PI3Ki BKM120 in the treatment of cancer.Methods: The antitumor effects of HCQ and BKM120 on three different types of tumor cells were assessed by in vitro PrestoBlue assay, colony formation assay and in vivo zebrafish and nude mouse xenograft models. The involved molecular mechanisms were investigated by MDC staining, LC3 puncta formation assay, immunofluorescent assay, flow cytometric analysis of apoptosis and ROS, qRT-PCR, Western blot, comet assay, homologous recombination (HR) assay and immunohistochemical staining. Results: HCQ significantly sensitized cancer cells to BKM120 in vitro and in vivo. Interestingly, the sensitization mediated by HCQ could not be phenocopied by treatment with other autophagy inhibitors (Spautin-1, 3-MA and bafilomycin A1) or knockdown of the essential autophagy genes Atg5/Atg7, suggesting that the sensitizing effect might be mediated independent of autophagy status. Mechanistically, HCQ induced ROS production and activated the transcription factor NRF2. In contrast, BKM120 prevented the elimination of ROS by inactivation of NRF2, leading to accumulation of DNA damage. In addition, HCQ activated ATM to enhance HR repair, a high-fidelity repair for DNA double-strand breaks (DSBs) in cells, while BKM120 inhibited HR repair by blocking the phosphorylation of ATM and the expression of BRCA1/2 and Rad51. Conclusions: Our study revealed that HCQ and BKM120 synergistically increased DSBs in tumor cells and therefore augmented apoptosis, resulting in enhanced antitumor efficacy. Our findings provide a new insight into how HCQ exhibits antitumor efficacy and synergizes with PI3Ki BKM120, and warn that one should consider the “off target” effects of HCQ when used as autophagy inhibitor in the clinical treatment of cancer.

AN ACCURATE METHOD FOR THE ESTIMATION OF LOW CONCENTRATIONS OF DEXTRAN IN PLASMA

1957 ◽  
Vol 35 (6) ◽  
pp. 383-390 ◽  
Author(s):  
Robert E. Semple
Keyword(s):  
Aqueous Extract ◽  
Accurate Method ◽  
Protein Precipitation ◽  
In Vitro Tests ◽  
Plasma Samples ◽  
Carbohydrate Concentration ◽  
Low Concentrations ◽  
Standard Deviations

A method is presented for the determination in plasma of small (50–150 mg./100 ml.) amounts of dextran. The procedure, which requires between 3 and 4 hours, consists of protein precipitation, glucose removal by dialysis, and the determination of the carbohydrate concentration of the resulting aqueous extract by a modified anthrone technique. Results of in vitro tests show that average dextran recovery is essentially 100% and that standard deviations in recovery range from 1.7 to 2.5% depending upon the dextran concentration. Deviations are reduced to a range of 1.4–1.7% by the use of duplicate plasma samples.

scholarly journals Zinc(II) Terpyridine Complexes: Substituent Effect on Photoluminescence, Antiproliferative Activity, and DNA Interaction

Molecules ◽  
2019 ◽  
Vol 24 (24) ◽  
pp. 4519 ◽  
Author(s):  
Jiahe Li ◽  
Rongping Liu ◽  
Jinzhang Jiang ◽  
Xing Liang ◽  
Ling Huang ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Antiproliferative Activity ◽  
Conformational Transition ◽  
Dna Interaction ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Human Carcinoma ◽  
Ic50 Values ◽  
The Difference

A series of ZnCl2 complexes (compounds 1–10) with 4′-(substituted-phenyl)-2,2′:6′,2′′-terpyridine that bears hydrogen (L1), p-methyl (L2), p-methoxy (L3), p-phenyl (L4), p-tolyl (L5), p-hydroxyl (L6), m-hydroxyl (L7), o-hydroxyl (L8), p-carboxyl (L9), or p-methylsulfonyl (L10) were prepared and then characterized by 1H NMR, electrospray mass-spectra (ESI-MS), IR, elemental analysis, and single crystal X-ray diffraction. In vitro cytotoxicity assay was used to monitor the antiproliferative activities against tumor cells. Absorption spectroscopy, fluorescence titration, circular dichroism spectroscopy, and molecular modeling studied the DNA interactions. All of the compounds display interesting photoluminescent properties and different maximal emission peaks due to the difference of the substituent groups. The cell viability studies indicate that the compounds have excellent antiproliferative activity against four human carcinoma cell lines, A549, Bel-7402, MCF-7, and Eca-109, with the lowest IC50 values of 0.33 (10), 0.66 (6), 0.37 (7), and 1.05 (7) μM, respectively. The spectrophotometric results reveal that the compounds have strong affinity binding with DNA as intercalator and induce DNA conformational transition. Molecular docking studies indicate that the binding is contributed by the π…π stacking and hydrogen bonds, providing an order of nucleotide sequence binding selectivity as ATGC > ATAT > GCGC. These compounds intercalate into the base pairs of the DNA of the tumor cells to affect their replication and transcription, and the process is supposed to play an important role in the anticancer mechanism.

