scholarly journals Isolation of Cyanobacterial Strains from Water and Soil Samples in Hanoi and Investigation of Their Cytotoxic Activity

2021 ◽  
Vol 37 (3) ◽  
Author(s):  
Ngo Thi Trang ◽  
Tong Thi Ngoc Anh ◽  
Lai Ngoc Khanh ◽  
Tran Thi Hang ◽  
Nguyen Thi Bich Loan ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Hela Cells ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Soil Samples ◽  
Accurate Mass ◽  
Mtt Test ◽  
Cytotoxic Compounds ◽  
Water And Soil Samples ◽  
Ic50 Values

As a part of ongoing efforts to exploit the pharmaceutical potential of domestic cyanobacteria, six strains belonging to the Nostocales order have been isolated from several sampling sites in Ha Noi as prerequisite material. The cytotoxic activity evaluation based on the MTT test resulted in four extracts from two strains (NK7 and NK1111) exhibiting the inhibitory activity against HeLa cells, with IC50 values ranging from 84.6 µg/mL to 257.3 µg/mL. In addition, the bioassay-guided isolation of the HK7 methanol extract led to one cytotoxic activity K3 fraction possessing two natural compounds. Compounds 1 showed the accurate mass of 352.2633 Da with the formula of C21H36O4 similar to three cytotoxic compounds 7Z-plakortide H, 10-gingerdiol, and ebelactone B. Compound 2 had the accurate mass of 278.1545 Da with the formula of C16H22O4 similar to four cytotoxic compounds pestaloficiol G, penicitrinol E-D, and isoversiol C.

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.

Cytotoxic Constituents from the Bark of Erythrina poeppigiana Against the MCF-7 Breast Cancer Cell Lines

2020 ◽  
Vol 10 (3) ◽  
pp. 257-261
Author(s):  
Tati Herlina ◽  
Merlin ◽  
Mohd. Azlan ◽  
Unang Supratman
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Chemical Structure ◽  
Breast Cancer Cell Lines ◽  
Erythrina Poeppigiana ◽  
Structure Activity ◽  
Cancer Line ◽  
Cytotoxic Compounds ◽  
Ic50 Values ◽  
Mcf 7

Background: Erythrina poeppigiana (Leguminosae) is a high-growing plant with an orange flower that is widely distributed in tropical and subtropical countries. This particular plant is widely used in traditional medicine for gynecological complications and the treatment of various diseases. There exists no previous information regarding cytotoxic compounds from this plant. Objective: This research is to isolate cytotoxic compounds from E. poeppigiana. Methods: The isolation step was carried out using a combination of chromatographic techniques to obtain isolated three compounds (1, 2, and 3). Results: The chemical structure of isolated compounds was elucidated by spectroscopic methods and identified as β-erythroidine (1), 8-oxo-β-erythroidine (2), and 8-oxo-α-erythroidine (3). Compounds (1-3) showed cytotoxic activity against MCF-7 breast cancer line with IC50 values of 36.8, 60.8 and 875.4 μM, respectively. Conclusion: Three compounds have been successfully isolated from Erythrina poeppigiana (Leguminosae), showing cytotoxic properties against MCF-7 breast cancer line. Structure-activity relationship studies showed that the presence of enone moiety on compound 1 can reduce its cytotoxic activity towards MCF-7 breast cancer line.

scholarly journals Active Cytotoxic Compounds and Essential Oil from Bougainvillea Alba

2015 ◽  
Vol 15 (1) ◽  
pp. 49
Author(s):  
AbdEl-nabi E. EL-Deeb ◽  
Ibrahim M. Abdel-Aleem ◽  
Samir M. El-Amin ◽  
Laila A. Refahy ◽  
Maha A. El-Shazly
Keyword(s):  
Cytotoxic Activity ◽  
Methyl Palmitate ◽  
Methanol Extract ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
Srb Assay ◽  
Human Tumor Cell ◽  
Oil Fraction ◽  
Oil Fractions ◽  
Cytotoxic Compounds

