scholarly journals APRICOXIB

2018 ◽  
Vol 25 (12) ◽  
pp. 1915-1922
Author(s):  
Fatima Rizvi ◽  
Syed Mahboob Alam ◽  
Farah Asad ◽  
Hina Shams
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Mtt Assay ◽  
Cytotoxic Effects ◽  
Inflammatory Conditions ◽  
Ic50 Value ◽  
Ht 29 ◽  
Mcf 7

Background: Breast cancer is most frequently diagnosed cancer globally but there is not any ideal economical and safer agent that not only decreases the progression but also resolve complexities associated with breast cancer such as inflammatory conditions. There was strong link between inflammation and cancer specially breast cancer. Thus by inhibiting the COX enzyme may inhibit the progression of cancer beside of its role in inflammatory conditions of breast. Study Design: Interventional In Vitro trial. Setting: Department of Pharmacology in alliance with PCMD. Period: The duration of study from April 2016 to February 2017. Methodology: For this purpose we used five cancerous lines MCF-7, MDA-MB-231, MCF-10, HT-29 and Hela cell lines. For demonstrating the cytotoxic effects of Apricoxib we used MTT assay (for all cell Lines) and Trypan blue dye exclusion assay (Primarily for MCF-7 cell lines). For calculation of minimum dose required for exert cytotoxic effects of Apricoxib and its selectivitytowards cancerous cells of breast tissue we calculated its IC50 value and Selectivity Index (SI) by MTT assay. Results: Apricoxib significantly reduce the viability of MCF-7, MDA-MB-231, Hela, HT-29 as assessed by MTT assay in dose dependent manner (χ2 (2) = 26.483, p<0.001), (χ2 (2) = 26.49, p<0.001), (χ2 (2) = 26.062, p<0.001) and (χ2 (2) = 26.062, p<0.001) respectively. However Apricoxib had non-significant effects on % viability of MCF-10 cell line (χ2 (2) = 4.167, p=0.654) as assessed by MTT assay. Furthermore Apricoxib had lowest IC50 value against MCF-7 cell line. Conclusion: This study demonstrated that beside of primarily anti-inflammatory effects Apricoxib have additional benefits in term of exerting the cytotoxic effects (in vitro) on cancerous cell lines as indicated by reducing the % viability and reducing the Absorbance value of test sample as compare to control. This opens the newer path for researcher to evaluate different aspects of Apricoxib in field of chemotherapy.

scholarly journals The Cytotoxic Effects of Humic Acid on Human Breast Cancer Cells

Proceedings ◽  
2018 ◽  
Vol 2 (25) ◽  
pp. 1565
Author(s):  
Asli Aykac ◽  
Eda Becer ◽  
Tuğçe Balcı Okcanoğlu ◽  
Meryem Güvenir ◽  
Kaya Süer ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Humic Acid ◽  
Cell Line ◽  
Cytotoxic Effect ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Cytotoxic Effects ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

Breast cancer is the most common cancer among women and in order to create alternative treatments different types of in vivo and in vitro studies have used various plant-based therapeutic agents. Humic acid (HA) induces apoptosis and has various pharmacological properties including anti-inflammatory and anti-proliferative effects. In our study, we examined the cytotoxic effects of HA at concentrations of 5, 10, 20, 50 and 100 μg/mL in human breast adenocarcinoma MCF-7 cell line for 24 and 48 h. By using MTT method, it has been found out that HA 100 g/mL had cytotoxic effect on human breast adenocarcinoma MCF-7 cell line at both 24 and 48 h; also found out that the effective dose of HA at the same time (24 and 48 h) was 50 μg/mL. The results of our study will shed light on the development of alternative therapeutic approaches in the treatment of cancer by evaluating the cytotoxic effect of HA.

scholarly journals In vitro apoptosis induction ability of methanolic extract of Paramignya trimera root (Xao tam phan) in breast cancer stem cells

2019 ◽  
Vol 6 (8) ◽  
pp. 3325-3332 ◽  
Author(s):  
Sinh Truong Nguyen ◽  
Le Van Manh Hung ◽  
Nguyen Thi Thanh Mai ◽  
Nguyen Trung Nhan ◽  
Nguyen Xuan Hai ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Treatment ◽  
Cell Line ◽  
Cell Lines ◽  
Plant Extract ◽  
Methanolic Extract ◽  
Fluorescent Microscopy ◽  
Apoptosis Induction ◽  
Ic50 Value

