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Fulltext Multivariate statistical analysis of antioxidants in dates (Phoenix dactylifera)

Abbas, F.M.A., Foroogh, B., Liong, M.T., Azhar, M.E.

International Food Research Journal, 2008;15(2):193-200.
MyJurnal

Four types of soft dates (SD), three types of semi-dried dates (SDD) and one type of dried dates (DD) were used in this study. The antioxidant activities were assessed using TEAC method (ABTS assay) and the ferric reducing/antioxidant power method (FRAP assay), while total phenolic content (TPC) and total flavonoid content (TFC) were measured using Folin-Ciocalteau and aluminum chloride colorimetric methods. Multivariate analysis of variance (MANOVA), discriminant analysis (DA) and principal component analysis (PCA) were used to analyze the data. MANOVA showed a strong significant difference between the eight types of dates. DA identified the relative contribution of each parameter in distinguishing the dates. DA also identified two functions responsible for discriminating the dates and showed the difference between different types of dates. The first function distinguished DD from other types of dates, whilst the second function discriminated SD and SDD, affording 100% correct assignation. PCA identified only one component responsible for explaining 98.85% of the total variance in antioxidant data. It is suggested that the TEAC method and the quantitative determination of TPC and TFC was suitable for differentiation of dates and quality control.

Matched MeSH terms: Flavonoids
New chrysin-functionalized silica-core shell magnetic nanoparticles for the magnetic solid phase extraction of copper ions from water samples

Abd Ali LI, Ibrahim WA, Sulaiman A, Kamboh MA, Sanagi MM

Talanta, 2016 Feb 1;148:191-9.
PMID: 26653440 DOI: 10.1016/j.talanta.2015.10.062

This study describes the synthesis, characterization and application of a new chrysin-based silica core-shell magnetic nanoparticles (Fe3O4@SiO2-N-chrysin) as an adsorbent for the preconcentration of Cu(II) from aqueous environment. The morphology, thermal stability and magnetic property of Fe3O4@SiO2-N-chrysin were analyzed using FTIR, FESEM, TEM, XRD, thermal analysis and VSM. The extraction efficiency of Fe3O4@SiO2-N-chrysin was analyzed using the batch wise method with flame atomic absorption spectrometry. Parameters such as the pH, the sample volume, the adsorption-desorption time, the concentration of the desorption solvent, the desorption volume, the interference effects and the regeneration of the adsorbent were optimized. It was determined that Cu(II) adsorption is highly pH-dependent, and a high recovery (98%) was achieved at a pH 6. The limit of detection (S/N=3), the limit of quantification (S/N=10), the preconcentration factor and the relative standard deviation for Cu(II) extraction were 0.3 ng mL(-1), 1 ng mL(-1), 100 and 1.9% (concentration=30 ng mL(-1), n=7), respectively. Excellent relative recoveries of 97-104% (%RSD<3.12) were achieved from samples from a spiked river, a lake and tap water. The MSPE method was also validated using certified reference materials SLRS-5 with good recovery (92.53%).

Matched MeSH terms: Flavonoids
Fulltext Molecular Docking Study of Naturally Derived Flavonoids with Antiapoptotic BCL-2 and BCL-XL Proteins toward Ovarian Cancer Treatment

Abd Ghani MF, Othman R, Nordin N

J Pharm Bioallied Sci, 2020 Nov;12(Suppl 2):S676-S680.
PMID: 33828360 DOI: 10.4103/jpbs.JPBS_272_19

