Indonesian Journal of Cancer Chemoprevention
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Anti-Inflammatory Activity of The Extract of Guava Leaves (Psidium guajava L) in The Rat (Rattus norvegicus L)
Get PDFUsing of natural sources that have anti-inflammatory activity for the prevention and treatment of degenerative diseases began to be further explored. An investigation on the anti-inflammatory activity of the aqueous extract of guava leaves (Psidium guajava L.) from Sawangan, Depok on white male rats of Sprague-Dawley strain had been carried out on the carrageenan-induced paw edema method. To examine the effect of guava extract on subcutan at different doses of 125, 250 and 500 mg/kg of body weight (BW). Indometacine at dose of 10 mg/kg BW was used as a positive control. Observations were made during five hours with an interval of one hour. These results demonstrate that the percentage of inflammation or edema (% E) optimal at the 4th hour and then decreased at the 5th hour, while the percentage of optimal inhibition occurred at the 5th hour. Guava extract at 125, 250 and 500 mg/kg BW reduced inhibitory percentage activities by 40.81, 55.45 and 43.61% (p< 0.05) respectively. In conclusion, this study suggests that guava extract has anti-inflammatory properties by decreasing edema level.Keywords: Anti-inflammatory, guava leaves, edema
Molecular Docking of Robustaflavone Derivatives on Pi3k Protein Target and The Correlation With Its Cytotoxic Activity on Cancer Cells
Get PDFRobustaflavone derivatives have cytotoxic effect on cancer cell. Inhibition of PI3K on cancer cell has correlation with apoptotic induction. The aim of this research is to observe interaction from robustaflavone derivatives on PI3K receptor that may give contribution to the cytotoxic effect of the compounds on cancer cell line. Geometric optimization of robustaflavone derivatives structured was done used Hyperchem 7.5 software. Arguslab 4.01 software with GAdock method applied for the docking step. The docking result showed that robustaflavone 7,4',7''- trimethyl ether (RTE) has affinity on PI3K target receptor which gave the lowest Gibbs free energy (∆G -10,855 kcal/mol).Keywords: robustaflavone, PI3K, cancer, dockin
In Vitro Anti-Cancer Alkaloid and Flavonoid Extracted from the Erythrina variegata (Leguminoseae) Plant
Get PDFErythrina plants, locally known as “dadap ayam”, are higher plant species and have been used as a folk medicine for treatment of cancer. To prove the effectiveness of the leaves and stem bark of E. variegata as an anti-cancer agent, the assay in this research was focused on in vitro test towards breast cancer cell T47D. In the course of our continuing search for novel anti-cancer agent from Erythrina plants, the methanol extract of the leaves and stem bark of E. variegata showed significant anti-cancer activity against breast cancer cell T47D in vitro using the Sulphorhodamine B (SRB) assay. By using the anti-cancer activity to follow the separations, the methanol extract was separated by combination of column chromatography. The chemical structure of an anti-cancer compounds were determined on the basis of spectroscopic evidence and comparison with the previously reported and identified as an erythrina alkaloid (1) and isoflavonoid (2). Compounds (1-2) showed anti-cancer activity against breast cancer cell T47D used with IC50 of 1.0 and 3.3 µg/mL, respectively. This results strongly suggested that E. variegata is promising sources for anti-cancer agents. Keywords: Anti-cancer, Erythrina variegata, Leguminosea
Molecular Docking of Lunacridine from Lunasia amara to DNA : Its Inhibition And Interaction Study Correlated With The Cytotoxic Activity on P388 Murine Leukemia Cells
Get PDFDNA Topoisomerase II inhibitors are a type of anticancer drugs. These drugs perform their biological activity either by forming a DNA-intercalator-topoisomerase II ternary complex or by inhibiting other enzymes and/or transcription factors that act on DNA. The strong interactions with DNA play a crucial role for their pharmacological properties. Lunacridine, the active principle from Lunasia amara, was known as DNA intercalating Topoisomerase II inhibitor. With the aims to explore the affinity and molecular interaction of lunacridine compound isolated from Lunasia amara with DNA, molecular docking study has been carried out with DNA model using Autodock 4.0 software. Cytotoxicity test on P388 murine leukemia cells was done also using 100, 30, 10, 3 and 1 μg/ml series of lunacridine concentration. The docking result shows that Lunacridine itself could to dock intercalatively between base pairs of DNA and the possibility interaction with adenine, thymine and cytosine by dipole-dipole interaction. The lowest predicted binding energy of lunacridine is –6,22 kcal/mol, whereas original ligand bis thiazole is -16,37 kcal/mol. Lunacridine compound itself has less cytotoxic activity on P388 murine leukemia cells with the IC50 value of 39,52 μg/ml or 129,41 μM. The binding energy of lunacridine on DNA higher than original ligand show that the interaction of lunacridine with DNA is not stable afford the less cytotoxic activity. However, based on the IC50 value, lunacridine could be depeloved as anticancer.Key words: docking, lunacridine, Lunasia amara, cytotoxic, P388 murine leukimia cells
