scholarly journals The Anticancer Activity of Srikaya Leaves Fraction (Annona squamosa L.): An In Vitro Study

2019 ◽  
Vol 3 (4) ◽  
pp. 39-44
Author(s):  
Makbruri Amin ◽  
Irsan Saleh ◽  
Rachmat Hidayat
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Anticancer Drugs ◽  
T Test ◽  
Therapeutic Effects ◽  
Annona Squamosa ◽  
Methanol Fraction ◽  
T47d Cells ◽  
Average Percentage ◽  
Ic50 Value

Abstract Introduction: Anticancer drugs are aimed primarily at inhibiting the growth and proliferation of cancer cells. Srikaya leaves (Annona squamosa L.) had been proven to possess various therapeutic effects and potential to be developed as anticancer drugs due to its cytotoxic activity. Aim of study: This study aimed to assess the anticancer activity of srikaya leaves (Annona squamosa L.) fraction. Methods: Methanol fraction of srikaya leaves were obtained at concentrations of 500; 250; 125; 62.5; 31.25 µg/ml. Srikaya methanol fraction and cisplatin as control were given to a plate that was sealed with T47D cells for MTT assay. Identification of compounds in the methanol fraction of srikaya leaves was performed with thin layer chromatography (TLC). Data were collected in the form of absorbance value and half-maximal inhibitory concentration (IC50) value was determined ​​by linear regression. Data analysis was carried out with paired T test, unpaired T test, and ANOVA. Results: Average percentage of T47D cells viability increased with the decrease in the concentration of srikaya methanol fraction. Obtained IC50 value was 174.25 µg/ml which was quite active and potential to be developed as an anticancer drug. Methanol fraction of srikaya leaves contained secondary terpenoid metabolites, steroids, phenols, flavonoids, alkaloids and tannins. Flavonoid was the dominant metabolites in phytochemical tests and believed to play a major role in cytotoxic activity of srikaya leaves. Conclusion: Methanol fraction of srikaya leaves possessed the cytotoxic effect on T47D cancer cell line through the role of flavonoid metabolites.   Keywords: srikaya, Annona squamosa, anticancer, T47D cells

scholarly journals CYTOTOXIC EFFECT OF AQUADEST, ETHANOLIC, AND CHLOROFORM EXTRACTS OF Spathoglottis plicata Blume ON BREAST CANCER CELLS LINE (T47D CELLS)

2015 ◽  
Vol 2 (1) ◽  
pp. 64
Author(s):  
Mukhlish Jamal Musa Holle ◽  
Hestri Dyah Puspitasari ◽  
Andaru Satryo ◽  
Wahyu Dewi Astuti Ningrum ◽  
Digdo Sudigyo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Mtt Assay ◽  
Breast Cancer Cells ◽  
Chloroform Extract ◽  
Probit Analysis ◽  
Antioxidant Compounds ◽  
T47d Cells ◽  
Ic50 Value

Breast cancer is one of cancer with high mortality. This cancer not only attacks women, but also men. Indonesia has many plants which potential as anticancer, such as orchids. Spathoglottis plicata is one of the orchid species that abundant in Indonesia and has a lot of antioxidant compounds which is guessed have anticancer properties. The objectives of this study were to study the cytotoxic activity and IC50 value of aquadest, ethanolic, and chloroform extracts of S. plicata’s pseudobulbs, leaves, and whole plants on T47D cells (breast cancer cells line) as well as cytotoxic activity of the specific fraction of the most toxic crude extract. S. plicata used in this study was obtained from Bungarinte nursery. Extractions were done by maceration method using aquadest, ethanol, and chloroform as the solvent. Cytotoxic test on T47D cells were done by MTT assay. The cytotoxic data were analyzed using one-way ANOVA followed by Tukey’s HSD test. The IC50 of each extracts were calculate by probit analysis. The lowest IC50 value among all extracts was fractionated and isolated by preparative TLC. The cytotoxic activity and IC50 of this fractions were analyzed. The results showed that only 2 from 9 crude extracts that able to calculate its IC50 because those two extracts have concentration dependent pattern of inhibition concentration. Chloroform extract have the lowest IC50 value (369,837 μg/mL). Then, this extract fractionated by eluen n-hexane : ethyl acetate 4:1. Four fractions were collected. The lowest IC50 value is fraction IV (144,41 μg/mL). Based on the results it could be concluded that S. plicata leaves have moderate potency to develop as anticancet agents, especially on breast cancer. Keywords: S. plicata, T47D cells, cytotoxic, MTT assay, preparative TLC. 

