Anticancer Potential of Flavonoids: An Overview with an Emphasis on Tangeretin.

Natural compounds with pharmacological activity, flavonoids have been the subject of an exponential increase in studies in the field of scientific research focused on therapeutic purposes due to their bioactive properties, such as antioxidant, anti-inflammatory, anti-aging, antibacterial, antiviral, neuroprotective, radioprotective, and antitumor activities. The biological potential of flavonoids, added to their bioavailability, cost-effectiveness, and minimal side effects, direct them as promising cytotoxic anticancer compounds in the optimization of therapies and the search for new drugs in the treatment of cancer, since some extensively antineoplastic therapeutic approaches have become less effective due to tumor resistance to drugs commonly used in chemotherapy. In this review, we emphasize the antitumor properties of tangeretin, a flavonoid found in citrus fruits that has shown activity against some hallmarks of cancer in several types of cancerous cell lines, such as antiproliferative, apoptotic, anti-inflammatory, anti-metastatic, anti-angiogenic, antioxidant, regulatory expression of tumor-suppressor genes, and epigenetic modulation.

Chemical composition and anti-proliferative activity of essential oils from some medicinal plants from Cachicadán, Región La Libertad, Perú.

This study evaluated the chemical composition and anti-proliferative activity of essential oils (EOs) obtained by hydrodistillation from seven medicinal plants from Cachicadán, La Libertad Región, Perú. Limonene (0.64 to 44.43%) and linalool (0.36 to 2.12%) were identified in all EOs by gas chromatography coupled to mass spectrometry analysis. The major components (relative intensity ≥ 10%) were cis-dihydro carvone, carvone, and cis-piperitone epoxide for Minthostachys mollis leaves; ß-pinene, limonene, and ledol for Lepechinia heteromorpha leaves; limonene, neral, and geranial for Aloysia citriodora, both leaves and flowers; α-pinene, and limonene for Myrcianthes myrsinoides leaves; and α-pinene, ß-myrcene, and (E)-ß-Ocimene for Dalea carthagenensis leaves. Constituted by (Z)-ß-ocimene, dihydrotagetone, (Z)-tagetone, and car-3-en-2-one, EO of Tagetes minuta leaves induced an irreversible cytostatic effect against MCF-7 human breast tumor cells. Further in vivo studies must be carried out to establish the safe and efficient dose of T. minuta EO as adjuvant treatment in oncological therapies.

Silver nanoparticles induce a non-immunogenic tumor cell death.

Immunogenic cell death (ICD) is a form of cell death characterized by the release of danger signals required to trigger an adaptive immune response against tumor-associated antigens. Silver nanoparticles (AgNP) display anti-proliferative and cytotoxic effects in tumor cells, but it has not been previously studied whether AgNP act as an ICD inductor. The present study evaluated the in vitro release of calreticulin as a damage-associated molecular pattern (DAMP) associated with the cytotoxicity of AgNP and their in vivo anti-cancer effects. In vitro, mouse CT26 colon carcinoma and MCA205 fibrosarcoma cells were exposed to AgNP and then cell proliferation, adhesion, and release of calreticulin were determined. The results indicated there were time- and concentration-related anti-proliferative effects of AgNP in both the CT26 and MCA205 lines. Concurrently, changes in cell adhesion were detected mainly in the CT26 cells. Regarding DAMP detection, a significant increase in calreticulin was observed only in CT26 cells treated with doxorubicin and AgNP; however, no differences were found in the MCA205 cells. In vivo, the survival and growth of subcutaneous tumors were monitored after vaccination of mice with cell debris from tumor cells treated with AgNP or after intra-tumoral administration of AgNP to established tumors. Consequently, anti-tumoral prophylactic immunization with AgNP-dead cells failed to protect mice from tumor re-challenge; intra-tumor injection of AgNP did not induce a significant effect. In conclusion, there was a noticeable anti-tumoral effect of AgNP in vitro in both CT26 and MCA205 cell lines, accompanied by the release of calreticulin in CT26 cells. In vivo, immunization with cell debris derived from AgNP-treated tumor cells failed to induce a protective immune response in the cancer model mice. Clearly, further research is needed to determine if one could combine AgNP with other ICD inducers to improve the anti-tumor effect of these nanoparticles in vivo.