Chemical analysis of methanol extract of flowers and leaves of Bougainvillea alba led to isolation of four compounds identified as 3’, 4’, 6 - trimethoxy, 5 – hydroxyl 7-prenyl 3-O- (feruloyl (1→2) - rhamnpyranosyl) flavone[1], 3-O β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl (1→3”) β-D-glucopyranosyl (1→3”’) α-L–xylopyrenoside [2], Lepidolide [3], E feruloyl 3-O- Coumaroyl α-L Rhamnopyranoside [4]. In addition, two oil fractions, the major identified components of oil are Elemene, Lanceol , Nerolidol , Methyl palmitate and Abietatriene. Cytotoxic activity of methanol extract of both leaves and flowers of <em>Bougainvillea alba</em>, isolated compounds and oil fractions were determined using the SRB Assay on human tumor cell line (Hepatocyte generation 2, HepG2). The isolated compounds showed cytotoxic activity at LC50 15.2, 17.2, 15.6 and 2.82 μg/ml for compound 1,2, 3 and 4 respectively, while the two oil fraction showed activity at 2.67 μg/ml.

scholarly journals Chemical constituents and theira-glucosidase inhibitory activity of the stem of Salacia chinensis L.

2021 ◽  
Vol 5 (3) ◽  
pp. first
Author(s):  
Huu Tho Le ◽  
Truc Thanh Thi Duong ◽  
Phu Hoang Dang ◽  
Truong Nhat Van Do ◽  
Hai Xuan Nguyen ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Back Pain ◽  
Inhibitory Activity ◽  
Spectroscopic Analysis ◽  
Methanol Extract ◽  
Chemical Constituents ◽  
Positive Control ◽  
Ic50 Values ◽  
Treatment Of Diabetes ◽  
Chcl3 Fraction

Salacia chinensis L., known as “Chop mao” in Vietnam, is a climbing shrub that belongs to the Celastraceae family. The stem of S. chinensis L. is used as a traditional medicine for the treatment of diabetes, rheumatoid arthritis, back pain, … The dried powdered stem of S. chinensis L. was collected in Phu Yen province and was extracted with methanol to yield methanol extract. The methanol extract was suspended in H2O and partitioned successively with n-hexane, CHCl3, EtOAc to obtain n-hexane, CHCl3, EtOAc, and H2O fractions, respectively. The CHCl3 fraction was subjected to a series of chromatographic separation to afford four purified compounds including 3-oxolup-20(29)-en-30-al (1), betulin-3-caffeate (2), 2-(4-hydroxy-3,5-dimethoxylphenyl)ethanol (3), and acetosyringone (4). Their structures were elucidated on the basis of the spectroscopic analysis and comparison with literature data. The isolated compounds were tested for their α-glucosidase inhibitory activity. The result indicated that all compounds (1-4) possessed significant α-glucosidase at the testing concentration of 100 µM with the percent inhibition values of 9.5 ± 1.3, 70.89 ± 0.25, 44.2 ± 1.6, and 6.7 ± 1.7 %, respectively. In addition, betulin-3-caffeate (2) and 2-(4-hydroxy-3,5-dimethoxylphenyl)ethanol (3) show more potent α-glucosidase inhibitory activity, with IC50 values of 69.7 and 152.0 µM, respectively, than that of positive control acarbose (IC50 = 214.5 µM).

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 The Effect of Marigold Leaves and Doxorubicin Toward Cell Cycle and Apoptosis of T47D Cells

2017 ◽  
Vol 7 (3) ◽  
pp. 79
Author(s):  
Anis Fauzia ◽  
Umi Any Tiyas Wati ◽  
Cahyaning Gita Rizkita ◽  
Eka Wahyuni Nurul Qori'ah ◽  
Ibrahim Arifin
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Methanol Extract ◽  
Apoptosis Induction ◽  
Use Values ◽  
Ic50 Values ◽  
Index Value