Objective: Cancer has been considered as one of the world's leading causes of death. Recently, the Paramignya trimera plant, locally called ``Xao Tam Phan'', has become a popular Vietnamese medicinal herb that is used as alternative medicine for cancer treatment support with minimal side effects. In this study, we aimed to demonstrate the cytotoxicity of methanolic extract of Paramignya trimera on a Vietnamese breast cancer stem cell line (VNBRCA1) in vitro. Methods: We used the MTT assay to determine the cytotoxicity of the extract on VNBRCA1 cells and human fibroblast (HF) cell line was used as a control for the plant extract treatment. Clinically used anticancer drug, doxorubicin, was used as a control drug (for relative comparison to the plant extract) to evaluate the selective cytotoxicity of the plant extract on VNBRCA1 and HF cells. We examined the apoptosis induction by the plant extract on VNBRCA1by Annexin V/7AAD staining and flow cytometry analysis. In addition, the morphology of apoptotic nuclei of treated cells was observed by fluorescent microscopy using double fluorescent staining: Hoechst 33342 and propidium iodide (PI). Results: In comparison between the cytotoxicity of the plant extract and Doxorubicin on both cell lines (VBRCA1 and HF), we observed that plant extract was selectively cytotoxic against VNBRCA1 with an IC50 value of 10610 μg/mL, while Doxorubicin was discriminatorily cytotoxic against HF with an IC50 value of 0.135+/-0.09 μg/mL. We also found that the plant extract induced apoptosis VNBRCA1 in a dose-dependent manner. In addition, fluorescent microscopy revealed disintegrated nuclei of plant extract-treated cells, representing a hallmark of apoptosis. Conclusions: These results showed that Paramignya trimera methanolic extract selectively killed VNBRCA1 cell lines, indicating that Paramignya trimera methanolic extract may represent a potential agent for cancer treatment.

scholarly journals Sitotoksisitas in vitro ekstrak etanolik buah parijoto (Medinilla speciosa, reinw.ex bl.) terhadap sel kanker payudara T47D

2014 ◽  
Vol 2 (2) ◽  
pp. 53-58 ◽  
Author(s):  
Iin Tusanti ◽  
Andrew Johan ◽  
RA Kisdjamiatun
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Colorimetric Assay ◽  
Ethanolic Extract ◽  
T47d Cell ◽  
Ic50 Value ◽  
T47d Cell Line

Background: Several studies focused on phytochemical as agents of cancer prevention and co-chemotherapy. One of Indonesian plant which has edible fruit but it hasn’t been completely explored is Medinilla speciosa (Reinw.ex Bl.). Objective : The aim of this study is to examine the cytotoxic activity (IC50 value) of Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract. Methods : Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract was used in this study. The cytotoxic activity was investigated in vitro on human breast cancer T47D cell-line. The cells viability were assessed using MTT colorimetric assay. Breast cancer T47D cell lines was treated with fruit ethanolic extract (10, 25, 50, 100, 250, 500 and 1000 µg/ml) for 24 hour of incubation. This study also identified phytochemical compound of the fruit with thin layer chromatography (TLC). Results: The result showed that ethanolic extract of Medinilla speciosa (Reinw.ex Bl.) has moderate cytotoxicity on breast cancer T47D cell line with IC50 value of 614.50 µg/ml and yield the decrease of cell viability at higher concentration. Medinilla speciosa fruit can not be used as anticancer agent but chemoprevention agent. Phytochemical test showed that the fruit extract contain flavonoid and saponin compound. Conclusion: Ethanolic extract of Medinilla speciosa fruit exhibited moderate cytotocicity on breast cancer T47D cell lines with IC50 value was 614,50 µg/ml thus it can be used as chemopreventioan agent.

scholarly journals Cytotoxic activities of Methanolic and Chloroform Extract of Cryptocarya Massoy (Oken) Kosterm. Bark on MCF-7 human breast cancer cell line