Bioactive Activities of the Phenolic Extract from Sterile Bracts of Araucaria angustifolia.

Sterile bracts can represent 80% of Araucaria angustifolia pinecone and are a rich source of phenolic compounds. This study aimed to optimize the extraction of the phenolic compounds from Araucaria angustifolia bracts using response surface methodology; the bioactivity properties were also investigated. The effects of the ethanol concentration, solute/solvent ratio, and temperature in relation to the phenolic composition and antioxidant activity were evaluated. The quantification and identification of the individual phenolic compounds (using high-performance liquid chromatography) and their bioactivity were evaluated. The optimized extraction conditions, which detected gallic acid, catechin, epicatechin, quercetin, and kaempferol, were obtained using 60% ethanol at a ratio of 1:38 (w/v) and a temperature of 80 °C. The extract showed high levels of phenolic classes and antioxidant activity. The extract also showed an inhibitory activity for pathogenic (approximately 80%, 10,000 µg/mL) and lactic acid (27.9%, 15,000 µg/mL) bacteria strains. The α-glucosidase inhibitory activity was approximately ten times greater than acarbose, demonstrating its high antiglycemic potential. No antioxidant and anti-inflammatory cellular activity were determined; however, a high cytotoxicity for non-tumor cells and the antiproliferative activity against the tumor cells were observed. Overall, the phenolic extract showed promising action in relation to the fight against the diseases related to oxidative stress and, hopefully, the application of the safe concentrations of the extract, based on bioavailability assays, can be verified.

Mentha aquatica L. aerial parts: in vitro anti-proliferative evaluation on human tumour and non-tumour cell lines.

Bearing in mind the several medicinal properties of Mentha genus, this work aimed to evaluate the anti-proliferative potential of the ethanolic extract (EE) and fractions from M. aquatica L aerial parts. Using the anti-proliferative protocol developed by the NCI/USA, four fractions (F2 - F4 and F6) obtained from EE showed promising anti-proliferative profile against a panel of human tumor and non-tumor cell lines. After 24-h exposure, F2 (0.25 µg/mL) showed potent and irreversible anti-proliferative effect without inducing cell cycle arrest in both NCI-H460 and MCF-7 cells, without (anti) estrogenic activity. These effects were lost after storage of F2 diluted in dimethyl sulfoxide at -80 °C during 2 weeks. Analysis by gas chromatography coupled to mass detection evidenced some chemical changes induced by F2 storage in solution. The present study demonstrated the anti-proliferative effect of M. aquatica. Further studies are necessary to determine better storage conditions to enhance F2 stability.

Recent Trends in Drug Development for the Treatment of Adenocarcinoma Breast Cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds.

Thiazoles, triazoles, and thiosemicarbazones function as efficient scaffolds in compounds for the treatment of several illnesses, including cancers. In this review article, we have demonstrated various studies involving these three pharmacophore classes (thiazoles, triazoles, and thiosemicarbazones) in medicinal chemistry over the last decade (2011-2021) with a focus on MCF-7 adenocarcinoma breast cancer cells. Our objective is to facilitate drug discovery of novel chemotherapeutic agents by detailing anti-proliferative compounds.

Evaluation of some in vitro bioactivities of sunflower phenolic compounds.

Phenolic compounds in crude extracts were obtained from defatted sunflower seed flour using sodium bisulfite and ethanol solutions as extracting agents. The antioxidant, antimicrobial, anti-proliferative, and DNA protective activities of the phenolic compounds in crude extract were analyzed. The phenolic compound contents were determined as chlorogenic acid (CGA) equivalent, presenting 11.57 and 15.44 g CGA eq/100g regarding the sodium bisulfite extract and ethanolic extract, respectively. The ORAC, DPPH, and ABTS methods were used to evaluate antioxidant activity. Both extracts presented antioxidant properties, considering that the ethanolic extract demonstrated higher values (EC50 0.36 g extract/g DPPH•). The antimicrobial action was analyzed as to the minimal inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC) of 4 kinds of bacteria (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis). The ethanolic extract was effective against all of these microorganisms, out of which E. coli was the most sensitive, with a MIC of 11.6 mg CGA/mL. The ethanolic extract presented DNA protective activity without cytotoxic activity concerning in vitro anti-proliferative assay. These findings can be considered as initial evidence of the potential use of phenolic compounds obtained from sunflower seed flour as natural additives in the food industry.