The naturally derived flavonoids are well known to have anticarcinogenic effects. Flavonoids could be an alternative strategy for ovarian cancer treatment, due to existing platinum-based drugs are reported to develop resistance with low survival rates. Inhibition of antiapoptotic proteins, namely B-cell lymphoma (Bcl-2) and B-cell lymphoma-extra large (Bcl-xl), is the key target to stimulate apoptosis process in cancer cells. This study aimed to determine the binding interaction of five naturally derived flavonoids (biochanin A, myricetin, apigenin, galangin, and fisetin) with potential antiapoptotic target proteins (Bcl-2 and Bcl-xl). The molecular docking study was conducted using AutoDock Vina program. The binding affinity and the presence of hydrogen bonds between the flavonoids and target proteins were predicted. Our findings showed that all the flavonoids showed better binding affinity with Bcl-xl than that of Bcl-2 proteins. The highest binding affinity was recorded in fisetin-Bcl-xl protein complex (-8.8 kcal/mol). Meanwhile, the other flavonoids docked with Bcl-xl protein showed binding affinities, ranging from -8.0 to -8.6 kcal/mol. A total of four hydrogen bonds, four hydrophobic contacts, and one electrostatic interaction were detected in the docked fisetin-Bcl-xl complex, explaining its high binding affinity with Bcl-xl. The present results indicate that all flavonoids could potentially serve as Bcl-xl protein inhibitors, which would consequently lead to apoptotic process in ovarian cancers.

Matched MeSH terms: Flavonoids
Fulltext Moringa Genus: A Review of Phytochemistry and Pharmacology

Abd Rani NZ, Husain K, Kumolosasi E

Front Pharmacol, 2018;9:108.
PMID: 29503616 DOI: 10.3389/fphar.2018.00108

Moringa
is a genus of medicinal plants that has been used traditionally to cure wounds and various diseases such as colds and diabetes. In addition, the genus is also consumed as a source of nutrients and widely used for purifying water. The genus consists of 13 species that have been widely cultivated throughout Asia and Africa for their multiple uses. The purpose of this review is to provide updated and categorized information on the traditional uses, phytochemistry, biological activities, and toxicological research ofMoringaspecies in order to explore their therapeutic potential and evaluate future research opportunities. The literature reviewed for this paper was obtained from PubMed, ScienceDirect, and Google Scholar journal papers published from 1983 to March 2017.Moringaspecies are well-known for their antioxidant, anti-inflammatory, anticancer, and antihyperglycemic activities. Most of their biological activity is caused by their high content of flavonoids, glucosides, and glucosinolates. By documenting the traditional uses and biological activities ofMoringaspecies, we hope to support new research on these plants, especially on those species whose biological properties have not been studied to date.

Matched MeSH terms: Flavonoids
Fulltext Eupatorin Suppressed Tumor Progression and Enhanced Immunity in a 4T1 Murine Breast Cancer Model

Abd Razak N, Yeap SK, Alitheen NB, Ho WY, Yong CY, Tan SW, et al.

Integr Cancer Ther, 2020 8 25;19:1534735420935625.
PMID: 32830560 DOI: 10.1177/1534735420935625

Eupatorin is a polymethoxy flavone extracted from Orthosiphon stamineus and was reported to exhibit cytotoxic effects on several cancer cell lines. However, its effect as an anti-breast cancer agent in vivo has yet to be determined. This study aims to elucidate the potential of eupatorin as an anti-breast cancer agent in vivo using 4T1 challenged BALB/c mice model. In this article, BALB/c mice (20-22 g) challenged with 4T1 cells were treated with 5 mg/kg or 20 mg/kg eupatorin, while the untreated and healthy mice were fed with olive oil (vehicle) via oral gavage. After 28 days of experiment, the mice were sacrificed and blood was collected for serum cytokine assay, while tumors were harvested to extract RNA and protein for gene expression assay and hematoxylin-eosin staining. Organs such as spleen and lung were harvested for immune suppression and clonogenic assay, respectively. Eupatorin (20 mg/kg) was effective in delaying the tumor development and reducing metastasis to the lung compared with the untreated mice. Eupatorin (20 mg/kg) also enhanced the immunity as the population of NK1.1+ and CD8+ in the splenocytes and the serum interferon-γ were increased. Concurrently, eupatorin treatment also has downregulated the expression of pro-inflammatory and metastatic related genes (IL-1β. MMP9, TNF-α, and NF-κB). Thus, this study demonstrated that eupatorin at the highest dosage of 20 mg/kg body weight was effective in delaying the 4T1-induced breast tumor growth in the animal model.

