scholarly journals Potensi antitumor dari beberapa spons laut asal teluk Manado

2017 ◽  
Vol 2 (2) ◽  
pp. 99
Author(s):  
Wilson Alexander Raymond Rombang
Keyword(s):  
Cell Activity ◽  
Leukemia Cell ◽  
Marine Sponges ◽  
Meoh Extract ◽  
Etoac Extract ◽  
Etoh Extract ◽  
Boring Sponge ◽  
Ic50 Value ◽  
Cytotoxic Compounds ◽  
Murine Leukemia Cell

Screening of antitumor for the extract and fraction from the marine sponges ofManado Gulf, Aaptos sp., Acervochalina sp., Gelliodes sp., Theonella sp., and orangeboring sponge have been done by use P388 murine leukemia cell. Activity test resultshowed IC50 of the extract and fraction from Aaptos sp were: MeOH extract 5938ng/mL and BuOH extract 125000 ng/mL; Acervochalina sp: EtOH extract 125000ng/mL, PE extract 125000 ng/mL, EtOAc extract 4251 ng/mL, BuOH extract125000 ng/mL; Gelliodes sp: EtOH extract 125000 ng/mL; Theonella sp: EtOHextract 125000 ng/mL, PE extract 9282 ng/mL, EtOAc extract 3273 ng/mL, BuOHextract 125000 ng/mL; orange boring sponge: MeOH extract 1422 ng/mL. Based onthe IC50 value, it could be concluded that MeOH extract of Aaptos sp., EtOAc extractof boring sponge could be a sources for cytotoxic compounds.

scholarly journals Triterpenoids from the Bark of Aglaia glabrata and their In vitro Effects on P-388 Murine Leukemia Cells

2019 ◽  
Vol 35 (1) ◽  
pp. 134-139
Author(s):  
Desi Harneti ◽  
Asep Supriadin ◽  
Rani Maharani ◽  
Nurlelasari Nurlelasari ◽  
Tri Mayanti ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Leukemia Cell ◽  
2D Nmr ◽  
Leukemia Cell Lines ◽  
Ic50 Value ◽  
In Vitro Effects ◽  
Murine Leukemia Cell ◽  
Reported Data ◽  
Murine Leukemia

Four dammarane-type triterpenoids, dammardienon (1), aglaiabbreviatin E (2), dammar-20,25-dien-3b,24-diol (3) and dammar-24-en-3b,20-diol (4) were isolated from methanolic extract of the bark of Aglaia glabrata. The structures of all triterpenoids were elucidated by 1D-, 2D-NMR, and comparison with previously reported data. All triterpenoids were applied into in vitro bioassay against P-388 murine leukemia cell. Dammar-24-en-3b,20-diol (4) has cytotoxic activity with IC50 value of 9.45 mM towards P-388 murine leukemia cell lines.

Cytotoxic and Pro-apoptotic Activities of Diterpenoids from Zhumeria Majdae

2020 ◽  
Vol 17 ◽  
Author(s):  
Abolfazl Shakeri ◽  
Samira Navabi Nejad ◽  
Javad Asili ◽  
Milena Masullo ◽  
Mansoor Saeidi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cytotoxic Effect ◽  
Therapeutic Agent ◽  
2D Nmr ◽  
Etoac Extract ◽  
Chemical Structures ◽  
Ic50 Value ◽  
Cytotoxic Compounds ◽  
First Time ◽  
Mcf 7

Abstract:: Since the ethylacetate (EtOAc) extract of the roots of Zhumeria majdae had the potent cytotoxic effect (IC50 < 50 μg/ml) on three cancer cell lines; MCF-7, PC3 and MDA-MB-231, therefore the purpous of this study is to isolation of the responcible cytotoxic compounds from the plant. Isolation of the extract led to the identification of four diterpenoids named as lanugon Q (1), 12,16-dideoxy aegyptinone B (2), 12-deoxy-salvipisone (3) and manool (4). The chemical structures have been determined on the basis of 1D and 2D NMR experiments. Compound 1 is reported for the first time in the plants of Zhumeria genus. The results of cytotoxic and apoptotic evaluation revealed that compound 2 had the strong cytotoxic effect with the IC50 value of 15.90 μg/ml against MCF-7 cell lines. Sub-G1 peak in flow cytometry histogram of cells treated with EtOAc axtract and compound 2 showed the induction of apoptosis. Changes in the Bax/Bcl-2 ratio and cleavage of PARP were observed. It is to be noted that owing to strong cytotoxic effect, Z. majdae extract could be represented as therapeutic agent against cancer.