The Effect of Addition of Antioxidant to The Stability of Green Tea Water Extract As Anti Acne
Get PDFThere are so many potential effects that green tea, such as antibacterial activity against Propionibacterium acnes, that caused acne. In the previous study, green tea had been made in gel. In this study, formula of green tea water extract gel is developed with addition of antioxidant so that stability of the gel would increase. Gel of green tea water extract were made using Carbopol 940 with glycerin as the solvent. The chosen antioxidant was sodium sulfite. It is also combined with chelating agent, EDTA (Edetic Acid). The activity of green tea water extract gel was determined and tetracycline HCl gel was used as the reference. The addition of sodium sulfite 1% w/w into gel with Carbopol 940 1% w/w as the base prevent the change of color in more than eight weeks. Minimum Inhibitory Concentration (MIC) of green tea water extract without either sodium sulfite or EDTA was 1.20 ± 0.11 cm against Propionibacterium acne. MIC of green tea water extract with addition of sodium sulfite 1% w/w was 1.19 ± 0.28 cm. MIC of green tea water extract with addition of sodium sulfite 1% w/w and EDTA 0.1% w/w was 1.25 ± 0.22 cm. The addition of sodium sulfite 1% w/w caused viscosity of gel decrease 42.1%. The addition of sodium sulfite 1% w/w increased the color stability of green tea water extract. The addition of sodium sulfite 1% w/w didn’t decrease its antibacterial activity against Propionibacterium acnes.Keywords: green tea, anti acne, Propionibacterium acnes, gel, antioxidan
Secretion of Indoleamine 2,3-Dioxygenase, an Immunomodulatory Substance, by Adipose-Derived Mesenchymal Stem Cell
Get PDFLipoaspirate, a wasted by product from liposuction procedure recently has been shown to contain abundant adipose-derived-mesenchymal stem cells (MSCs). Mesenchymal stem cells (MSCs) have been studied in many research areas to regenerate many cell lineages. In addition, MSCs have immunomodulatory effect. This capability has been utilized in several clinical studies in hematopoetic stem cell and organ transplantation as a strategy to reduce the risk of Graft versus Host Disease (GvHD). It has been reported that the ‘stimulated’ MSC is able to secrete substances to suppress tissue rejection. One of the substances was known to be indoleamine 2,3-dioxygenase (IDO). A previous study has characterized the secretion of IDO by bone marrow-derived MSCs stimulated by an inflammatory mediator interferon gamma (IFN-γ). IDO has been detected using Western blot analysis and by High Performance Liquid Chromatography (HPLC) assay. The aim of this study was to detect the presence of IDO in AD-MSCs culture with and without INFγ stimulation. Our study showed that AD-MSC stimulated with IFN-γ significantly secreted high level of IDO as detected by Enzyme-Linked Immuno Sorbent Assay (ELISA). Despite its property as a proinflammatory mediator, IFN-γ has shown to be able to induce IDO secretion in MSC culture which suggests the immuno modulatory effect of MSC. This study clearly demonstrates the potential application of adipose-derived MSC in the immunomodulatory strategy for allogenic transplantation. Keyword : mesenchymal stem cell, indoleamine 2,3-dioxygenase, IFN-
Antioxidant Activity Test of 2,6-bis-(2’-furilidyn)-Cyclohexanone, ; 2,5-bis-(2’-furilidyn)-Cyclopentanone; 1,5-Difuryl-1,4-pentadien-3-one
Get PDFAntioxidant is an essential compound to keep man’s health due to its function as radical scavenging. Curcumin analog compounds can function as antioxidant (Sardjiman, 2000). The aim of the experiment was to find out the antioxidant activity of 2,.6-bis-(2’-furilidin)-cyclohexanone, 2,.5-bis-(2’furilidin)-cyclopentanone, and 1,.5-difuril-1.4-pentadien-3-one compounds, and the antioxidant activity of each compound against DPPH radical with IC50 parameter as well as the correlation of compounds structure’s activities against antioxidant. The antioxidant activity of curcumin analog compounds wereas tested against DPPH free radical. The test was conducted in 5 series of concentrations by adding 4.0 ml test solutions with 1.0 ml DPPH. The antioxidant activity against free radical was measured usingwith spectrophotometer at 517 nm wavelength and determined for the IC50 value. The experiment employed rutin as positive control. The result of the experiment showed that curcumin analog compounds have antioxidant activity with IC50 of rutin, 2,.6-bis-(2’-furilidin)-cyclohexanone, 2,.5-bis-(2’furilidin)-cyclopentanone, and 1,.5-difuril-1.4-pentadien-3-one as follows: 4.93 ppm, 22.73 ppm, 20.67 ppm, and 18.80 ppm respectively. The highest antioxidant activity belonged to 1,.5-difuril-1.4-pentadien-3-one compound which is 18.80 ppm . Correlation of activity structure of the 3 compounds can be seen from the log p parameter and energy space of HOMO-LUMO.Key words: Antioxidant, DPPH, Analog Curcumi
Cyclosporine A and FK506 as Potent Inhibitors of Streptococcus intermedius Intermedilysin-Induced NFAT-1 Activation