Matched MeSH terms: Flavonoids
Fulltext Alterations in Herbage Yield, Antioxidant Activities, Phytochemical Contents, and Bioactive Compounds of Sabah Snake Grass (Clinacanthus Nutans L.) with Regards to Harvesting Age and Harvesting Frequency

Abd Samat NMA, Ahmad S, Awang Y, Bakar RAH, Hakiman M

Molecules, 2020 Jun 19;25(12).
PMID: 32575450 DOI: 10.3390/molecules25122833

Sabah snake grass or Clinacanthus nutans has drawn public interest having significant economic benefits attributable to the presence of phytochemicals and several interesting bioactive constituents that may differ according to harvesting age and harvesting frequency. The current study was aimed to evaluate the effect of harvesting age and harvesting frequency towards herbal yield, antioxidant activities, phytochemicals synthesis, and bioactive compounds of C. nutans. A factorial randomized completely block design with five replications was used to illustrate the relationship between herbal yield, DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ferric reducing antioxidant power (FRAP) assays, total phenolic and flavonoid content affected by harvesting age (week 8, 12, and 16 after transplanting), and harvesting frequency (harvest 1, 2, and 3). The bioactive compounds by HPLC were also determined to describe the interaction effect between both harvesting age and harvesting frequency. The yield, antioxidant activities, and phytochemical contents were gradually increased as the plant grew, with the highest recorded during week 16. However, the synthesis and activities of phytochemicals were reduced in subsequent harvests despite the increment of the herbal yield. All bioactive compounds were found to be influenced insignificantly and significantly by harvesting age and harvesting frequency, respectively, specifically to shaftoside, iso-orientin, and orientin. Among all constituents, shaftoside was the main compound at various harvesting ages and harvesting frequencies. These results indicated that harvesting at week 16 with 1st harvest frequency might enhance the yield while sustaining the high synthesis of polyphenols and antioxidant activities of C. nutans.

Matched MeSH terms: Flavonoids
Fulltext Chemical reaction of soybean flavonoids with DNA: a computational study using the implicit solvent model

Abdallah HH, Mavri J, Repič M, Lee VS, Wahab HA

Int J Mol Sci, 2012;13(2):1269-83.
PMID: 22408390 DOI: 10.3390/ijms13021269

Genistein, daidzein, glycitein and quercetin are flavonoids present in soybean and other vegetables in high amounts. These flavonoids can be metabolically converted to more active forms, which may react with guanine in the DNA to form complexes and can lead to DNA depurination. We assumed two ultimate carcinogen forms of each of these flavonoids, diol epoxide form and diketone form. Density functional theory (DFT) and Hartree-Fock (HF) methods were used to study the reaction thermodynamics between active forms of flavonoids and DNA guanine. Solvent reaction field method of Tomasi and co-workers and the Langevin dipoles method of Florian and Warshel were used to calculate the hydration free energies. Activation free energy for each reaction was estimated using the linear free energy relation. Our calculations show that diol epoxide forms of flavonoids are more reactive than the corresponding diketone forms and are hence more likely flavonoid ultimate carcinogens. Genistein, daidzein and glycitein show comparable reactivity while quercetin is less reactive toward DNA.

Matched MeSH terms: Flavonoids/chemistry*
Chemical composition, antioxidant and antibacterial properties of the essential oils of Etlingera elatior and Cinnamomum pubescens Kochummen

Abdelwahab SI, Zaman FQ, Mariod AA, Yaacob M, Abdelmageed AH, Khamis S

J Sci Food Agric, 2010 Dec;90(15):2682-8.
PMID: 20945508 DOI: 10.1002/jsfa.4140

Plant essential oils are widely used as fragrances and flavours. Therefore, the essential oils from the leaves of Cinnamomum pubescens Kochummen (CP) and the whole plant of Etlingera elatior (EE) were investigated for their antioxidant, antibacterial and phytochemical properties.

Matched MeSH terms: Flavonoids/analysis; Flavonoids/pharmacology*
Combined extract of Moringa oleifera and Centella asiatica modulates oxidative stress and senescence in hydrogen peroxide-induced human dermal fibroblasts

Abdul Hisam EE, Rofiee MS, Khalid AM, Jalaluddin AF, Mohamad Yusof MI, Idris MH, et al.

