scholarly journals Synthesis of N-methyl-4-piperidone Curcumin Analogues and Their Cytotoxicity Activity against T47D Cell Lines

2018 ◽  
Vol 18 (2) ◽  
pp. 362 ◽  
Author(s):  
Yum Eryanti ◽  
Rudi Hendra ◽  
Tati Herlina ◽  
Adel Zamri ◽  
Unang Supratman
Keyword(s):  
Condensation Reaction ◽  
Yellow Crystal ◽  
T47d Cell ◽  
Crystal Form ◽  
Moderate Activity ◽  
Light Yellow Powder ◽  
Cytotoxicity Activity ◽  
Curcumin Analogues ◽  
Light Yellow ◽  
Ic50 Value

Three piperidone curcumin analogues (N-methyl-(3E,5E)-3,5-bis-(2-chlorobenzylidene)-4-piperidone (1), N-methyl-(3E,5E)-3,5-bis-(3-bromobenzylidene)-4-piperidone (2) and N-methyl-(3E,5E)-3,5-bis-(4-chlorobenzylidene)-4-piperidone (3)) were synthesized from N-methyl-4-piperidone with halogenbenzaldehyde, 2-chlorobenzaldehyde, 3-bromobenzaldehyde and 4-chlorobenzaldehyde. The Claisen-Schmidt condensation reaction was used in alkali condition with combinatorial. All the compounds showed light yellow needle, light yellow powder, and yellow crystal form with percentage of yield 39, 66, and 40%, respectively. All the structure compounds were confirmed by using UV, IR, 13C-NMR, 1H-NMR and MS. Apart from that, the cytotoxicity results against breast cancer cell (T47D) showed strong to moderate activity with the IC50 value 8, 4, and 45 µg/mL, respectively.

scholarly journals Cytotoxic Prenyl and Geranyl Coumarins from the Stem Bark of Casimiroa edulis

2020 ◽  
Vol 17 (9) ◽  
pp. 680-687
Author(s):  
Khun Nay Win Tun ◽  
Nanik Siti Aminah ◽  
Alfinda Novi Kristanti ◽  
Rico Ramadhan ◽  
Yoshiaki Takaya
Keyword(s):  
Methanolic Extract ◽  
T47d Cell ◽  
Stem Bark ◽  
Moderate Activity ◽  
Compound K ◽  
Pure Compound ◽  
Phytochemical Investigation ◽  
Ic50 Value ◽  
Casimiroa Edulis ◽  
First Time

Phytochemical investigation of the methanolic extract of the stem bark of Casimiroa edulis afforded four coumarins. Various spectroscopic experiments were used to characterize the isolated coumarins. The structures were identified as auraptene (K-1), suberosin (K-2), 5-geranyloxypsoralen (bergamottin) (K-3), and 8-geranyloxypsoralen (K-4), based on the chemical and spectral analysis. Among these compounds, suberosin (K-2) and 5-geranyloxypsoralen (bergamottin) (K-3) were isolated for the first time from this genus, and auraptene (K-1) was isolated from this plant for the first time. Cytotoxicity of pure compound K-4 and sub-fraction MD-3 was evaluated against HeLa and T47D cell lines and moderate activity was found with an IC50 value in the range 17.4 to 72.33 μg/mL.

scholarly journals Alkaloid Caulerpin and Cytotoxic Activity against NCL-H460 Lung Cancer Cells Isolated along with β-sitosterol from the Halimeda cylindracea Decaisne

2021 ◽  
Vol 50 (9) ◽  
pp. 2663-2674
Author(s):  
Iwan Dini ◽  
Nunuk Hariani Soekamto ◽  
Firdaus Firdaus ◽  
Unang Supratman ◽  
Jalifah Latip
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Chemical Structure ◽  
Spectroscopic Method ◽  
Lung Cancer Cells ◽  
Moderate Activity ◽  
Cytotoxicity Activity ◽  
Ic50 Value ◽  
First Time

Alkaloid caulerpin (1), along with β-sitosterol (2), were isolated from the n-hexane extract of the macroalga Halimeda cylindracea Decaisne. The chemical structure was identified by a spectroscopic method including IR, MS, UV, NMR 1D, NMR 2D, and comparison with data of spectra previously reported. Compounds (1) and (2) were isolated for the first time from this macroalga. Compund (1) were evaluated for their cytotoxicity activity against NCL-H460 lung cancer cells in vitro and showed moderate activity with IC50 value of 20.05 µg/mL.

scholarly journals Preliminary Screening of Corn Silk (Zea mays L.) for Antioxidant Properties and Cytotoxicity Activity on Human Myelogenous Leukemia Cell Line