Polyphenolic Flavonoid Compound Quercetin Effects in the Treatment of Acute Myeloid Leukemia and Myelodysplastic Syndromes.

Flavonoids are ubiquitous groups of polyphenolic compounds present in most natural products and plants. These substances have been shown to have promising chemopreventive and chemotherapeutic properties with multiple target interactions and multiple pathway regulations against various human cancers. Polyphenolic flavonoid compounds can block the initiation or reverse the promotion stage of multistep carcinogenesis. Quercetin is one of the most abundant flavonoids found in fruits and vegetables and has been shown to have multiple properties capable of reducing cell growth in cancer cells. Acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) therapy remains a challenge for hematologists worldwide, and the outcomes for patients with both disorders continue to be poor. This scenario indicates the increasing demand for innovative drugs and rational combinative therapies. Herein, we discuss the multitarget effects of the flavonoid quercetin, a naturally occurring flavonol, on AML and MDS.

Metabolite Profiling of Rosemary Cell Lines with Antiproliferative Potential against Human HT-29 Colon Cancer Cells.

Rosemary (Rosmarinus officinalis) is a culinary and medicinal plant used in food and pharmaceutical industry. The wide range of biological activities is mainly related to phenolic and terpenic compounds; like carnosic acid (CA), carnosol (CS) and rosmarinic acid (RA), mainly reported in rosemary leaf extracts, and recently described in rosemary callus extracts. The aim of this work was to investigate the chemical profile of rosemary cell lines and evaluate their antiproliferative potential against human HT-29 colorectal cancer cell lines. For this purpose, rosemary leaf explants were dedifferentiated on MS medium and added with 2, 4-D (2, 4-dichlorophenoxyacetic acid; 2 mg/L) and BAP (6-benzylaminopurine; 2 mg/L). Cell aggregates were separated according to colour and three rosemary cell lines cultures were established: green (RoG), yellow (RoY) and white (RoW). The chemical profile of rosemary cell lines extracts was characterized by combining HPLC and GC platforms coupled to HR-MS/MS. The antiproliferative activity against HT-29 cell line was analyzed with MTT assay. A total of 71 compounds, including hydroxycinnamic acid and hydroxybenzoic acid derivatives, flavonoids, phenolic di- and triterpenes, as well as relevant unsaturated fatty acids and their esters, phytosterols, and carotenoids were tentatively identified in the extract of the target cell lines. The antiproliferative activity test against HT-29 cell using the MTT assay revealed that the viability of HT-29 colon cancer cells was affected after treatment with the RoW extract (IC50 of 49.63 µg/mL) at 48 h. These results showed that rosemary cell lines can also accumulate other bioactive phytochemicals with demonstrated antiproliferative potential.

Bioactive compounds from Octopus vulgaris ink extracts exerted anti-proliferative and anti-inflammatory effects in vitro.

Underutilized marine food products such as cephalopods' ink could be sources of bioactive compounds providing health benefits. This study aimed to assess the anti-proliferative and anti-inflammatory effects from Octopus vulgaris ink extracts (hexane-, ethyl acetate-, dichloromethane- (DM), and water extracts) using human colorectal (HT-29/HCT116) and breast (MDA-MB-231) cancer cells, and LPS-challenged murine RAW 264.7 cells. Except by ethyl-acetate, all of the extracts exhibited anti-proliferative effects without being cytotoxic to ARPE-19 and RAW 264.7 cells. Among DM fractions (F1/F2/F3), DM-F2 showed the highest anti-proliferative effect (LC50 = 52.64 µg/mL), inducing pro-apoptotic morphological disruptions in HCT116 cells. On RAW 264.7 cells, DM-F2 displayed the lowest nitrites reduction and up-regulation of key-cytokines from the JAK-STAT, PI3K-Akt, and IL-17 pathways. Compared to control, DM-F2 increased IL-4 and decreased NF-κB fluorometric expression in peripheral blood mononuclear cells (PBMCs). Metabolomic analysis of DM-F2 highlighted hexadecanoic acid and 1-(15-methyl-1-oxohexadecyl)-pyrrolidine as the most important metabolites. These compounds also exhibited high in silico binding affinity (-4.6 to -5.8 kcal/mol) to IL-1α, IL-1ß, and IL-2. Results suggested the joint immuno-modulatory and anti-proliferative effect derived from selected compounds of underutilized marine food products such as ink. This is the first report of such biological activities in extracts from O. vulgaris ink.