scholarly journals The Effect of Soursop Leaves Fraction (Annona squamosa L.) as Anticancer

2020 ◽  
Vol 1 (1) ◽  
pp. 32-40
Author(s):  
Makbruri Amin ◽  
Irsan Saleh
Keyword(s):  
Cell Line ◽  
In Vitro Study ◽  
T47d Cell ◽  
Polar Fraction ◽  
Annona Squamosa ◽  
Methanol Fraction ◽  
Ic50 Value ◽  
T47d Cell Line

Anticancer drugs are primarily aimed at inhibiting the growth andproliferation of cancer cells. The soursop plant (Annona squamosa L.) has thepotential to be developed as an anticancer drug. This plant contains severalactive compounds including flavonoids, borneol, camphor, alkaloids, terpenes,saponins, tannins, polyphenols and polyketide compounds. This study wasconducted to assess the efficacy of the polar fraction of soursop leaves oncytotoxic activity based on the IC₅₀ value in T47D cells. This research isexperimental in vitro study using cell line T47D. The methanol fraction ofsoursop leaves was diluted with DMSO and DMEM to obtain a concentration of500; 250; 125; 62.5; 31.25 µg/ mL cisplatin with a concentration of 50:25:12,5:6,25:3,125 µg/mL. The methanol fraction of soursop from the highestconcentration of 500 µg/ml has average viability of 46.77% and the averagepercentage of viability will increase in proportion to the decrease in theconcentration of the test compound. The IC50 value shows the concentrationvalue that results in the inhibition of cell proliferation by 50% of the population.In conclusion, methanol fraction of soursop leaves have an anticytotoxic effecton T47D cell line through the role of flavonoid metabolites.

scholarly journals Synergistic Combination of Ciplukan (Physalis angulata) Herbs Ethanolic Extract and Doxorubicin on T47D Breast Cancer Cells

2010 ◽  
Vol 1 (1) ◽  
pp. 26
Author(s):  
Inna Armandari ◽  
Kartika Dyah Palupi ◽  
Sofa Farida ◽  
Adam Hermawan ◽  
Ratna Asmah Susidarti ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Cardiac Toxicity ◽  
Chemotherapeutic Agent ◽  
Ethanolic Extract ◽  
High Dose ◽  
T47d Cells ◽  
Ic50 Value

Doxorubicin is one of chemotherapeutic agent widely used in breast cancer treatment, but in high dose doxorubicin gives negative side effect, including vomit, nausea, immune suppression, and cardiac toxicity. This toxicity hopefully could be reduced by combination chemotherapy using natural herbs such as ciplukan herb. This research was conducted to explore cytotoxic activity of single ciplukan herbs ethanolic extract and its combination with doxorubicin on T47D breast cancer cells. Cytotoxic activity of ciplukan herbs ethanolic extract only and its combination with doxorubicin were tested on T47D cells using MTT assay to obtain IC50 value and combination index (CI), respectively. Single extract showed cytotoxic activity on T47D cells with IC50 value of was 160 µg/ml. Thus, combination treatment from ciplukan herbs ethanolic extract and doxorubicin showed synergistic effect (CI<1,0). This effect was reached at concentration of ciplukan herbs ethanolic extract-doxorubicin 80 μg/ml- 2 nM, 80 μg/ml-4 nM, and 80 μg/ml-8 nM. This research indicated that ciplukan herbs ethanolic extract is potential to be applied as co-chemotherapeutic agent in breast cancer therapy.Key word : ciplukan herbs, doxorubicin, co-chemotherapy, T47D cells

scholarly journals Cytotoxic Assay of Semipolar Fraction Of Ethanolic Extract From Sugar Apple (Annona Squamosa L.) Stem Bark on T47D Cells