Doxorubicin is a commonly used chemotherapeutic agent in patients with breast cancer. The risk of side effect using of doxorubicin  such as cardiomyopathy and congestive heart failure which can lead to death. One of the  approach to overcome overloaded use of doxorubicin is the combined use with a chemopreventive agent (cochemotherapy), including the leaf extract of marigolds (Cosmos caudatus Kunth.). This research aims to reviewing the effect of the methanol extract of leaves of marigolds on the cytotoxic activity of doxorubicin in modulating cell cycle and apoptosis of breast cancer cells T47D. Determination of the cytotoxic activity of methanol extract of leaves of marigolds and doxorubicin as well as a combination of both conducted by MTT assay. modulation surveillance of cell cycle and apoptosis induction is done by using flowcytometry and analyzed by FACS Calibur program. Cytotoxicity assay single treatment of the methanol extract of leaves of marigolds produce use values of IC50 504,840 μg/ml, whereas IC50 values doxorubicin is 141,055 nM. The synergistic effect was shown a combination of methanol extract leaves marigolds and doxorubicin at concentrations of 84,17 μg/ml -23,5 nM; 84,17 μg/ml -47 nM; 126,25 μg/ml -23,5 nM; 252,5 μg/ml -35,25 nM and 252,5 μg/ml -71 nM with a combination index value (CI) consecutively of 0,5; 0,6; 0,6; 0,6 and 0,6. Observations modulation of cell cycle and apoptosis induction combination of methanol extract leaves marigolds and doxorubicin at concentrations of 84,17 μg/ml -23,5 nM, said that a combination of the methanol extract of leaves of marigolds and doxorubicin to inhibit the proliferation of cells in G2 / M phase and able to induce apoptosis of breast cancer cells T47D.Keywords: methanol extract of leaves of marigolds, doxorubicin, flowcytometry, cell cycle, apoptosis.

scholarly journals 4-Benzyloxylonchocarpin and Muracatanes A-C from Ranunculus muricatus L. and Their Biological Effects

Biomolecules ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 1562
Author(s):  
Hidayat Hussain ◽  
Iftikhar Ali ◽  
Daijie Wang ◽  
Nilufar Z. Mamadalieva ◽  
Wahid Hussain ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Nmr Spectroscopy ◽  
Thyroid Carcinoma ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
Colorectal Adenocarcinoma ◽  
Biological Effects ◽  
Current Investigation ◽  
Inhibitory Effects ◽  
Ic50 Values

Ranunculus muricatus L. is a spiny fruit buttercup that is used in various traditional medicinal systems. In the current investigation of R. muricatus, the new chalcone 4-benzyloxylonchocarpin (1), the new anthraquinone muracatanes A (2), the new-to-nature anthraquinone muracatanes B (3), and the new naphthalene analog muracatanes C (4) were isolated, in addition to the three previously reported compounds, 4-methoxylonchocarpin (5), β-sitosterol (6), and β-sitosterol β-D-glucopyranoside (7). Their structures were elucidated using 1D (1H and 13C) and 2D (COSY, HSQC, and HMBC) NMR spectroscopy and HR-ESI-MS. Chalcone 1 showed potent acetylcholinesterase inhibitory effects with Ki of 5.39 µM and Ki′ of 3.54 µM, but none of the isolated compounds showed inhibitory activity towards butyrylcholinesterase. Anthraquinone 3 illustrated α-glucosidase inhibitory effects with IC50-values of 164.46 ± 83.04 µM. Compound 5 displayed moderate cytotoxic activity towards ovarian carcinoma (A2780, IC50 = 25.4 µM), colorectal adenocarcinoma (HT29, IC50 = 20.2 µM), breast cancer (MCF7, IC50 = 23.7 µM), and thyroid carcinoma (SW1736, IC50 = 26.2 µM) while it was inactive towards pharynx carcinoma (FaDu: IC50 > 30 µM).

Anti-HIV 1 Activity of Xanthones from the Bark of Mammea harmandii

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Ponsiri Liangsakul ◽  
Chutima Kuhakarn ◽  
Sakchai Hongthong ◽  
Surawat Jariyawat ◽  
Kanoknetr Suksen ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Chemical Structures ◽  
Anti Hiv ◽  
Hiv 1

A new xanthone glycoside 1 together with four known flavonoid derivatives, astilbin (2), neoastilbin (3), isoastilbin (4), and epicatechin (5) were isolated from the ethyl acetate fraction partitioned from the methanol extract of the bark of Mammea harmandii. The chemical structures of all isolated compounds were established on the basis of their spectroscopic data. Compound 1 exhibited selective significant inhibitory activity in the anti-syncytium assay with an EC50 value of 11.44 μM (SI = 14.03) while it was found inactive against HIV 1 reverse transcriptase as well as cytotoxic activity.

scholarly journals Assessment of antioxidant and xanthine oxidase inhibitory activity of Triadica cochinchinensis stem bark