scholarly journals Преимущества и возможности флуоресцентных методов для визуализации апоптоза и аутофагии в опухолевых клетках человека in vitro-=SUP=-*-=/SUP=-

2019 ◽  
Vol 126 (6) ◽  
pp. 771
Author(s):  
Н.А. Наволокин ◽  
Н.В. Полуконова ◽  
Д.А. Мудрак ◽  
А.М. Мыльников ◽  
М.А. Барышникова ◽  
...  
Keyword(s):  
Acridine Orange ◽  
Tumor Cells ◽  
Human Tumor ◽  
Double Staining ◽  
Chemotherapy Drugs ◽  
Autophagy Induction ◽  
Methods Of Evaluation ◽  
Staining Methods

The possibilities of using fluorescent research methods and their advantages for visualization and determination of the type of programmed cell death of human tumor cells under the action of flavonoids in experiments in vitro were investigated. The object of the study were the tumor cells of cervical cancer HeLa and A498 kidney carcinoma, the flavonoid containing extract of hedge hyssop (Gratiola officinalis L.) was used for testing in the experiments. The following fluorescent methods were used: the "living and dead" test with double staining - - iodide propidium and acridine orange, the method of double staining with annexin and iodide propidium. The confirmation of autophagy induction was performed using Muse cell analyzer with fluorescent reagents MuseAutophagy LC3-Antibody Based Kit. The application of fluorescent staining methods using double staining with acridine orange and iodide propidium in the "living and dead" test compared to phase microscopy allows to visualize the formation of apoptotic cells and autophagosomes in cells and, therefore, can serve as one of the methods of evaluation screening of the effectiveness of various chemotherapy drugs.

scholarly journals THE CYTOTOXIC EFFECT OF CHELIDONIUM MAJUS IN VITRO

2015 ◽  
Vol 8 (2) ◽  
Author(s):  
Vladimíra Tomečková ◽  
Veronika Tkáčová ◽  
Peter Urban ◽  
Marek Stupák
Keyword(s):  
Tumor Cells ◽  
Hela Cells ◽  
Antiproliferative Activity ◽  
Cytotoxic Effect ◽  
Lymphoblastic Leukemia ◽  
Mammary Adenocarcinoma ◽  
Chelidonium Majus ◽  
Mcf 7 ◽  
Lipophilic Substances

The effect of aqueous and ether Chelidonium majus haulms extract on cervical HeLa tumor cells, mammary adenocarcinoma MCF 7 tumor cells and acute lymphoblastic leukemia CEM tumor cells in vitro have been studied. The purpose of this research was to compare the effect of aqueous and ether Chelidonium majus haulms extract on selected tumor cells. Colorimetric MTT assay have been used for the study of the antiproliferative effect of aqueous and ether haulms extract of Chelidonium majus on cell viability in vitro. The results of the experiments have shown the cytotoxic effect of the aqueous and the ether Chelidonium majus haulms extract on the individual tumor cells. The aqueous Chelidonium majus haulms extract was the most effective on CEM cells, it was less effective on MCF 7 cells and it was the least effective on HeLa cells. The ether haulms extract of Chelidonium majus was the most effective at all of studied concentrations on CEM cells and MCF 7 cells in comparison with HeLa cells, where it was significantly effective only at the highest concentration. Aqueous and ether haulms extract of Chelidonium majus tested in vitro indicated their cytotoxic activity. Both haulms extract of Chelidonium majus were more efficient on CEM cells. It is assumed that higher antiproliferative activity of ether haulms extract of Chelidonium majus is the result of higher antiproliferative activity of lipophilic substances. The lipophilic substances pass through membrane and bind to various proteins and change their biological activity.

scholarly journals Simultaneous Quantification of Hederacoside C and α-hederin in Hedera Nepalensis K.Koch Using HPLC-UV