Turk J Biol, 2018;42(1):33-44.
PMID: 30814868 DOI: 10.3906/biy-1708-23

Moringa oleifera Lam. and Centella asiatica (L.) Urb. leaves have been previously reported to exhibit antioxidant activity. The objective of the present study is to determine the in vitro antioxidant activity of the combined extracts of M. oleifera and C. asiatica (TGT-PRIMAAGE) and its effect on hydrogen peroxide (H 2O2)-induced oxidative stress in human dermal fibroblasts. TGTPRIMAAGE acted on the mechanism of hydrogen transfer as it showed scavenging activity in the DPPH assay. This is due to the presence of phenolics and flavonoids in TGT-PRIMAAGE. TGT-PRIMAAGE effectively reduced cellular generation of reactive oxygen species induced by H O2. The activities of superoxide dismutase and catalase were also increased in cells treated with TGT-PRIMAAGE. 2 Treatment with TGT-PRIMAAGE showed significant reduction (P < 0.05) in the number of senescent cells. Significant reduction (P < 0.05) of malondialdehyde was also seen in cells treated with TGT-PRIMAAGE. The p53 protein level was reduced in TGT-PRIMAAGEtreated cells, which indicates its potential in protecting the cells from oxidative stress induced by H2O2.

Matched MeSH terms: Flavonoids
Nutritional values and bioactive components of under-utilised vegetables consumed by indigenous people in Malaysia

Abdul Wahab N, Ahdan R, Ahmad Aufa Z, Kong KW, Johar MH, Shariff Mohd Z, et al.

J Sci Food Agric, 2015 Oct;95(13):2704-11.
PMID: 25410129 DOI: 10.1002/jsfa.7006

Diverse plants species in the forest remain under-utilised and they are mainly consumed only by local people. However, increasing issues in food security prompted the present study, which explores the nutritional and antioxidant aspects of Malaysian under-utilised vegetables. The studied vegetables were Paku Nyai (Stenochlaena palustris), Cemperai (Champereia manillana), Maman Pasir (Cleome viscose), Dudung (Erechtites valerianifolia) and Semambuk (Ardisia pendula).

Matched MeSH terms: Flavonoids/analysis; Flavonoids/pharmacology
Therapeutic uses of epicatechin in diabetes and cancer

Abdulkhaleq LA, Assi MA, Noor MHM, Abdullah R, Saad MZ, Taufiq-Yap YH

Vet World, 2017 Aug;10(8):869-872.
PMID: 28919675 DOI: 10.14202/vetworld.2017.869-872

Epicatechin is a natural flavonoid found in green tea. It has been reported to possess an immense antioxidant effect which contributes to its therapeutic effect against a handful of ailments. In this review, we discuss its therapeutic role in the management of two of the most important human diseases; diabetes and cancer. The consumption of epicatechin has been shown to reduce blood glucose levels in diabetic patients, while is anticancer effect was attributed to its antioxidant properties, antiangiogenic and direct cytotoxicity to cancer cells. Although the exact mechanism of action of epicatechin is still being explored, there is no doubt that it is a promising candidate as an alternative. The significance of this review is to highlight the importance of the usage of natural products (in this case, epicatechin) as an alternative for the treatment of two potentially fatal diseases which is diabetes and cancer. The aim of this review is to educate the scientific community on the role of epicatechin in ameliorating the effects of diabetes and cancers on human while understanding the potential mechanisms of these aforementioned effects.

Matched MeSH terms: Flavonoids
Fulltext Chemical Constituents of Malaysian U. cordata var. ferruginea and Their in Vitro α-Glucosidase Inhibitory Activities