2020 ◽  
Vol 17 (2) ◽  
pp. 148-156
Author(s):  
Cita Hanif Muflihah ◽  
Haryoto Haryoto ◽  
Peni Indrayudha
Keyword(s):  
Qualitative Analysis ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Mobile Phase ◽  
Ethanolic Extract ◽  
Stem Bark ◽  
Annona Squamosa ◽  
T47d Cells ◽  
Apple Stem ◽  
Vacuum Liquid Chromatography

Previous research has shown that some compounds in leaves and seeds of sugar apple have a cytotoxic activity. The aim of this research was to determine the cytotoxicity of semipolar fraction of ethanolic extract from sugar apple stem bark (Annona squamosa L.) on T47D cancer cells. The semipolar fraction of ethanolic extract from sugar apple stem bark was collected by fractionation using Vacuum Liquid Chromatography (VLC) with hexane:ethyl acetic (9:1, 8:2, 7:3, and  6:4)  as  mobile  phase.  Cytotoxicity from the fractions of five different concentration namely; 25, 50, 100, 150, and 250, µg/mL was measured by MTT assay. The potency of the cytotoxicity was defined by the ability of the fraction to inhibit the growth of T47D cells indicated by the value of IC50. Qualitative analysis of contained compounds in the fraction was done by Thin Layer Chromatography (TLC) method using silica gel F 254 as a stationary phase and hexane:ethyl acetic (7:3) as a mobile phase. UV 254 and 366 nm lamp also Dragendorff, citroboric, and FeCl3 spray reagents were used to visualize the spots of the secondary metabolites. The result proved that the semipolar fraction of ethanolic extract from sugar apple stem bark showed potential cytotoxicity on T47D cancer cells with IC50value of 70,77 µg/mL. Qualitative analysis showed that the fraction contained flavonoids and alkaloids which is presumably responsible for its cytotoxic activity. 

scholarly journals CYTOTOXIC ACTIVITY AND APOPTOSIS INDUCTION OF T47D CELL LINES BY Turbinaria decurrens EXTRACT

2013 ◽  
Vol 8 (1) ◽  
pp. 23 ◽  
Author(s):  
Muhammad Nursid ◽  
Nurrahmi Dewi Fajarningsih ◽  
Ekowati Chasanah
Keyword(s):  
Flow Cytometry ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Crude Extract ◽  
T47d Cell ◽  
Apoptosis Induction ◽  
Flow Cytometry Analysis ◽  
Methanol Fraction ◽  
Ic50 Value

Marine algae is known to contain a wide variety of biomedical compounds having pharmaceutical applications. The aim of this research was to evaluate cytotoxic activity and apoptosis induction of Turbinaria decurrens extract on T47D cell lines.  Cytotoxic activity test was conducted by using MTT assay whereas detection of apoptosis was evaluated by DNA fragmentations and flow cytometry analysis. The MTT test showed that crude extract had medium cytotoxic activity to T47D, HepG2, and C28 cell lines with IC50 value of 172, againts 360 and 330 µg ml-1, respectively. After solvent partition of crude extract, the cytotoxic activity of n-hexane and ethyl acetate fractions T47D cell increased, the cytotoxic activity of n. hexane and ethyl acetate fractions T47D cell increased with  IC50  value of with IC50  43.1 and 51.9 µg ml-1, respectively, whereas IC50 value of methanol fraction was 383.0 µg ml-1. Analysis of DNA fragmentation of T47D cell showed that  both n-hexane and ethyl acetate fractions could not fragment DNA as a features of apoptosis. However, flow cytometry analysis by using annexin-V and propidium iodide staining revealed that n-hexane and ethyl acetate fractions could induce apoptosis in T47D cell. This research indicated that Turbinaria decurrens had potency to induce apoptosis in T47D cells.