Antioxidant effects and in vitro cytotoxicity on human cancer cell lines of flavonoid-rich Flamboyant (Delonix regia (Bojer) Raf.) flower extract

2020 ◽  
Vol 21 ◽  
Author(s):  
Putthiporn Khongkaew ◽  
Phanphen Wattanaarsakit ◽  
Konstantinos I. Papadopoulos ◽  
Watcharaphong Chaemsawang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Leukemia Cell Line ◽  
Flower Extract ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Murine Leukemia Cell ◽  
Dose Dependent

Background: Cancer is a noncommunicable disease with increasing incidence and mortality rates both worldwide and in Thailand. Its apparent lack of effective treatments is posing challenging public health issues. Introduction: Encouraging research results indicating probable anti-cancer properties of the Delonix regia flower extract (DRE) have prompted us to evaluate the feasibility of developing a type of product for future cancer prevention or treatment. Methods and Results: In the present report, using High Performance Liquid Chromatography (HPLC), we demonstrate in the DRE, the presence of high concentrations of three identifiable flavonoids, namely rutin 4.15±0.30 % w/w, isoquercitrin 3.04±0.02 %w/w, and myricetin 2.61±0.01 % w/w respectively while the IC50 of DPPH and ABTS assay antioxidation activity was 66.88±6.30 µg/ml and 53.65±7.24 µg/ml respectively. Discussion: Our cancer cell line studies using the MTT assay demonstrated DREs potent and dose dependent inhibition of murine leukemia cell line (P-388: 35.28±4.07% of cell viability remaining), as well as of human breast adenocarcinoma (MCF-7), human cervical carcinoma (HeLa), human oral cavity carcinoma (KB), and human colon carcinoma (HT-29) cell lines in that order of magnitude. Conclusion: Three identifiable flavonoids (rutin, isoquercitrin and myricetin) with high antioxidation activity and potent and dose dependent inhibition of murine leukemia cell line and five other cancer cell lines were documented in the DRE. The extract’s lack of cytotoxicity in 3 normal cell lines is a rare advantage not usually seen in current antineoplastic agents. Yet another challenge of the DRE was its low dissolution rate and long-term storage stability, issues to be resolved before a future product can be formulated.

scholarly journals A KDM4A-PAF1-mediated epigenomic network is essential for acute myeloid leukemia cell self-renewal and survival

2021 ◽  
Vol 12 (6) ◽  
Author(s):  
Matthew E. Massett ◽  
Laura Monaghan ◽  
Shaun Patterson ◽  
Niamh Mannion ◽  
Roderick P. Bunschoten ◽  
...  
Keyword(s):  
Acute Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Cell Activity ◽  
Leukemia Cell ◽  
Gene Signature ◽  
Pathological Feature ◽  
Self Renewal ◽  
Stem Cell Activity ◽  
Molecular Mechanism Of Action ◽  
Acute Myeloid

AbstractEpigenomic dysregulation is a common pathological feature in human hematological malignancies. H3K9me3 emerges as an important epigenomic marker in acute myeloid leukemia (AML). Its associated methyltransferases, such as SETDB1, suppress AML leukemogenesis, whilst H3K9me3 demethylases KDM4C is required for mixed-lineage leukemia rearranged AML. However, the specific role and molecular mechanism of action of another member of the KDM4 family, KDM4A has not previously been clearly defined. In this study, we delineated and functionally validated the epigenomic network regulated by KDM4A. We show that selective loss of KDM4A is sufficient to induce apoptosis in a broad spectrum of human AML cells. This detrimental phenotype results from a global accumulation of H3K9me3 and H3K27me3 at KDM4A targeted genomic loci thereby causing downregulation of a KDM4A-PAF1 controlled transcriptional program essential for leukemogenesis, distinct from that of KDM4C. From this regulatory network, we further extracted a KDM4A-9 gene signature enriched with leukemia stem cell activity; the KDM4A-9 score alone or in combination with the known LSC17 score, effectively stratifies high-risk AML patients. Together, these results establish the essential and unique role of KDM4A for AML self-renewal and survival, supporting further investigation of KDM4A and its targets as a potential therapeutic vulnerability in AML.

scholarly journals Cytotoxic Compounds Derived from Marine Sponges. A Review (2010–2012)

Molecules ◽  
2017 ◽  
Vol 22 (2) ◽  
pp. 208 ◽  
Author(s):  
Roberto Mioso ◽  
Francisco Marante ◽  
Ranilson Bezerra ◽  
Flávio Borges ◽  
Bárbara Santos ◽  
...  
Keyword(s):  
Marine Sponges ◽  
Cytotoxic Compounds

scholarly journals CYTOTOXIC BIOACTIVE COMPOUNDS FROM CALOTROPIS GIGANTEA STEM BARK

2016 ◽  
Vol 8 (9) ◽  
pp. 111
Author(s):  
Kartini Hasballah ◽  
Murniana . ◽  
Erya . ◽  
Ardian .
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Ethyl Acetate Extract ◽  
Leukemia Cell ◽  
Stem Bark ◽  
Hexane Extract ◽  
Leukemia Cell Line ◽  
Calotropis Gigantea ◽  
Murine Leukemia Cell ◽  
Main Components