2020 ◽  
Vol 2 (1) ◽  
pp. 52
Keyword(s):  
Ethyl Acetate ◽  
Mtt Assay ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Myelogenous Leukemia ◽  
Leukemia Cell Line ◽  
Total Phenolic ◽  
Cytotoxicity Activity ◽  
Corn Silk ◽  
Ic50 Value

One of the traditionally used herbs is the byproduct of the maize plant, the 10-20 cm long corn silk which from the female maize flowers. The aim of this study is to evaluate the total phenolic content, antioxidant activity, and cytotoxicity activity of corn silk. The corn silk was minced and was extracted with methanol-water (80 % v/v), methanol, ethanol, ethyl acetate, and hexane by using the maceration method. The total phenolic content (TPC) of corn silk was determined to assess the presence and level of phenolic compounds in each sample. The antioxidant activities of all corn silk extracts were determined via DPPH method, and MTT assay was used to study the viability of the cells after the cells were treated with corn silk extracts at different time intervals. The highest phenolic content was exhibited by the methanol extract. The EC50 value for methanol-water (80 % v/v), methanol, ethanol, ethyl acetate and hexane extracts were 251 μg/ ml, 300 μg/ ml, 330 μg/ ml, 550 μg/ ml and 1736 μg/ ml respectively. The MTT assay, the lowest IC50 values at 24 and 48 hours intervals, was exhibited by methanol-water extract (104 μg/ ml). In contrast, methanol (308 μg/ ml) was found with the highest IC50 value for all 24, 48, and 72 hours intervals. At 72 hours interval, ethyl acetate (88 μg/ ml) shown the lowest IC50 value. This study suggested that corn silk could be potentially used as a source of antioxidant and can further evaluate for cancer studies.

Synthesis and Evaluation of in vitro Antiplatelet Aggregation Activities of 2-Methoxy-5-Aminobenzamides

2019 ◽  
Vol 16 (9) ◽  
pp. 1040-1050
Author(s):  
Lili Liu ◽  
Xiujie Liu ◽  
Guangling Chen ◽  
Kai Qiu
Keyword(s):  
L929 Cells ◽  
Cytotoxicity Activity ◽  
Antiplatelet Aggregation ◽  
Ic50 Value ◽  
Lower Effect ◽  
New Compounds ◽  
Group Characteristics ◽  
Better Than ◽  
Methoxybenzoic Acid

Objective: According to the principles of drug design, the structures of picotamide and betrixaban were combined to design novel series of 2-methoxy-5-aminobenzamides. A total of twenty new compounds 1a-1t have been synthesized and evaluated for their antiplatelet aggregation activities in vitro. Methods: In the structural design of target compounds 1a-1t, the betrixaban was retained group characteristics and the picotamide was retained its 1, 3, 4-substitution position. With 2-methoxybenzoic acid as starting material, compounds 1a-1t were synthesized after 5 steps of nitration, acylation, ammoniation, reduction and secondary ammoniation. And their antiplatelet aggregation activities in vitro were assessed by the Born test with ADP, arachidonic acid and collagen as inducing agents, respectively, and with aspirin and picotamide as two reference drugs. Results: The compound 1f (46.14%±0.07) had the highest activity for ADP and its IC50 value was 0.17 µM, far better than the two control drugs aspirin (0.44 µM) and picotamide (0.47 µM). The IC50 value of four compounds 1i (0.24 µM), 1j (0.22 µM), 1r (0.25 µM) and 1t (0.24 µM), displayed higher antiplatelet activities in vitro for AA than aspirin (0.43 µM) and picotamide (0.34 µM). Evaluation of cytotoxicity activity of the compounds against L929 cells line revealed that at lower concentration of 10 µmol·L-1, compound 1p had lower effect on L929 cells, and its cell survival rate (88.24%±4.16) was higher than that (82.35%±4.16) of picotamide. Conclusion: Novel series of 2-methoxy-5-aminobenzamides has shown higher in vitro antiplatelet activities and lower effect on L929 cells at lower concentration.

scholarly journals Chemical Composition and Lipoxygenase Inhibitory Activity of the Essential Oil of Alstonia Angustiloba

2021 ◽  
Author(s):  
Wan Mohd Nuzul Hakimi Wan Salleh ◽  
Muhammad Helmi Nadri ◽  
Shamsul Khamis
Keyword(s):  
Gas Chromatography ◽  
Essential Oil ◽  
Inhibitory Activity ◽  
Mass Spectrometry Analysis ◽  
Gas Chromatography Mass Spectrometry ◽  
Chemical Components ◽  
Moderate Activity ◽  
Spectrometry Analysis ◽  
Ic50 Value ◽  
Total Oil