Molecular modeling and LC-MS-based metabolomics of a glutamine-valproic acid (Gln-VPA) derivative on HeLa cells.

Glutaminase plays an important role in carcinogenesis and cancer cell growth. This biological target is interesting against cancer cells. Therefore, in this work, in silico [docking and molecular dynamics (MD) simulations] and in vitro methods (antiproliferative and LC-MS metabolomics) were employed to assay a hybrid compound derived from glutamine and valproic acid (Gln-VPA), which was compared with 6-diazo-5-oxo-L-norleucine (DON, a glutaminase inhibitor) and VPA (contained in Gln-VPA structure). Docking results from some snapshots retrieved from MD simulations show that glutaminase recognized Gln-VPA and DON. Additionally, Gln-VPA showed antiproliferative effects in HeLa cells and inhibited glutaminase activity. Finally, the LC-MS-based metabolomics studies on HeLa cells treated with either Gln-VPA (IC60 = 8 mM) or DON (IC50 = 3.5 mM) show different metabolomics behaviors, suggesting that they modulate different biological targets of the cell death mechanism. In conclusion, Gln-VPA is capable of interfering with more than one pharmacological target of cancer, making it an interesting drug that can be used to avoid multitherapy of classic anticancer drugs.

Antiproliferative potential of 3ß,5α,6ß,7α-tetrahydroxyergosta-8(14),22-diene produced by Acremonium persicinum isolated from an alkaline crater lake in Puebla, Mexico.

The sterol 3ß,5α,6ß,7α-tetrahydroxyergosta-8(14),22-diene was obtained from bio-guided fractioning of the chloroform extract of 50 L of liquid culture of Acremonium persicinum. This fungal strain was selected because of its anti-proliferative activity against solid human tumour cell lines (GI50 ≤ 50 µg/mL) in a bio-prospective study of fungi isolated from plant material, sediment and water samples obtained from alkaline lakes Alchichica and Atexcac in Puebla, Mexico. This compound showed GI50 (µM) values of: 16, 24, 18, 15 and 12 against tumour cell lines A-549, HBL-100, HeLa, T-47D and WiDr respectively. GI50 effects against tumour lines T-47D and WiDr were found to be greater than the clinically used drugs Etoposide and Cisplatin. Because of this, the results obtained support the pharmacological importance of the microorganisms that develop in these ecosystems and strengthen the non-invasive bio-prospection studies that our work group has developed in recent years.

Anti-proliferative or Cytopathic Potential of Thapsia garganica, Citrus sinensis, Citrus limon and Vinca rosea Extracts Against Human Embryonic Kidney Carcinoma Cell Line

ABSTRACT Objective: Developing anti-cancer drugs from natural products is receiving increasing interest worldwide due to limitations and side effects of anti-cancer drugs. The purpose of this study was to explore the anti-proliferative or cytopathic potential of natural compounds derived from plant sources as alternatives of synthetic compounds on human embryonic kidney carcinoma (HEK) cell line. Methods: In this study, aqueous and methanolic extracts were obtained from various plants, viz, Thapsia garganica, Citrus sinesis, Citrus limon and Vinca rosea. Extracts were serially diluted into 96-well microtitre plates and were screened for anti-proliferative potential against the HEK cell line via the neutral red dye uptake assay. Results: The findings revealed that methanolic extracts of T. garganica leaf and V. rosea leaf were the most effective as anti-proliferative or cytotoxic against the HEK cell line, with IC50 at 32-fold dilution of the extract. Conclusion: The extracts of T. garganic and V, rosea have been used as anti-proliferative drugs but after trial in experimental animals for being not toxic.

Phytochemical analysis and in vitro anti-proliferative activity of Viscum album ethanolic extracts.