2018 ◽  
Vol 9 (1) ◽  
pp. 57-62
Author(s):  
Yuli Widiyastuti ◽  
Ika Yanti M. Sholikhah ◽  
Sari Haryanti
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Cancer Cell Line ◽  
Chloroform Extract ◽  
Cytotoxic Activities ◽  
Litsea Cubeba ◽  
Mcf 7

Abstrak Latar Belakang. Krangean [Litsea cubeba (Lour.) Pers.] Adalah salah satu tanaman aromatik purba di Indonesia. Tanaman ini adalah anggota keluarga Lauraceae, tumbuh liar di dataran tinggi Sumatera, Kalimantan, dan pulau Jawa. Aktivitas antikanker tanaman ini belum banyak dieksplorasi. Penelitian ini bertujuan untuk mengetahui kandungan fitokimia dan aktivitas sitotoksik ekstrak buah krangean pada sel kanker manusia secara in vitro. Metode. Kloroform dan metanol digunakan untuk mempererat bubuk buah kering selama 3x24 jam. Senyawa fitokimia utama ditandai dengan KLT (kromatografi lapis tipis). Uji MTT dilakukan untuk mengamati morfologi dan viabilitas kanker serviks HeLa, kanker payudara MCF-7, dan sel HEPG2 hepar. Hasil. Hasil penelitian menunjukkan bahwa karakterisasi KLT ekstrak kloroform dan metanol Litsea cubeba menunjukkan profil yang sama, dengan senyawa utama yang ditemukan adalah terpenoid dan alkaloid. Uji MTT menemukan bahwa kedua ekstrak memiliki penghambatan kuat pada sel HeLa. Ekstrak kloroform menunjukkan aktivitas sitotoksik yang lebih kuat dibandingkan dengan metanol, dengan nilai IC50 masing-masing 33,7 dan 64,8 μg / mL. Kesimpulan. Esktrak kloroform dan ekstrak metanol dari Litsea cubeba memiliki aktivitas yang kuat terhadap sel HeLa dan aktivitas sedang terhadap sel HEPG2 dan MCF-7.  Selanjutnya disarankan untuk dilakukan penelitian lebih lanjut untuk mengathui senyawa aktif L. cubeba (Lour.) Pers. yang memiliki aktivitas antikanker potensial. Kata kunci: Litsea cubeba (Lour.) Pers., sitotoksik, HeLa, MCF-7, HebG2, MTT assay   Abstract Background. Krangean [Litsea cubeba (Lour.) Pers.] is one of ancient aromatic plants in Indonesia. This plant is the member of Lauraceae family, growing wild on the highlands of Sumatera, Kalimantan, and Java island. The anticancer activity of this plant haven’t been explored extensively.This research aimed to investigate phytochemical content and cytotoxic activity of krangean fruits extract on human cancer cell line in vitro. Method. Chloroform and methanol were used to macerate dried fruits powder for 3x24 hours. Major phytochemical compounds was characterized by TLC (thin layer chromatography). MTT assay was done to observe morphology and viability of HeLa cervical cancer, MCF-7 breast cancer, and HepG2 hepar cancer cell line. Result. The results showed that TLC characterization of chloroform and methanolic extracts of Litsea cubeba revealed similar profile, with the major compound found are terpenoid and alkaloid. The MTT assay found that both extracts have strong inhibition on HeLa cell line. Chloroform extract exhibited stronger cytotoxic activities compared to methanol, with the IC50 values of 33,7 and 64,8 μg/mL respectively. While, the both extract have moderate cytotoxic activities to HEPG2 and MCF-7 cancer cell line indicated by IC50value more than 100 mg/mL. Conclusion. Chloroform and methanolic extract of Litsea cubeba have a strong activity againts HeLa cancer cell lines and moderate activity to HEPG2 and MCF-7, thought chloroform extract of Litsea cubeba has stronger effect on cancer cell line viability. It is well recommended for further studies to investigate the active compound of L. cubeba (Lour.) Pers. for potential anticancer activity.   Key words: Litsea cubeba (Lour.) Pers., cytotoxic, HeLa, MCF-7, HebG2, MTT assay

ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

2017 ◽  
Vol 63 (1) ◽  
pp. 141-145
Author(s):  
Yuliya Khochenkova ◽  
Eliso Solomko ◽  
Oksana Ryabaya ◽  
Yevgeniya Stepanova ◽  
Dmitriy Khochenkov
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Antitumor Effect ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

(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.