This study was aimed to investigate the chemica l compositions and lipoxygenase inhibitory activity of the essential oil from Alstonia angustiloba growing in Malaysia. The essential oils were obtained by hydrodistillation and fully characterized by gas chromatography and gas chromatography-mass spectrometry. Analysis of the A. angustiloba essential oil resulted in the identification of twenty-five chemical components, attributed 90.8% of the total oil. The most abundant components of A. angustiloba oil were linalool (21.2%), 1,8-cineole (16.8%), α-terpineol (9.5%), terpinene-4-ol (8.5%), β-caryophyllene (6.2%), and caryophyllene oxide (5.2%). The essential oil displayed moderate activity towards lipoxygenase activity with IC50 value of 45.8 μg/mL.

scholarly journals Cytotoxic and Apoptotic-inducing Effect of Fraction Containing Brazilein from Caesalpinia sappan L. and Cisplatin on T47D Cell Lines

2017 ◽  
Vol 6 (3) ◽  
pp. 89
Author(s):  
Prisnu Tirtanirmala ◽  
Annisa Novarina ◽  
Rohmad Yudi Utomo ◽  
Raisatun Nisa Sugiyanto ◽  
Riris Istighfari Jenie ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Annexin V ◽  
T47d Cell ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Effects ◽  
Caesalpinia Sappan ◽  
Main Compound ◽  
T47d Breast Cancer Cell ◽  
Ic50 Value

Anticancer activity of secang’s heartwood (Caesalpinia sappan L.) is based on its main compound: brazilin and brazilein. Brazilin, brazilein, and other compounds such as caesalpiniaphenol can affect proteins that have a role in apoptosis. In this study, we observed cytotoxic activity of fraction containing brazilein (FCB) alone or in combination with chemotherapeutic agent, cisplatin and the ability of the combination to induce apoptosis in T47D breast cancer cell lines. Cytotoxicity assay was determined using MTT assay, whereas the detection apoptosis induction was conducted using flow cytometry using Annexin-V and propidium iodide. FCB and cisplatin showed cytotoxic effect on T47D cells with IC50 value of 68 µg/mL and 16 µM, respectively. Combination of FCB and cisplatin result synergistic combination at the concentration ratio of 1/2 IC50 with CI value of 0.66. Its combination also able to induce apoptosis on T47D cell population 13% larger than the single treatment. Based on this study, we conclude that FCB is able to enhance the cytotoxic effects of cisplatin by inducing apoptosis.Keywords:  Caesalpinia sappan L., cisplatin, apoptosis, breast cancer

scholarly journals Über Oxostannate(II), IV [1] Zur Kenntnis von Rb2SnO2 und K2SnO2 [2] / On Oxostannates(II), IV Rb2SnO2 and K2SnO2

1982 ◽  
Vol 37 (6) ◽  
pp. 688-694 ◽  
Author(s):  
Rolf M. Braun ◽  
Rudolf Hoppe
Keyword(s):  
Single Crystals ◽  
Lattice Energy ◽  
Yellow Powder ◽  
Light Yellow Powder ◽  
Ionic Radii ◽  
Space Group ◽  
Coordination Numbers ◽  
Binary Oxides ◽  
Light Yellow ◽  
Brown Powder

Abstract The new compound Rb2SnO2 was obtained as a light yellow powder by heating mixtures of the binary oxides (RbO0.48 + SnO, Rb: Sn = 2:1) under argon (sealed Ag cylinders, 600 °C, 3d). Subsequent annealing (550 °C, 8d and 500 °C, 17 d) led to light yellow transparent single crystals. Rb2SnO2 is extremely sensitive to moisture and decomposes into black products. It crystallizes orthorhombicly in the space group P212121-D42, with a = 5.761, b = 7.493, c= 11.167 Å, Z = 4, drö = 4.43 and dpyk = 4.46 gcm-3 , R= 11.8 and Rw = 12.0%. Effective Coordination Numbers, ECoN, these via Mean Fictive Ionic Radii, MEFIR, and the Madelung Part of Lattice Energy, MAPLE, have been calculated. Isotypic K2SnO2 was obtained similarly as a brown powder, a = 5.579, b = 7.246, c = 16.744 Å.

scholarly journals Isolation and Characterization of Secondary Metabilites and Evaluation of Antimicrobial, Antioxidant and Thrombolytic Potentials of Erythrina variegata L. Bark