Get PDFCyclosporine A (CsA) and tacrolimus (FK506), a member of calcineurin inhibitors, inhibit inflammation process as part of immune response. Nuclear activated T cells subfamily NFAT1 is a trascription factor responsible for the regulation of immune response genes. Streptococcus intermedius, an oral commensal bacterium, has been shown to strongly associate with liver abscess. The S. intermedius strains produce intermedilysin (ILY), which is responsible for the bacterial virulence. Cyclosporine A and FK506 have been widely used to control NFAT activation in most of cell types, however the ability of CsA and FK506 to inhibit ILY-induced NFAT1 activation remains to be investigated. The aim of this study was to investigate the effect of CsA and FK506 on NFAT1 activation caused by ILY. Human cholangiocellular cell line HuCCT1 was stimulated with various concentrations of ILY. The cell and nuclear morphological change was observed by microscopy analysis. The NFAT1 nuclear translocation that indicates its activation was detected by immunocytochemistry. The inhibitory effect of CsA and FK506 was tested after 30 min application before ILY treatment by using immunofluorescence microscope. The results showed cell and nuclear shrinkage in ILY-treated cells. The NFAT1 was translocated to the nuclei in HuCCT1 cells, and observed in dose dependent manner. Cyclosporine A and FK506 inhibited ILY-induced NFAT1 nuclear translocation. In conclusion, CsA and FK506 may act as potent inflammation control agents in S. intermedius ILY-infected cells.Keywords: Cyclosporine A, FK506, NFAT1, intermedilysi
Curcumin and Extract of Plantago major, L Increased SPF Value of Cold Cream Base
Get PDFOctyl methoxycinnamate as the active material of the sunscreen would be degradated after being exposed to the sunlight. Curcumin, rice flour and the extract of Plantago major, L was the material that could function as the sunscreen. The aim of this research was to know the SPF value and the physical characteristics of cream of the sunscreen with the active material octyl methoxycinnamate after the addition of the optimum composition of curcumin and the extract of Plantago major, L and the optimum composition of rice flour and the extract of Plantago major, L.In this research three formulas was examined, i.e. the formula I with the active material octyl methoxycinnamate, the formula II with the active material octyl methoxycinnamate and the optimum composition curcumin and the extract of Plantago major, L, Formula III with the active material octyl methoxycinnamate and the optimum composition rice flour and the extract of Plantago major, L. SPF value of each formula was determined by using the Petro method (1981) using UV spectrofotometric method at a l 290 nm-320 nm. The physical characteristics i.e. the power spread, the adhesiveness and the viscosity were also examined analysed with Anova one way at a confidence level 95%. Result of the research show that SPF value increased after the addition of the optimum composition of curcumin and the extract of Plantago major, L. The physical characteristics of cream of the sunscreen do not change after the addition of the optimum composition curcumin and the extract of Plantago major, L and the optimum composition rice flour and the extract of Plantago major, L.Key words: Octyl methoxycinnamate,curcumin,flour rice,extract of Plantago major, L,sunscree
Structure Modification of Ethyl p-methoxycinnamate Isolated from Kaempferia galanga Linn. and Citotoxicity Assay of The Products on WiDr Cells
Get PDFEthyl p-methoxycinnamate, major ingredient of Kaempferia galanga rhizome, have been reported not only has analgesic – anti inflammatory activities like NSAIDs which inhibited cyclooxygenase, but also inhibit tumor cell proliferation in specimen of mouse epidermis. Therefore, it will be interesting to carry out synthetic studies on the derivates of ethyl p-methoxycinnamate and searching their citotoxic activity on WiDr cell. We wish to report of structure modification on carboxyl moiety of ethyl p-methoxycinnamate and evaluation on their citotoxic activity on WiDr cell. Isolation of ethyl p-methoxycinnamate from Kaempferia galanga rhizome was carried out by percolation with ethanol 96% as solvent. Hydrolysis of ethyl p-methoxycinnamate in basic condition was performed to obtain p-methoxycinnamic acid. Preparation of some thiourea derivates of ethyl p-methoxycinnamate was carried out by microwave irradiation. Citotoxicity assay was carried out by MTT method for 48 h.Modification of carboxyl group of ethyl p-methoxycinnamate to its thiourea form could be carried out by microwave irradiation gave; (E)-3-(4-methoxyphenyl)-N-(phenylcarba- mothioyl)acrylamide (50%); (E)-3-(4-methoxyphenyl)-N-(4-methoxyphenylcarbamothi- oyl)acrylamide (26%) and (E)-3-(4-methoxyphenyl)-N-(4-methylphenylcarbamothioyl) acrylamide (54%), yield calculated for 2 step from the acid chloride. All compounds showed no citotoxic effect on WiDr cell at 48 h incubation.Keywords : ethyl p-methoxycinnamate, microwave irradiation, Kaempferia galanga, citotoxicity, WiDr cel