Abdullah NH, Salim F, Ahmad R

Molecules, 2016 Apr 27;21(5).
PMID: 27128898 DOI: 10.3390/molecules21050525

Continuing our interest in the Uncaria genus, the phytochemistry and the in-vitro α-glucosidase inhibitory activities of Malaysian Uncaria cordata var. ferruginea were investigated. The phytochemical study of this plant, which employed various chromatographic techniques including recycling preparative HPLC, led to the isolation of ten compounds with diverse structures comprising three phenolic acids, two coumarins, three flavonoids, a terpene and an iridoid glycoside. These constituents were identified as 2-hydroxybenzoic acid or salicylic acid (1), 2,4-dihydroxybenzoic acid (2), 3,4-dihydroxybenzoic acid (3), scopoletin or 7-hydroxy-6-methoxy-coumarin (4), 3,4-dihydroxy-7-methoxycoumarin (5), quercetin (6), kaempferol (7), taxifolin (8), loganin (9) and β-sitosterol (10). Structure elucidation of the compounds was accomplished with the aid of 1D and 2D Nuclear Magnetic Resonance (NMR) spectral data and Ultraviolet-Visible (UV-Vis), Fourier Transform Infrared (FTIR) spectroscopy and mass spectrometry (MS). In the α-glucosidase inhibitory assay, the crude methanolic extract of the stems of the plant and its acetone fraction exhibited strong α-glucosidase inhibition activity of 87.7% and 89.2%, respectively, while its DCM fraction exhibited only moderate inhibition (75.3%) at a concentration of 1 mg/mL. The IC50 values of both fractions were found to be significantly lower than the standard acarbose suggesting the presence of potential α-glucosidase inhibitors. Selected compounds isolated from the active fractions were then subjected to α-glucosidase assay in which 2,4-dihydroxybenzoic acid and quercetin showed strong inhibitory effects against the enzyme with IC50 values of 549 and 556 μg/mL compared to acarbose (IC50 580 μg/mL) while loganin and scopoletin only showed weak α-glucosidase inhibition of 44.9% and 34.5%, respectively. This is the first report of the isolation of 2-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid and loganin from the genus and the first report of the α-glucosidase inhibitory potential of 2,4-dihydroxybenzoic acid.

Matched MeSH terms: Flavonoids/pharmacology; Flavonoids/chemistry
Flavonoids from the leaves and heartwoods of Artocarpus lowii King and their bioactivities

Abdullah SA, Jamil S, Basar N, Abdul Lathiff SM, Mohd Arriffin N

Nat Prod Res, 2017 May;31(10):1113-1120.
PMID: 27564208 DOI: 10.1080/14786419.2016.1222387

A new dihydrochalcone, 2',4'-dihydroxy-3,4-(2″,2″-dimethylchromeno)-3'-prenyldihydrochalcone (1) together with 4-hydroxyonchocarpin (2), isobavachalcone (3), 4',5-dihydroxy-6,7-(2,2-dimethylpyrano)-2'-methoxy-8-γ,γ-dimethylallyflavone (4), artocarpin (5) and cycloheterophyllin (6) were successfully isolated from the leaves and heartwoods of Artocarpus lowii King (Moraceae). The structures of these compounds were fully characterised using spectroscopic methods and by direct comparison with published data. These compounds were tested for their antioxidant and tyrosinase inhibitory activities. Compound (1) displayed moderate antioxidant activity towards DPPH and tyrosinase inhibitory activities with SC50 value of 223.8 μM and IC50 value of 722.5 μM, respectively. Among the isolated compounds, cycloheterophyllin (6) showed the most potential antioxidant activity with SC50 value of 320.0 and 102.8 μM for ABTS and DPPH radicals scavenging activities, respectively, and also exhibited highest FRAP equivalent value of 4.7 ± 0.09 mM. Compound (6) showed tyrosinase inhibitory activity with the IC50 value of 104.6 μM.

Matched MeSH terms: Flavonoids
Phytochemicals and Potential Therapeutic Targets on Toxoplasma gondii Parasite

Abdullahi SA, Unyah NZ, Nordin N, Basir R, Nasir WM, Alapid AA, et al.

Mini Rev Med Chem, 2020;20(9):739-753.
PMID: 31660810 DOI: 10.2174/1389557519666191029105736

Identification of drug target in protozoan T. gondii is an important step in the development of chemotherapeutic agents. Likewise, exploring phytochemical compounds effective against the parasite can lead to the development of new drug agent that can be useful for prophylaxis and treatment of toxoplasmosis. In this review, we searched for the relevant literature on the herbs that were tested against T. gondii either in vitro or in vivo, as well as different phytochemicals and their potential activities on T. gondii. Potential activities of major phytochemicals, such as alkaloid, flavonoid, terpenoids and tannins on various target sites on T. gondii as well as other related parasites was discussed. It is believed that the phytochemicals from natural sources are potential drug candidates for the treatment of toxoplasmosis with little or no toxicity to humans.

