scholarly journals The Potential use of Geraniol Esters from Citronella Oil as Anticancer Agents

2019 ◽  
Vol 35 (3) ◽  
pp. 987-996
Author(s):  
Galuh Widiyarti ◽  
Megawati Megawati ◽  
Muhammad Hanafi
Keyword(s):  
Anticancer Agents ◽  
Vero Cells ◽  
Artemia Salina ◽  
Proton Nuclear Magnetic Resonance ◽  
Anticancer Compounds ◽  
Citronella Oil ◽  
Ic50 Values ◽  
Geranyl Butyrate ◽  
Gas Chromatography Mass Spectroscopy ◽  
Layer Chromatography

Geraniol which is mainly contained in citronella oil is one of the Indonesian natural products with anticancer potential. In this study, synthesis of geranyl butyrate, geranyl caproate, and geranyl caprylate from geraniol was conducted using sodium hydroxide as a catalyst. The aim was to enhance the anticancer activity of geraniol as a starting material. In order to achieve this, its esters were identified through the use of Gas Chromatography-Mass Spectroscopy (GCMS), Fourier Transform Infra Red (FTIR), Thin Layer Chromatography (TLC), and Proton Nuclear Magnetic Resonance (1H-NMR). They were analyzed for their potential as anticancer agents through Brine Shrimp Lethality Test (BSLT) against Artemia salina Leach, Mosmann method against murine leukemia (P388) cells and normal (Vero) cells. It was found that geraniol esters have the potential to be anticancer compounds. This was indicated by LC50 values of 0.96-1.46 µg/ml against A. salina L, IC50 values of 22.34-32.29 µg/ml against P388 cells, and very less cytotoxic effect on Vero cells with IC50 values of 116.08-172.93 µg/ml. Therefore, there is an expectation that acyclic ester compounds should be used in treating cancer.

scholarly journals Xanthohumol, a Prenylated Flavonoid from Hops, Induces DNA Damages in Colorectal Cancer Cells and Sensitizes SW480 Cells to the SN38 Chemotherapeutic Agent

Cells ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 932
Author(s):  
Alessandra Scagliarini ◽  
Aline Mathey ◽  
Virginie Aires ◽  
Dominique Delmas
Keyword(s):  
Colorectal Cancer ◽  
Dna Damage ◽  
Anticancer Agents ◽  
Ataxia Telangiectasia Mutated ◽  
Anticancer Compounds ◽  
Dna Damages ◽  
Systematic Screening ◽  
Colorectal Cancer Cells ◽  
Ic50 Values ◽  
First Time

In spite of chemotherapy and systematic screening for people at risk, the mortality rate of colorectal cancer (CRC) remains consistently high, with 600,000 deaths per year. This low success rate in the treatment of CRC results from many failures associated with high resistance and the risk of metastasis. Therefore, in response to these therapeutic failures, new strategies have been under development for several years aimed at increasing the effect of anticancer compounds and/or at reducing their secondary effects on normal cells, thus enabling the host to better withstand chemotherapy. This study highlights that xanthohumol (Xn) concentrations under the IC50 values were able to induce apoptosis and to enhance the DNA-damage response (DDR). We demonstrate for the first time that Xn exerts its anticancer activity in models of colon cancer through activation of the ataxia telangiectasia mutated (ATM) pathway. Subsequently, the ability of Xn to restore DNA damage in CRC cells can sensitize them to anticancer agents such as SN38 (7-ethyl-10-hydroxycamptothecin) used in chemotherapy.

scholarly journals Antioxidant Activity and Cytotoxicity Against WiDR Cell and Vero Cell of The Karamunting (Rhonomyrtus tomentosa L.) Leaves Ethanol Extract

2021 ◽  
Vol 8 (3) ◽  
pp. 111
Author(s):  
Marwati Marwati ◽  
Andi Anggriani ◽  
Asril Burhan ◽  
Akbar Awaluddin ◽  
Syamsu Nur ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Ethanol Extract ◽  
Vero Cells ◽  
Total Phenolic ◽  
Mtt Method ◽  
Ic50 Values ◽  
Diphenyl Tetrazolium Bromide ◽  
Phenolic And Flavonoid ◽  
Rhodomyrtus Tomentosa