2019 ◽  
Vol 1 (1) ◽  
pp. 39-44
Author(s):  
Carla Wulandari Sabandar ◽  
◽  
Juriyati Jalil ◽  
Norizan Ahmat ◽  
Nor-Ashila Aladdin ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Radical Scavenging ◽  
Stem Bark ◽  
Total Phenolic ◽  
Xanthine Oxidase Inhibitors ◽  
Ic50 Values ◽  
Organic Fractions ◽  
Promising Source

Triadica cochinchinensis has been used traditionally to treat diseases related to oxidative stress. Nonetheless, little is known about its biological activity. This study aimed to evaluate the antioxidant and xanthine oxidase inhibitory activity of this plant. For this purpose, qualitative phytochemicals, total phenolic, total flavonoid, antioxidant assays (DPPH and FRAP), and xanthine oxidase assay were evaluated towards methanol and organic fractions of its stem bark. Results showed the occurrence of flavonoids, tannins, terpenoids, steroids, and saponins in the methanol extract. The extract and its two fractions (ethyl acetate and methanol) exhibited promising radical scavenging (IC50 values between 3.6-4.5 μg/mL) and ferric reduction activities (4.2-5.5 μg/μg of equivalent trolox amount). They also exhibited inhibition on the xanthine oxidase activity ranging from 43.8 to 80.5% at a dose of 100 μg/mL. These activities could be attributed to the amount of phenolics in the methanol extract and active fractions (136.6-174.1 mg GAE/g of sample). Our results suggested that the methanol extract of T. cochinchinensis stem bark could be used as a promising source of lead molecules for antioxidant and xanthine oxidase inhibitors from natural source.

Novel Pyrazolo[3,4-d]pyrimidines as Potential Cytotoxic Agents: Design, Synthesis, Molecular Docking and CDK2 Inhibition

2019 ◽  
Vol 19 (11) ◽  
pp. 1368-1381
Author(s):  
Mai Maher ◽  
Asmaa E. Kassab ◽  
Ashraf F. Zaher ◽  
Zeinab Mahmoud
Keyword(s):  
Molecular Docking ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Agents ◽  
Human Cancer Cell Lines ◽  
Ic50 Values

Background: Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine. Objective: To design and synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives as bioisosters of roscovitine with potential cytotoxic and CDK2 inhibitory activity. Methods: A series of novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidines were designed and synthesized. Structural elucidation for all the newly synthesized compounds was achieved through performing MS, 1H NMR, 13C NMR and IR spectral techniques. Eight compounds were screened for their cytotoxic activity by National Cancer Institute (USA) against 60 different human cancer cell lines. Compounds 2a, 4, 6, 7b, 8a and 8b were further studied through the determination of their IC50 values against the most sensitive cell lines. The inhibitory activities of compounds 2a and 4 were evaluated against CDK2 enzyme. Results: Compound 4 exhibited the most prominent broad-spectrum cytotoxic activity against 42 cell lines representing all human cancer types showing growth inhibition percentages from 53.19 to 99.39. Compound 2a showed promising selectivity against several cell lines. Moreover, all the test compounds exhibited potent cytotoxic activity in nanomolar to micromolar range with IC50 values ranging from 0.58 to 8.32μM. Compound 2a showed significant cytotoxic activity against CNS (SNB-75), lung (NCI-H460) and ovarian (OVCAR-4) cancer cell lines with IC50 values 0.64, 0.78 and 1.9μM, respectively. Compound 4 showed promising potency against leukemia (HL-60) and CNS (SNB-75) cell lines (IC50 = 0.58 and 0.94μM, sequentially). Moreover, the antiproliferative activities of compounds 2a and 4 appeared to correlate well with their ability to inhibit CDK2 at sub-micromolar level (IC50 = 0.69 and 0.67μM, respectively) that were comparable to roscovitine (IC50=0.44μM). The Molecular docking results revealed that compound 4 interacted with the same key amino acids as roscovitine in the active site of CDK2 enzyme with a marked docking score (-14.1031 kcal/mol). Conclusion: 1-(4-Flourophenyl)pyrazolo[3,4-d]pyrimidine is a promising scaffold for the design and synthesis of potent cytotoxic leads.

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