2019 ◽  
Vol 31 (8) ◽  
pp. 1842-1846
Author(s):  
Fatema Tabassum ◽  
Choudhury Mahmood Hasan ◽  
Mohammad Mehedi Masud ◽  
Md. Imran Nur Manik ◽  
Monira Ahsan
Keyword(s):  
Methanolic Extract ◽  
Authentic Sample ◽  
Stem Bark ◽  
Moderate Activity ◽  
Zone Of Inhibition ◽  
Nmr Studies ◽  
Erythrina Variegata ◽  
Isolation And Characterization ◽  
Ic50 Value

Six compounds, sitosta-4-en-3-one (1), 3β,28-dihydroxyolean-12-en (2), scandenone (3), alpinum isoflavone (4), stigmasterol (5) and lupeol (6) were isolated from the methanol soluble extract of the stem bark of Erythrina variegata. The structure of the compounds was established by extensive NMR studies as well as co-TLC with authentic sample. The petroleum ether, carbon tetrachloride, chloroform and aqueous soluble fractions of the methanolic extract of Erythrina variegata were evaluated for antimicrobial, antioxidant and thrombolytic properties. In the antimicrobial study, most of the fractions of the extract exhibited mild to moderate antimicrobial activity where the zone of inhibition were ranging from 7.69 to 19.51 mm. The chloroform soluble fraction showed significant antioxidant activity with IC50 value 66.28 μg/mL as compared to standard BHT (IC50 value 23.09 μg/mL). The thrombolytic property of different extracts of E. variegata exhibited moderate activity ranging from 31.25 to 57.78 %.

scholarly journals Cytotoxic Test of Extract and Fraction of Dendrophtoe Pentandra (L) Miq on T47D Cell

2019 ◽  
Vol 22 (3) ◽  
pp. 73-78
Author(s):  
Masayu Farah Diba ◽  
Salni Salni ◽  
Subandrate Subandrate
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Effect ◽  
Linear Equations ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
T47d Cell ◽  
Assay Method ◽  
Cytotoxic Effects ◽  
Ic50 Value ◽  
Ethanol Fraction

Indonesia has a variety of plants that have the potential for medicine. One of the plants used by the community as a drug with anticancer effects is Dendrophtoe petandra (L.) Miq. This study aims to determine the cytotoxic effect of ethanol extract, ethyl acetate fraction and water ethanol fraction of Dendrophtoe petandra (L.) Miq on T47D breast cancer cells. The cytotoxic effects of ethanol extract, ethyl acetate fraction and water ethanol fraction were carried out by MTT assay method using series concentration. Cytotoxic effects were assessed by calculating IC50 values using linear equations. Phytochemical test showed that Dendrophtoe petandra (L.) Miq contained saponins, terpenoids, flavonoids and tannins. The IC50 value of the ethanol extract, ethyl acetate fraction and water ethanol fraction were 417.506 μg/mL, 233.617 μg/mL, and 2748.357 μg/mL, respectively. The smaller the IC50 value means that the compound is more active. Water ethanol fraction of Dendrophtoe petandra (L.) Miq does not have a cytotoxic effect, whereas ethanol extract and ethyl acetate fraction of Dendrophtoe petandra (L.) Miq have cytotoxic effects in the medium strength category. The content of flavonoids and saponins in ethanol extract and ethyl acetate fraction of Dendrophtoe petandra (L.) Miq is thought to play role in causing T47D cell death. Cytotoxic effects of ethyl acetate fraction are stronger than ethanol extracts.

Synthesis, in vitro Acetylcholinesterase Inhibitory Activity Evaluation and Docking Investigation of Some Aromatic Chalcones

MedPharmRes ◽  
2017 ◽  
Vol 1 (1) ◽  
pp. 15-25
Author(s):  
Dao Tran ◽  
Son Tran ◽  
Vi Nguyen ◽  
Tri Le ◽  
Minh Thai ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Condensation Reaction ◽  
Acetylcholinesterase Inhibitors ◽  
Docking Studies ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Ellman’S Method

In this study, a total of twenty chalcones were synthesized via Claisen-Schmidt condensation reaction and evaluated for their in vitro acetylcholinesterase inhibitory activities using Ellman’s method. Molecular docking studies on acetylcholinesterase were performed to elucidate the interactions between these chalcone derivatives and acetylcholinesterase active site at the molecular level. From the series, six compounds (S1-5 and S17) exhibited strong acetylcholinesterase inhibitory activities with IC50 values below 100 µM compared to the parent unsubstituted chalcone. Compound S17 (4’-amino-2-chlorochalcone) showed the strongest acetylcholinesterase inhibitory activity in the investigated group with IC50 value of 36.10 µM. Molecular modeling studies were consistent with the results of in vitro acetylcholinesterase inhibitory activities, and chalcone S17 could be considered as a potential lead compound for the development of new acetylcholinesterase inhibitors.

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