Matched MeSH terms: Flavonoids/pharmacology; Flavonoids/therapeutic use; Flavonoids/chemistry
Polyphenol-enriched extract of oil palm fronds (Elaeis guineensis) promotes vascular relaxation via endothelium-dependent mechanisms

Abeywardena M, Runnie I, Nizar M, Suhaila M, Head R, Suhaila Momamed

Asia Pac J Clin Nutr, 2002;11 Suppl 7:S467-72.
PMID: 12492636

Plant-based polyphenolic compounds have been reported to possess cardiovascular health benefits. Several dietary sources, including herbs and spices, fruits and vegetables, and tea and wine, contain an array of biologically active compounds that have been shown to be effective in retarding oxidation of low-density lipoproteins (LDL) and promoting vascular relaxation. In the present study four different plant sources, both edible and non-edible, were evaluated for potential activity. Organic extracts enriched in polyphenols were prepared from palm fronds (Elaesis guineensis); lemongrass (Cymbopogon citrates); papaya shoots (Carica papaya) and green chilli (Capsicum frutescenes) and tested for their ability to prevent in vitro oxidation of LDL, and for potential vascular relaxation actions. Rings of rat thoracic aorta and isolated perfused mesenteric vascular beds were mounted in organ baths, contracted using a half-maximal dose of noradrenaline and exposed to cumulative additions of test extracts. Palm frond extract resulted in considerable relaxation (>75%) in both preparations and was found to be endothelium-dependent as removal of endothelium or inhibition of endogenous nitric oxide (NO) led to a total loss in relaxant activity. Lemongrass extract caused a greater relaxation action in the mesenteric preparation compared to aortic rings, and appears to be mediated via NO-independent and non-prostanoid mechanisms. Of the extracts tested, palm fronds also demonstrated the highest antioxidant capacity, as determined by the ferric reducing activity/potential assay, and resulted in a significant delay (P < 0.05) in the oxidation of LDL. Collectively, these preliminary findings lend further support to the potential cardiovascular actions of plant polyphenols and also identify oil palm fronds as containing constituents that promote vascular relaxation via endothelium-dependent mechanisms.

Matched MeSH terms: Flavonoids*
Fulltext The antioxidant activities, cytotoxic properties, and identification of water-soluble compounds of Ficus deltoidea leaves

Abrahim NN, Abdul-Rahman PS, Aminudin N

PeerJ, 2018;6:e5694.
PMID: 30324012 DOI: 10.7717/peerj.5694

Leaves from three varieties of Ficus deltoidea, colloquially termed small- (FDS), medium- (FDM), and big-type leaf (FDB), were subjected to water extraction. The crude extracts were fractionated using water (WF) and ethyl acetate (EAF). The phenolic and flavonoid content, antioxidant activity, and cytotoxicity of the fractions were investigated. The EAF had the highest phenolic and flavonoid content compared to the other FDS fractions. Conversely, the FDM crude extract had the highest phenolic and flavonoid content compared to the other FDM samples. Antioxidant activity was highest in the FDB crude extract. Ultra-high-performance liquid chromatography showed that two compounds, vitexin and coumaric acid, were present in the FDB crude extract. Additionally, the F. deltoidea leaves caused no signs of toxicity in a normal liver cell line. Our findings show that F. deltoidea varieties have excellent antioxidant activity with no cytotoxic effects on normal liver cells.

Matched MeSH terms: Flavonoids
Fulltext Design, Synthesis and Docking Studies of Flavokawain B Type Chalcones and Their Cytotoxic Effects on MCF-7 and MDA-MB-231 Cell Lines

Abu Bakar A, Akhtar MN, Mohd Ali N, Yeap SK, Quah CK, Loh WS, et al.