Recent Design and Structure-Activity Relationship Studies on Modifications of DHFR Inhibitors as Anticancer Agents

2019 ◽  
Vol 26 ◽  
Author(s):  
Agnieszka Wróbel ◽  
Danuta Drozdowska
Keyword(s):  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Physicochemical Characterization ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Biological Research ◽  
Structure Activity ◽  
Dhfr Inhibitors

Background: Dihydrofolate reductase (DHFR) has been known for decades as a molecular target for antibacterial, antifungal and anti-malarial treatments. This enzyme is becoming increasingly important in the design of new anticancer drugs, which is confirmed by numerous studies including modelling, synthesis and in vitro biological research. This review aims to present and discuss some remarkable recent advances on the research of new DHFR inhibitors with potential anticancer activity. Methods: The scientific literature of the last decade on the different types of DHFR inhibitors has been searched. The studies on design, synthesis and investigation structure-activity relationship were summarized and divided into several subsections depending on the leading molecule and its structural modification. Various methods of synthesis, potential anticancer activity and possible practical applications as DHFR inhibitors of new chemical compounds were described and discussed. <p> Results: This review presents the current state of knowledge on the modification of known DHFR inhibitors and the structures and searching for over eighty new molecules, designed as potential anticancer drugs. In addition, DHFR inhibitors acting on thymidylate synthase (TS), carbon anhydrase (CA) and even DNA-binding are presented in this paper. <p> Conclusion: Thorough physicochemical characterization and biological investigations it is possible to understand structure-activity relationship of DHFR inhibitors. This will enable even better design and synthesis of active compounds, which would have the expected mechanism of action and the desired activity.

Design of Lamivudine Loaded Nanoparticles for Oral Application by Nano Spray Drying Method: A New Approach to use an Antiretroviral Drug for Lung Cancer Treatment

2020 ◽  
Vol 23 (10) ◽  
pp. 1064-1079
Author(s):  
Ahmet Alper Öztürk ◽  
İrem Namlı ◽  
Kadri Güleç ◽  
Şennur Görgülü
Keyword(s):  
Lung Cancer ◽  
Cancer Treatment ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Drugs ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lung Cancer Treatment ◽  
Anticancer Properties ◽  
Ft Ir

Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer. Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage. Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity. Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined. Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

Synthesis and Anticancer Activity of New Hydrazide-hydrazones and Their Pd(II) Complexes

2019 ◽  
Vol 16 (5) ◽  
pp. 522-532 ◽  
Author(s):  
Bedia Kocyigit-Kaymakcioglu ◽  
Senem Sinem Yazici ◽  
Fatih Tok ◽  
Miriş Dikmen ◽  
Selin Engür ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
A549 Cells ◽  
Cancer Cell Line ◽  
Fibroblast Cell ◽  
Reference Drug ◽  
A549 Cancer Cell Line

Background: Hydrazones, one of the important classes of organic molecules, are pharmaceutical agents comprising –CO-NH-N=CH- group in the structure therefore and exhibiting significant biological activity. Methods: 5-Chloro-N’-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II) complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer and normal 3T3 fibroblast cell lines, using the MTT assay. Results: Anticancer activity screening results revealed that some compounds showed remarkable cytotoxic effect. Among them, 5-chloro-N'-[(4-hydroxyphenyl)methylidene] pyrazine-2-carbohydrazide (3c) displayed higher cytotoxic activity against A549 cancer cell line than the reference drug cisplatin. Conclusion: Compound 3c showed high cytotoxic activity against A549 cancer cell line but it showed low cytotoxic effect against normal 3T3 fibroblast cell line. Antiproliferative and antimetastatic effects of 3c were determined by the real-time monitoring of cell proliferative system (RTCA DP). The cell proliferation, metastatic and invasive activities of A549 cells were decreased due to increased concentration of 3c.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

Cyclopentadienyl‐Based Anticancer Drugs: Improvement of Cytotoxic Activity through Functionalisation of the π Ligand

ChemMedChem ◽  
2021 ◽  
Author(s):  
Monika Absolonová ◽  
Lucie Melounková ◽  
Jaromír Vinklárek ◽  
Jan Honzíček ◽  
Libor Dostál ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Drugs
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