Karamunting (Rhodomyrtus tomentosa L.), a plant used as a traditional medicine, is widely distributed throughout Indonesia. Karamuting has the potential as an antioxidant and anticancer agents because of its phenolic and flavonoid components. This study aimed to determine total phenolic level, antioxidant activity and cytotoxic of karamunting leaves extract. The simplisia of karamunting leaves were extracted by maceration method using 96% ethanol, tested for its antioxidant activity using DPPH and its citotoxic by MTT method (3- (4,5-dimethyltiazol-2-il) -2,5-diphenyl tetrazolium bromide) on WiDr cells and Vero cells. The results of this study showed that the yield of karamunting extract were 15.635% with a total phenolic level of 0.76%, antioxidant activity (IC50 values) of 15,330 μg / mL and cytotoxicity (IC50 values) of 205.7069 μg / mL for WiDr cells and 44.87703 μg / mL for Vero cells. Ethanol extract of karamunting leaves possessed a very strong antioxidant activity while it showed a weak cytotoxic effect on WiDr cells and toxic effect on Vero cells.Keywords: Antioxidant, Anticancer, Karamunting

Synthesis, Characterization, and Biological Evaluation of Novel Naringenin Derivatives as Anticancer Agents

2020 ◽  
Vol 16 (4) ◽  
pp. 442-448 ◽  
Author(s):  
Yogesh Murti ◽  
Pradeep Mishra
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Colorimetric Assay ◽  
Biological Evaluation ◽  
Proton Nuclear Magnetic Resonance ◽  
Sulforhodamine B ◽  
Ic50 Values ◽  
Grinding Technique ◽  
Ht 29 ◽  
Mcf 7

Background: In the present study, a series of substituted naringenin derivatives was synthesized by Claisen–Schmidt reaction using grinding technique. Methods: Synthesized compounds were characterized on the basis of Fourier-Transform Infrared Spectroscopy (FTIR), proton Nuclear Magnetic Resonance (1H NMR), Mass Spectroscopy (MS) and elemental analysis. These derivatives were screened for anticancer activity on breast (MCF-7) and colon (HT-29) cell lines using Sulforhodamine B (SRB) colorimetric assay. Results: Results displayed improved inhibitory concentration (IC50) values of naringenin derivatives. IC50 values of 3(4-chlorobenzylidene)-5,7-dihydroxy-2(4-hydroxyphenyl)chroman-4-one are 10.35 μM (MCF-7) & 12.03 μM (HT-29), which is most potent compound in the series. These finding confirms the suitability of 3-substituted naringenin in improving the anticancer effect. Conclusion: Due to the intense interest in the development of drugs capable of inhibiting cancerous cells, naringenin derivatives may represent important precursor molecules for the therapeutic armamentarium of colon and breast cancer. Further structural modification in these structures will be of interest and may result in compounds having a better anticancer activity.

Cytotoxic Activity and DNA Binding Property of New Aminopyrimidine Derivatives

2020 ◽  
Vol 17 (5) ◽  
pp. 640-654
Author(s):  
Hamidreza Akrami ◽  
Bibi Fatemeh Mirjalili ◽  
Omidreza Firuzi ◽  
Azadeh Hekmat ◽  
Ali Akbar Saboury ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Lymphoblastic Leukemia ◽  
Cd Spectroscopy ◽  
Myelogenous Leukemia ◽  
Breast Adenocarcinoma ◽  
Binding Property ◽  
Anticancer Compounds ◽  
Calf Thymus ◽  
Dna Binding Property

Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT assay. The interaction of the most promising compound with calf-thymus DNA was also studied using spectrometric titrations and Circular Dichroism (CD) spectroscopy. Results: Most compounds showed promising activity against tested cell lines. Among them, 2,4- dimethoxyanilino derivative 6g exhibited the best profile of activity against tested cell lines (IC50s = 1.6-6.1 μM) with no toxicity against NIH3T3 normal cell (IC50 >200 μM). The spectrometric studies exhibited that compound 6g binds to DNA strongly and may change DNA conformation significantly, presumably via a groove binding mechanism. Conclusion: The results of this study suggest that the prototype compound 6g can be considered as a novel lead compound for the design and discovery of novel anticancer agents.