Molecules, 2018 Mar 08;23(3).
PMID: 29518053 DOI: 10.3390/molecules23030616

Flavokawain B (1) is a natural chalcone extracted from the roots of Piper methysticum, and has been proven to be a potential cytotoxic compound. Using the partial structure of flavokawain B (FKB), about 23 analogs have been synthesized. Among them, compounds 8, 13 and 23 were found in new FKB derivatives. All compounds were evaluated for their cytotoxic properties against two breast cancer cell lines, MCF-7 and MDA-MB-231, thus establishing the structure-activity relationship. The FKB derivatives 16 (IC50 = 6.50 ± 0.40 and 4.12 ± 0.20 μg/mL), 15 (IC50 = 5.50 ± 0.35 and 6.50 ± 1.40 μg/mL) and 13 (IC50 = 7.12 ± 0.80 and 4.04 ± 0.30 μg/mL) exhibited potential cytotoxic effects on the MCF-7 and MDA-MB-231 cell lines. However, the methoxy group substituted in position three and four in compound 2 (IC50 = 8.90 ± 0.60 and 6.80 ± 0.35 μg/mL) and 22 (IC50 = 8.80 ± 0.35 and 14.16 ± 1.10 μg/mL) exhibited good cytotoxicity. The lead compound FKB (1) showed potential cytotoxicity (IC50 = 7.70 ± 0.30 and 5.90 ± 0.30 μg/mL) against two proposed breast cancer cell lines. It is evident that the FKB skeleton is unique for anticancer agents, additionally, the presence of halogens (Cl and F) in position 2 and 3 also improved the cytotoxicity in FKB series. These findings could help to improve the future drug discovery process to treat breast cancer. A molecular dynamics study of active compounds revealed stable interactions within the active site of Janus kinase. The structures of all compounds were determined by ¹H-NMR, EI-MS, IR and UV and X-ray crystallographic spectroscopy techniques.

Matched MeSH terms: Flavonoids/chemical synthesis; Flavonoids/pharmacology*; Flavonoids/chemistry*
Fulltext Optimization of Extraction Conditions of Phytochemical Compounds and Anti-Gout Activity of Euphorbia hirta L. (Ara Tanah) Using Response Surface Methodology and Liquid Chromatography-Mass Spectrometry (LC-MS) Analysis

Abu Bakar FI, Abu Bakar MF, Abdullah N, Endrini S, Fatmawati S

Evid Based Complement Alternat Med, 2020;2020:4501261.
PMID: 32047524 DOI: 10.1155/2020/4501261

Gout is a common disease affected most of the people due to the elevation of uric acid in the blood. Flavonoid and phenolic compounds are reported to exert the anti-gout activity of medicinal plants. Hence, this study aimed at optimizing the extraction conditions of phenolic and flavonoid compounds as well as the anti-gout (xanthine oxidase inhibitory activity) in vitro of Euphorbia hirta using response surface methodology (RSM). The plant part used was the whole plant excluding roots. The effects of three independent variables (extraction time, X1; extraction temperature, X2; and solid-to-liquid ratio, X3) on three response variables (total flavonoid content, Y1; total phenolic content, Y2; and xanthine oxidase inhibitory activity, Y3) were determined using central composite design (CCD) while phytochemical profiling of the extracts was determined by liquid chromatography-mass spectrometry (LC-MS). Quadratic models produced a satisfactory fitting of the experimental data with regard to total flavonoid content (r2 = 0.9407, p < 0.0001), total phenolic content (r2 = 0.9383, p < 0.0001), and xanthine oxidase inhibitory activity (r2 = 0.9794, p < 0.0001). The best extraction conditions observed for total flavonoid content, total phenolic content, and xanthine oxidase inhibitory activity were at a temperature of 79.07°C for 17.42 min with solid-to-liquid ratio of 1 : 20 g/ml. The optimum values for total flavonoid, total phenolic, and xanthine oxidase inhibitory activity were 67.56 mg RE/g, 155.21 mg GAE/g, and 91.42%, respectively. The main phytochemical compounds in the optimized E. hirta extract are neochlorogenic acid, quercetin-3β-D-glucoside, syringic acid, caffeic acid, ellagic acid, astragalin, afzelin, and quercetin. As conclusion, this study clearly demonstrated the best conditions to obtain higher xanthine oxidase inhibitory activity and phytochemical compounds which can be further used for the development of anti-gout agents.