<p><strong>Objective: </strong>The present study deals with the cytotoxic activity of n-hexane and ethyl acetate extracts of <em>Calotropis gigantea</em> L. stem bark and its fractions such as A, B, C, D and E fractions on murine leukemia cell line P388.</p><p><strong>Methods: </strong>The crude extracts of <em>C. gigantea</em> stem bark were prepared using n-hexane and ethyl acetate solvents. The plant extracts were subjected to vacuum liquid chromatography followed by TLC. According to the similarity of stain patterns, the fractions were combined. The extracts and its combined fractions were then subjected for the phytochemical test. Cytotoxic activity of those extracts and its combined fractions were tested using MTT assay. Fraction D was subjected to gravity column chromatography followed by TLC. Then, fractions A, B, and D2 were crystallized and subjected to GC-MS.</p><p><strong>Results: </strong>The qualitative screening of n-hexane extract of <em>Calotropis gigantea</em> L. stem bark for secondary metabolites showed the presence of terpenoid, flavonoids, phenolics and coumarins. While the ethyl acetate extract contained phenolics, steroids, flavonoids, saponins and coumarins compounds. IC<sub>50 </sub>values for n-hexane extract and E fraction are 76.29 µg/ml and 18.48 µg/ml, respectively. In the ethyl acetate extract and C fraction obtained IC<sub>50</sub> values 57.05 µg/ml and 52.58 µg/ml.</p><p><strong>Conclusion: </strong>Cytotoxic activity from E fraction of n-hexane extract of <em>C. gigantea</em> stem bark is the most potent and containing flavonoids, phenolics and coumarins. The main components from several compounds of n-hexane extract of <em>C. gigantea</em> are germacrane-A, (-)-globulol, urs-12-ene and veridiflorol. </p>

Review: Highly Selective Compounds for the Antibody-Directed Enzyme Prodrug Therapy of Cancer

2003 ◽  
Vol 56 (9) ◽  
pp. 841 ◽  
Author(s):  
Lutz F. Tietze ◽  
Tim Feuerstein
Keyword(s):  
Monoclonal Antibody ◽  
Malignant Cells ◽  
High Potency ◽  
Selective Treatment ◽  
Enzyme Prodrug Therapy ◽  
Ic50 Value ◽  
Tumour Associated Antigens ◽  
Cytotoxic Compounds

Antibody-directed enzyme prodrug therapy (ADEPT) is a recent development for a selective treatment of cancer, based on site-directed formation at the surface of malignant cells of cytotoxic compounds from non-toxic prodrugs with a conjugate of an appropriate enzyme and a monoclonal antibody which binds to tumour-associated antigens. New potent prodrugs of analogues of the antibiotic CC-1065 have been developed. These show a remarkable selectivity with a Q(IC50) value of up to more than 3000. Moreover, the formed drug has a high potency with an IC50 of 30 pM.

scholarly journals Terpenoids from the Deep-Sea-Derived Fungus Penicillium thomii YPGA3 and Their Bioactivities

Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 164 ◽  
Author(s):  
Zhongbin Cheng ◽  
Wan Liu ◽  
Runzhu Fan ◽  
Shouye Han ◽  
Yuanli Li ◽  
...  
Keyword(s):  
Deep Sea ◽  
Chemical Study ◽  
Positive Control ◽  
Hydroxyl Group ◽  
Etoac Extract ◽  
The Third ◽  
Ic50 Value ◽  
Ic50 Values ◽  
New Compounds ◽  
First Time

A chemical study of the ethyl acetate (EtOAc) extract from the deep-sea-derived fungus Penicillium thomii YPGA3 led to the isolation of a new austalide meroterpenoid (1) and seven known analogues (2−8), two new labdane-type diterpenoids (9 and 10) and a known derivative (11). The structures of new compounds 1, 9, and 10 were determined by comprehensive analyses via nuclear magnetic resonance (NMR) and mass spectroscopy (MS) data. The absolute configurations of 1, 9, and 10 were determined by comparisons of experimental electronic circular dichroism (ECD) with the calculated ECD spectra. Compound 1 represented the third example of austalides bearing a hydroxyl group at C-5 instead of the conserved methoxy in other known analogues. To our knowledge, diterpenoids belonging to the labdane-type were discovered from species of Penicillium for the first time. Compound 1 showed cytotoxicity toward MDA-MB-468 cells with an IC50 value of 38.9 μM. Compounds 2 and 11 exhibited inhibition against α-glucosidase with IC50 values of 910 and 525 μM, respectively, being more active than the positive control acarbose (1.33 mM).

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