Pyrrolizines as Potential Anticancer Agents: Design, Synthesis, Caspase-3 activation and Micronucleus (MN) Induction

2019 ◽  
Vol 18 (15) ◽  
pp. 2124-2130
Author(s):  
Amany Belal
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Assay Method ◽  
Breast Adenocarcinoma ◽  
Compound I ◽  
Design Synthesis ◽  
Ic50 Values ◽  
New Compounds

Background: For further exploration of the promising pyrrolizine scaffold and in continuation of our previous work, that proved the potential anticancer activity of the hit compound I, a new series of pyrrolizines 2-5 and 7-9 were designed and synthesized. Methods: Structures of the new compounds were confirmed by IR, 1H-NMR, 13C-NMR and elemental analysis. Antitumor activity for the prepared compounds against human breast adenocarcinoma (MCF-7), liver (HEPG2) and colon (HCT116) cancer cell lines was evaluated using SRB assay method. Result: Compounds 2, 3 and 5 were the most potent on colon cancer cells, their IC50 values were less than 5 µM. Compounds 2, 3 and 8 were the most potent on liver cancer cells, their IC50 values were less than 10 µM. As for MCF7, compounds 2, 7, 8 and 9 were the most active with IC50 values less than 10 µM. We can conclude that combining pyrrolizine scaffold with urea gave abroad spectrum anticancer agent 2 against the three tested cell lines. Micronucleus assays showed that compounds 2, 3, 8 are mutagenic and can induce apoptosis. In addition, caspase-3 activation was evaluated and compound 2 showed increase in the level of caspase-3 (9 folds) followed by 3 (8.28 folds) then 8 (7.89 folds). Conclusion: The obtained results encourage considering these three compounds as novel anticancer prototypes.

scholarly journals In Search of Effective Anticancer Agents—Novel Sugar Esters Based on Polyhydroxyalkanoate Monomers

2021 ◽  
Vol 22 (13) ◽  
pp. 7238
Author(s):  
Wojciech Snoch ◽  
Dawid Wnuk ◽  
Tomasz Witko ◽  
Jakub Staroń ◽  
Andrzej J. Bojarski ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Prostate Cancer Cell ◽  
Fatty Acid Esters ◽  
Skin Melanoma ◽  
Cancer Treatments ◽  
Sugar Esters ◽  
Hydroxylated Fatty Acids ◽  
Ic50 Values ◽  
Metastatic Process ◽  
Acid Esters

Cancer is one of the deadliest illness globally. Searching for new solutions in cancer treatments is essential because commonly used mixed, targeted and personalized therapies are sometimes not sufficient or are too expensive for common patients. Sugar fatty acid esters (SFAEs) are already well-known as promising candidates for an alternative medical tool. The manuscript brings the reader closer to methods of obtaining various SFAEs using combined biological, chemical and enzymatic methods. It presents how modification of SFAE’s hydrophobic chains can influence their cytotoxicity against human skin melanoma and prostate cancer cell lines. The compound’s cytotoxicity was determined by an MTT assay, which followed an assessment of SFAEs’ potential metastatic properties in concentrations below IC50 values. Despite relatively high IC50 values (63.3–1737.6 μM) of the newly synthesized SFAE, they can compete with other sugar esters already described in the literature. The chosen bioactives caused low polymerization of microtubules and the depolymerization of actin filaments in nontoxic levels, which suggest an apoptotic rather than metastatic process. Altogether, cancer cells showed no propensity for metastasis after treating them with SFAE. They confirmed that lactose-based compounds seem the most promising surfactants among tested sugar esters. This manuscript creates a benchmark for creation of novel anticancer agents based on 3-hydroxylated fatty acids of bacterial origin.

scholarly journals PPO-Inhibiting Herbicides and Structurally Relevant Schiff Bases: Evaluation of Inhibitory Activities against Human Protoporphyrinogen Oxidase

Processes ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 383
Author(s):  
Milan Jakubek ◽  
Michal Masařík ◽  
Tomáš Bříza ◽  
Robert Kaplánek ◽  
Kateřina Veselá ◽  
...  
Keyword(s):  
Melting Temperature ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Protoporphyrin Ix ◽  
Docking Study ◽  
Structural Motif ◽  
Protoporphyrinogen Oxidase ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Potential Inhibitors

The study of human protoporphyrinogen oxidase (hPPO) inhibition can contribute significantly to a better understanding of some pathogeneses (e.g., porphyria, herbicide exposure) and the development of anticancer agents. Therefore, we prepared new potential inhibitors with Schiff base structural motifs (2-hydroxybenzaldehyde-based Schiff bases 9–13 and chromanone derivatives 17–19) as structurally relevant to PPO herbicides. The inhibitory activities (represented by the half maximal inhibitory concentration (IC50) values) and enzymatic interactions (represented by the hPPO melting temperatures) of these synthetic compounds and commercial PPO herbicides used against hPPO were studied by a protoporphyrin IX fluorescence assay. In the case of PPO herbicides, significant hPPO inhibition and changes in melting temperature were observed for oxyfluorten, oxadiazon, lactofen, butafenacil, saflufenacil, oxadiargyl, chlornitrofen, and especially fomesafen. Nevertheless, the prepared compounds did not display significant inhibitory activity or changes in the hPPO melting temperature. However, a designed model of hPPO inhibitors based on the determined IC50 values and a docking study (by using AutoDock) found important parts of the herbicide structural motif for hPPO inhibition. This model could be used to better predict PPO herbicidal toxicity and improve the design of synthetic inhibitors.

scholarly journals Novel Marine Compounds: Anticancer or Genotoxic?