In Vitro Evaluation of Chitosan Induced Cytotoxicity against Cancerous Cell lines: MCF-7, Saos-2 and HeLa

2019 ◽  
Vol 19 ◽  
Author(s):  
Zeinab Abedian ◽  
Niloofar Jenabian ◽  
Ali Akbar Moghadamnia ◽  
Ebrahim Zabihi ◽  
Roghayeh Pourbagher ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Fibroblast Cells ◽  
Apoptosis Induction ◽  
Cytotoxic Effects ◽  
Cancerous Cell ◽  
Significant Concentration ◽  
Mcf 7

Objective/ Background: Cancer is still the most common cause of morbidity in world and new powerful anticancer agents without severe side effects from natural sources is important. Methods: The evaluation of cytotoxicity and apoptosis induction was carried out in MCF-7,HeLa and Saos-2 as cancerous cell lines with different histological origin and human fibroblast served as control normal cell. The cells were treated with different concentrations of chitosan and the cytotoxicity was determined using MTT assay after 24, 48 and 72 h .The mode of death was evaluated by flow cytometry . Results: While both types of chitosan showed significant concentration-dependently cytotoxic effects against the three cancerous cell lines, fibroblast cells showed somehow more compatibility with chitosan. On the other hand, there were no significant differences between LMWC and HMWC cytotoxicity in all cell lines. The flow cytometry results showed the apoptosis pattern of death more in Saos-2 and HeLa while necrosis was more observable with MCF7. Also higher viability with both types of chitosan was seen in fibroblast as normal cells Conclusion: Chitosan shows anticancerous effect against 3 cancerous cell lines, while it is compatible with normal diploid fibroblast cells. Furthermore, it seems that the molecular weight of chitosan does not affect its anticancerous property.

Design, Synthesis and Cytotoxicity Evaluation of New 3, 5-Disubstituted-2-Thioxoimidazolidinones

2018 ◽  
Vol 18 (4) ◽  
pp. 573-582 ◽  
Author(s):  
Khaled R.A. Abdellatif ◽  
Mostafa M. Elbadawi ◽  
Mohammed T. Elsaady ◽  
Amer A. Abd El-Hafeez ◽  
Takashi Fujimura ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Topoisomerase I ◽  
Cancer Cell Line ◽  
Cytotoxic Agents ◽  
Dependent Manner ◽  
Human Lung Fibroblast ◽  
Mcf 7

Background: Some 2-thioxoimidazolidinones have been reported as anti-prostate and anti-breast cancer agents through their inhibitory activity on topoisomerase I that is considered as a potential chemotherapeutic target. Objective: A new series of 3,5-disubstituted-2-thioxoimidazolidinone derivatives 10a-f and their S-methyl analogs 11a-f were designed, synthesized and evaluated for cytotoxicity against human prostate cancer cell line (PC-3), human breast cancer cell line (MCF-7) and non-cancerous human lung fibroblast cell line (WI-38). </P><P> Results and Method: While compounds 10a-f showed a broad range of activities against PC-3 and MCF-7 cell lines (IC50 = 34.0 – 186.9 and 24.6 – 147.5 µM respectively), the S-methyl analogs 11a-f showed (IC50 = 22.7 – 198.5 and 16.9 – 188.2 µM respectively) in comparison with 5-fluorouracil (IC50 = 60.7 and 40.7 µM respectively). 11c (IC50 = 22.7 and 29.2 µM) and 11f (IC50 = 28.7 and 16.9 µM) were the most potent among all compounds against both PC-3 and MCF-7 respectively with no cytotoxicity against WI-38. Conclusion: The newly synthesized compounds showed good activity against PC-3 and MCF-7 cell lines in comparison with 5-fluorouracil. Compounds 11c and 11f bound with human topoisomerase I similar to its known inhibitors and significantly inhibited its DNA relaxation activity in a dose dependent manner which may rationalize their molecular mechanism as cytotoxic agents.

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