BACKGROUND: Viscum album L. (Santalaceae), commonly known as mistletoe, is a hemiparasitic plant traditionally used in complementary cancer treatment. Its antitumor potential is mostly attributed to the presence of aqueous soluble metabolites; however, the use of ethanol as solvent also permits the extraction of pharmacological compounds with antitumor potential. The clinical efficacy of mistletoe therapy inspired the present work, which focuses on ethanolic extracts (V. album "mother tinctures", MT) prepared from different host trees. METHODS: Samples from three European subspecies (album, austriacum, and abietis) were harvested, and five different V. album-MT strains were prepared. The following phytochemical analyses were performed: thin layer chromatography (TLC), high-performance liquid chromatography (HPLC) and liquid chromatography-high resolution mass spectrometry (LC-HRMS). The proliferation assay was performed with WST-1 after incubation of tumor (Yoshida and Molt-4) and fibroblast cell lines (NIH/3 T3) with different MT concentrations (0.5 to 0.05% v/v). The cell death mechanism was investigated by flow cytometry (FACS) using Annexin V-7AAD. RESULTS: Chemical analyses of MT showed the presence of phenolic acids, flavonoids and lignans. The MT flavonoid and viscotoxin contents (mg/g fresh weight) were highest in Quercus robur (9.67 ± 0.85 mg/g) and Malus domestica (3.95 ± 0.58 mg/mg), respectively. The viscotoxin isoform proportions (% total) were also different among the VA subspecies with a higher content of A3 in V. album growing on Abies alba (60.57 ± 2.13). The phytochemical compounds as well as the viscotoxin contents are probably related to the antitumor effects of MT. The cell death mechanisms evaluated by colorimetric and FACS methodologies involved necrotic damage, which was host tree-, time- and dose- dependent, with different selectivity to tumor cells. Mother tincture from V. album ssp. abietis was the most effective at inducing in vitro cellular effects, even when incubated at the smallest concentration tested, probably because of the higher content of VT A3. CONCLUSION: Our results indicate the promising antitumor potential of Viscum album ethanolic extracts and the importance of botanical and phytochemical characterization for in vitro anti-proliferative effects.

Immunosuppression in Kidney Transplantation: State of the Art and Current Protocols.

Currently, kidney transplantation is the best treatment option for kidney failure for a majority of eligible patients. It is associated with a better quality of life and reduced mortality as compared to staying on dialysis. Many of the improvements in kidney transplant outcomes, observed in recent decades, are due to more efficient immunosuppression strategies. Therefore, developing expertise in the management of immunosuppressive drugs is key to the success of kidney transplantation. In this review, the historical aspects of organ transplant immunosuppression are briefly addressed and the basis of the allograft immune response to contextualize the main topic is provided, which is a deeper view of the immunosuppressive agents, including their known mechanisms of action, pharmacokinetics, interactions, toxicities, and clinical use. The most commonly used immunosuppressive protocols employed based on patients' and donors' characteristics are also presented here.

Anti-Estrogenic Activity of Guajadial Fraction, from Guava Leaves (Psidium guajava L.).

The research of natural products has allowed for the discovery of biologically relevant compounds inspired by plant secondary metabolites, which contributes to the development of many chemotherapeutic drugs used in cancer treatment. Psidium guajava leaves present a diverse phytochemical composition including flavonoids, phenolics, meroterpenoids, and triterpenes as the major bioactive constituents. Guajadial, a caryophyllene-based meroterpenoid, has been studied for potential anticancer effects tested in tumor cells and animal experimental models. Moreover, guajadial has been reported to have a mechanism of action similar to tamoxifen, suggesting this compound as a promisor phytoestrogen-based therapeutic agent. Herein, the anti-estrogenic action and anti-proliferative activity of guajadial is reported. The enriched guajadial fraction was obtained by sequential chromatographic techniques from the crude P. guajava dichloromethane extract showing promising anti-proliferative activity in vitro with selectivity for human breast cancer cell lines MCF-7 and MCF-7 BUS (Total Growth Inhibition = 5.59 and 2.27 µg·mL-1, respectively). Furthermore, evaluation of anti-estrogenic activity in vivo was performed demonstrating that guajadial enriched fraction inhibited the proliferative effect of estradiol on the uterus of pre-pubescent rats. These results suggest a relationship between anti-proliferative and anti-estrogenic activity of guajadial, which possibly acts in tumor inhibition through estrogen receptors due to the compounds structural similarity to tamoxifen.

Foodomics evaluation of the anti-proliferative potential of Passiflora mollissima seeds.