2004 ◽  
Vol 2004 (2) ◽  
pp. 93-98 ◽  
Author(s):  
Jamal M. Arif ◽  
Amal A. Al-Hazzani ◽  
Muhammed Kunhi ◽  
Fahad Al-Khodairy
Keyword(s):  
Clinical Trials ◽  
Anticancer Agents ◽  
Screening Tests ◽  
Tumor Xenograft ◽  
Anticancer Compounds ◽  
Early Exit ◽  
Marine Compounds ◽  
Xenograft Models ◽  
Pharmaceutical Industries ◽  
Carcinogenesis Models

In the past several decades, marine organisms have generously gifted to the pharmaceutical industries numerous naturally bioactive compounds with antiviral, antibacterial, antimalarial, anti-inflammatory, antioxidant, and anticancer potentials. But till date only few anticancer drugs (cytarabine, vidarabine) have been commercially developed from marine compounds while several others are currently in different clinical trials. Majority of these compounds were tested in the tumor xenograft models, however, lack of anticancer potential data in the chemical- and/or oncogene-induced pre-initiation animal carcinogenesis models might have cost some of the marine anticancer compounds an early exit from the clinical trials. This review critically discusses importance of preclinical evaluation, failure of human clinical trials with certain potential anticancer agents, the screening tests used, and choice of biomarkers.

Cationicity and hydrophobicity enhance the cytotoxic potency of Phoratoxin C anticancer peptide analogues against triple negative breast cancer cells

2021 ◽  
Vol 17 ◽  
Author(s):  
Chu Xin Ng ◽  
Cheng Foh Le ◽  
Sau Har Lee
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Breast Cancer Cells ◽  
Critical Role ◽  
Three Dimensional ◽  
Vero Cells ◽  
Anticancer Peptides ◽  
Α Helix ◽  
Peptide Analogues

Background: Anticancer peptides (ACPs) have received increasing attention as a promising class of novel anticancer agents owing to its potent and rapid cytotoxic properties. In this study, we aim to investigate the effects of cationicity and hydrophobicity in modulating the cytotoxicity of PtxC, a class of ACP from the leafy mistletoe Phoradendron tomentosum against the MDA-MB-231 and Vero cells. Method: We designed a series of four PtxC analogues (PA1 – PA4) by residual substitutions with specific amino acids to introduce the specific charge and hydrophobicity alterations to the analogues. The cytotoxicity strength of the PtxC analogues on MDA-MB-231 and Vero cells were tested by using MTT assay at 24 hours post treatment. Results: PA1, PA2 and PA4 displayed marked increases in cytotoxicity against both MDA-MB-231 and Vero cells and can be ranked in the order of PA2 > PA4 > PA1 > PtxC > PA3. Sequence-activity relationship analyses of the designed analogues showed that an increase in the level of cationicity and hydrophobicity correlated well with the enhanced cytotoxic activity of PtxC analogues. This was observed with PA1 (netC +8) and PA2 (netC +10) in comparison to PtxC (netC +7). Similar finding was observed for PA4 (GRAVY +0.070) in contrast to PtxC (GRAVY -0.339). Three-dimensional modelling predicted a double α-helix structure in PtxC class of ACP. The larger first helix in PA2 and PA4 was suggested to be responsible for the enhanced cytotoxicity observed. Conclusion: The critical role of cationicity and hydrophobicity in enhancing cytotoxicity of PtxC class of ACPs were clearly demonstrated in our study. The current findings could be extrapolated to benefit peptide design strategy in other classes of ACPs toward the discovery of highly potent ACPs against cancer cells as potential novel therapeutic agents.

Advancements in the Use of Platinum Complexes as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Rajiv Sharma ◽  
Vikram Jeet Singh ◽  
Pooja A Chawla
Keyword(s):  
Anticancer Agents ◽  
Biomedical Applications ◽  
Clinical Importance ◽  
Platinum Complexes ◽  
Water Soluble ◽  
Platinum Compounds ◽  
Anticancer Compounds ◽  
Cellular Resistance ◽  
Anti Cancer ◽  
Target Effects

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Method: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.

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