2020 ◽  
Vol 36 (3) ◽  
Author(s):  
Do Thi Thuy Linh ◽  
Hoang Thanh Duong ◽  
Nguyen Tuan Hiep ◽  
Pham Thanh Huyen ◽  
Nguyen Minh Khoi ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Rapid Determination ◽  
Publishing House ◽  
Leaf Extracts ◽  
Hedera Helix ◽  
Dipeptidyl Peptidase 4 ◽  
Simultaneous Quantification ◽  
Study Results

 This study develops a high performance liquid chromatography with ultraviolet detection (HPLC-UV) for simultaneous quantification of hederacoside C and α-hederin in Hedera nepalensis K. Koch. The method proposed in this study was validated in terms of the analytical parameters such as high repeatability, high accuracy and good sensitivity. The method was used to determine the content of hederacoside C and α-hederin in Hedera nepalensis K. Koch, which had been collected in Ha Giang, Lao Cai and Lai Chau. The study results show that the content of hederacoside C and the content of α-hederin ranged from 0.40 to 4.01% and 0.21 – 0.54% based on absolute dry mass, respectively. Keywords Hedera nepalensis K. Koch, hederacoside C, α-hederin, HPLC-UV. References [1] L. Jafri, et al, In vitro assessment of antioxidant potential and determination of polyphenolic compounds of Hedera nepalensis K. Koch, Arabian Journal of Chemistry. 10 (2017) 3699-3706. https://doi.org/10.1016/j.arabjc.2014.05.002.[2] S. Saleem, et al, Plants Fagonia cretica L, and Hedera nepalensis K. Koch contain natural compounds with potent dipeptidyl peptidase-4 (DPP-4) inhibitory activity, Journal of ethnopharmacology. 156 (2014) 26-32. https://doi.org/10.1016/j.jep.2014.08.017[3] D.H. Bich, Medicinal plants and animals for medicine in Vietnam, Vol 1, Science and Technics Publishing House, Hanoi, 2006 (in Vietnamese).[4] National Institute Of Medicinal Materials, List of medicinal plants in Vietnam, Science and Technics Publishing House, Hanoi, 2016 (in Vietnamese).[5] L. Jafri, et al, Hedera nepalensis K. Koch: A Novel Source of Natural Cancer Chemopreventive and Anticancerous Compounds, Phytotherapy research. 30(3) (2016) 447-453. https://doi.org/10.1002/ptr.5546. [6] S. Kanwal, et al, Antioxidant, antitumor activities and phytochemical investigation of Hedera nepalensis K. Koch, an important medicinal plant from Pakistan, Pakistan Journal of Botany. 43 (2011) 85-89. [7] G. Uddin, et al, Biological screening of ethyl acetate extract of Hedera nepalensis stem, African Journal of Pharmacy and Pharmacology. 6(42) (2012) 2934-2937. https://doi.org/10.5897/AJPP12.828 [8] H. Kizu, et al, Studies on Nepalese Crude Drugs, III, On the Saponins of Hedera nepalensis K. Koch, Chemical and Pharmaceutical Bulletin. 33(8) (1985) 3324-3329. https://doi.org/0.1248/cpb.33.3324[9] X. Tong, et al, Extraction and GC-MS Analysis of Volatile Oil from Hedera nepalensis var sinensis, Fine Chemicals. 24(6) (2007) 559-561. [10] EDQM, European Pharmacopoeia, fifth ed., Council of Europe, France, 2015. [11] N.T.H. Mai, et al, Simultaneous Quantification of Hederacoside C and α-Hederin from the Leaves of Hedera helix L. by HPLC, Journal of Medicinal Material. 21(6) (2016). (in Vietnamese).[12] L. Havlíková, et al, Rapid Determination of α-Hederin and Hederacoside C in Extracts of Hedera helix Leaves Available in the Czech Republic and Poland, Natural product communications. 10(9) (2015). https://doi.org/10.1177/1934578X1501000910[13] M. Yu, et al, Determination of Saponins and Flavonoids in Ivy Leaf Extracts Using HPLC-DAD, Journal of Chromatographic Science. 53(4) (2014) 478-483. https://doi.org/10.1093/chromsci/bmu068.[14] EMEA, Validation of analytical procedures: text and methodology Q2 (R1), in International conference on harmonization, Geneva, Switzerland, 2005. [15] W. Horwitz, Official methods of analysis, 12 ed., Vol 1, Association of Official Analytical Chemists, Washington DC, 1975.

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