The anti-proliferative potential of Passiflora mollissima seeds, an underexplored agri-food waste, was investigated in this work by evaluating the molecular changes induced at transcript and metabolite expression levels on HT-29 human colon cancer cells. For this purpose, a pressurized-liquid extract from P. mollissima seeds obtained under optimized conditions was used for the treatment of HT-29 cells and a multi-omics strategy applied, integrating transcriptomics and metabolomics analysis, along with viability and cell cycle assays to study the molecular mechanisms that explain the anti-proliferative activity of this fruit by-product. After treatment for 48 and 72 h, the viability of HT-29 colon cancer cells was markedly affected, whereas minor effects were observed on normal human colon fibroblast cells. The bioactive extract was shown to arrest HT-29 cells in the S and G2/M phases of the cell cycle, which might be mediated by the inactivation of the FAT10 cancer signalling pathway among other genes identified as altered in the transcriptomic analysis. In addition, cellular redox homeostasis, as well as the polyamines pathway and methionine metabolism were found to be affected as suggested from the metabolomics data. Finally, the Foodomics integration enabled the identification of genes, such as MAD2L1, involved in the polyamine and glutathione metabolism, or the inactivation of the NUPR1 transcription factor, that might be related with the alteration of the intracellular ceramide levels in response to endoplasmic reticulum stress.

Jabuticaba residues (Myrciaria jaboticaba (Vell.) Berg) are rich sources of valuable compounds with bioactive properties.

Jabuticaba (Myrciaria jaboticaba (Vell.) Berg) is a Brazilian berry, very appreciated for in natura consumption. However, its epicarp is not normally consumed due to its stiffness and astringent taste, and in manufacture of products from jabuticaba fruit, it is responsible for the generation of large amounts of residues. The exploration of by-products is becoming important for the obtainment of valuable bioactive compounds for food and pharmaceutical industries. In this context, jabuticaba epicarp was studied regarding its chemical composition, namely in terms of phenolic compounds, tocopherols, and organic acids, and its bioactive properties, such as antioxidant, anti-proliferate, anti-inflammatory, and antimicrobial activities. A total of sixteen phenolic compounds, four tocopherols and six organic acids were identified in jabuticaba epicarp. Regarding bioactive properties, it showed high antioxidant activity, also presenting moderate anti-inflammatory, anti-proliferative, and antimicrobial activities. The extract did not present hepatotoxicity, confirming the possibility of its applications without toxicity issues.

Synthesis, anti-proliferative activity, theoretical and 1H NMR experimental studies of Morita-Baylis-Hillman adducts from isatin derivatives.

Quaternary or spirocyclic 3-substituted-3-hydroxy-2-oxindole is considered a privileged scaffold. In other words, it is a molecular core present on several compounds with a wide spectrum of biological activities. Among its precursors, activated ketones (isatin nucleus) can be used as interesting starting points to Morita-Baylis-Hillman adducts derivatives, a class of compounds with good cytotoxic potential. In this paper, we present the synthesis, anti-proliferative activity against lung cancer cell line and a theoretical conformational study of 21 of Morita-Baylis-Hillman adducts from isatin derivatives, by DFT quantum chemical calculations, followed by a SAR and QSAR analysis. Besides, an efficient synthetic protocol and good biological activity profile were highlighted interesting observations about 1H NMR experimental spectra, molecular modeling results and crystallographic data available.

Oleanolic acid from black raisins, Vitis vinifera with antioxidant and antiproliferative potentials on HCT 116 colon cancer cell line

Vitis vinifera (black raisin) is commonly used in traditional medicine for the treatment of various ailments. In the present study, anti-oxidative and anti-cancer efficacy of oleanolic acid from ethyl acetate fraction of black raisins was evaluated and oleanolic acid was isolated without using of any chromatographic techniques and subjected to spectral assessment using UV-Vis spectrophotometer, 1H NMR, 13C NMR, MS and FT-IR for structural confirmation. Antiproliferative efficacy of oleanolic acid against human colon adenocarcinoma HCT-116 cells was assessed using cell viability assay. The minimum inhibitory concentration (IC50) was determined and found to be 40 µg/mL at 48h incubation. Furthermore, antioxidant property of oleanolic acid was analyzed using DPPH method (IC50 is 61.5µg/mL) by compared to standard antioxidants ascorbic acid, gallic acid, pyrogallol and butylated hydroxytoluene. Hence, the present study aims to establish the use of oleanolic acid as a potential therapeutic agent against human colon cancer.