Matched MeSH terms: Flavonoids
Fulltext Phytochemical Constituents, Antioxidant and Antiproliferative Properties of a Liverwort, Lepidozia borneensis Stephani from Mount Kinabalu, Sabah, Malaysia

Abu Bakar MF, Abdul Karim F, Suleiman M, Isha A, Rahmat A

Evid Based Complement Alternat Med, 2015;2015:936215.
PMID: 26640502 DOI: 10.1155/2015/936215

The study aimed to investigate the phytochemical contents, antioxidant and antiproliferative activity of 80% methanol extract of Lepidozia borneensis. The total phenolic and total flavonoid contents were analysed using Folin-Ciocalteu and aluminium chloride colorimetric methods. Antioxidant properties were evaluated by using FRAP, ABTS, and DPPH assays while the effects of L. borneensis on the proliferation of MCF-7 cell line were evaluated by using MTT assay. The results showed that the total phenolic and flavonoid contents were 12.42 ± 0.47 mg GAE/g and 9.36 ± 1.29 mg CE/g, respectively. The GC-MS analysis revealed the presence of at least 35 compounds. The extract was found to induce cytotoxicity against MCF-7 cell line with IC50 value of 47.33 ± 7.37 µg/mL. Cell cycle analysis showed that the extract induced significant arrest at G0/G1 at 24 hours of treatment. After 72 hours of treatment, the proportion of cells in G0/G1 and G2-M phases had decreased significantly as compared to their control. Apoptosis occurred during the first 24 hours and significantly increased to 30.8% after 72 hours of treatment. No activation of caspase 3 was observed. These findings suggest that L. borneensis extract has the potential as natural antioxidant and anticancer agents.

Matched MeSH terms: Flavonoids
Fulltext Evaluation of Antinociceptive Profile of Chalcone Derivative (3-(2,5-dimethoxyphenyl)-1-(5-methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo

Abu Bakar NA, Sulaiman MR, Lajis N, Akhtar MN, Mohamad AS

J Pharm Bioallied Sci, 2020 Nov;12(Suppl 2):S711-S717.
PMID: 33828366 DOI: 10.4103/jpbs.JPBS_344_19

Introduction: Pain is a major global health issue, where its pharmacotherapy prompts unwanted side effects; hence, the development of effective alternative compounds from natural derivatives with lesser side effects is clinically needed. Chalcone; the precursors of flavonoid, and its derivatives have been widely investigated due to its pharmacological properties.
Objective: This study addressed the therapeutic effect of 3-(2,5-dimethoxyphenyl)-1-(5-methyl furan-2-yl) prop-2-en-1-one (DMPF-1); synthetic chalcone derivative, on antinociceptive activity in vivo.
Materials and Methods: The antinociceptive profile was evaluated using acetic-acid-induced abdominal writhing, hot plate, and formalin-induced paw licking test. Capsaicin, phorbol 12-myristate 12 acetate (PMA), and glutamate-induced paw licking test were carried out to evaluate their potential effects toward different targets.
Results: It was shown that the doses of 0.1, 0.5, 1, and 5 mg/kg of DMPF-1 given via intraperitoneal injection showed significant reduction in writhing responses and increased the latency time in hot-plate test where reduced time spent on licking the injected paw in formalin and dose contingency inhibition was observed. The similar results were observed in capsaicin, PMA, and glutamate-induced paw licking test. In addition, the challenge with nonselective opioid receptor antagonist (naloxone) aimed to evaluate the involvement of the opioidergic system, which showed no reversion in analgesic profile in formalin and hot-plate test.
Conclusion: Collectively, this study showed that DMPF-1 markedly inhibits both peripheral and central nociception through the mechanism involving an interaction with vanilloid and glutamatergic system regardless of the activation of the opioidergic system.

Matched MeSH terms: Flavonoids

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