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Fulltext Inhibitory effects of tangeretin and trans-ethyl caffeate on the HMG-CoA reductase activity: Potential agents for reducing cholesterol levels

Pangestika I, Oksal E, Tengku Muhammad TS, Amir H, Syamsumir DF, Wahid MEA, et al.

Saudi J Biol Sci, 2020 Aug;27(8):1947-1960.
PMID: 32714018 DOI: 10.1016/j.sjbs.2020.06.010

One of the pathways to reduce cholesterol production in the liver is through the inhibition of HMG-Coa reductase (HMGCR) by current drugs, statins. However, these have side effects if consumed in prolonged periods. Tangeretin and trans-ethyl caffeate as alternative drugs in reducing hypercholesterolemia and preventing atherosclerosis have never been reported. Their effects on inhibiting HMGCR activity were investigated through enzymatic method (in vitro and in vivo). The toxicity property was analyzed on the Serum Glutamate Oxalate Transaminase (SGOT)/Serum Glutamate Piruvate Transaminase (SGPT) levels and rat liver histology. The results showed that both compounds inhibited HMGCR activity significantly compare to the control simvastatin (p

Matched MeSH terms: Flavones
Fulltext Chemical constituents, usage and pharmacological activity of Cassia alata

Fatmawati S, Yuliana, Purnomo AS, Abu Bakar MF

Heliyon, 2020 Jul;6(7):e04396.
PMID: 32685725 DOI: 10.1016/j.heliyon.2020.e04396

Cassia alata or locally known as Ketepeng Cina (Indonesia) and Gelenggang (Malaysia) has been used as a traditional medicine to treat various diseases, especially skin diseases. In addition, C. alata has been reported to have potential anti allergic, anti inflammatory, antioxidant, anticancer, antidiabetic, and antifungal. Metabolite compounds that have been isolated from C. alata include flavones, flavonols, flavonoids glycosides, alatinon, alanonal and β-sitosterol-β-D-glucoside. The compounds have been isolated mainly from the leaves. Further identification is needed to discover the secondary metabolites from other parts of the plant such as seed, flower and bark which are reported to have potent antibacterial and antifungal activity. Therefore, this article highlights the secondary metabolites and biological activity of this plant which has been shown to have pharmacological properties against selected diseases.

Matched MeSH terms: Flavones
Fulltext Antioxidant and LC-QToF-MS/MS analysis of polyphenols in polar and non-polar extracts from Strobilanthes crispus and Clinacanthus nutans

Tan, H. M., Leong, K. H., Song, J., Mohd Sufian, N. S. F., Mohd Hazli, U. H. A., Chew, L. Y., et al.

International Food Research Journal, 2020;27(5):903-914.
MyJurnal

Strobilanthes crispus and Clinacanthus nutans are popular herbal plants in the Southeast
Asian region. The present work was aimed at determining the antioxidant activities and the
associated components in the leaf extracts of both species using polar and non-polar solvents
namely water, methanol, ethyl acetate, and hexane. The total phenolic content (TPC) and total
flavonoid content (TFC) were higher in the leaf extracts of S. crispus as compared to C.
nutans. Among the solvents, methanol was the best solvent in extracting the antioxidant
components for S. crispus (TPC: 159.85 ± 0.89 mg GAE/g extract and TFC: 955.47 ± 2.66 mg
RE/g extract). However, for C. nutans, its methanolic extract yielded the highest TPC (36.39
± 0.17 mg GAE/g extract), whereas ethyl acetate yielded the highest TFC (229.61 ± 7.81 mg
RE/g extract). The high levels of both TPC and TFC contributed to the antioxidant activities
of S. crispus extract as reflected in the methanolic extract attaining the highest level of
antioxidant activities, measured by ferric reducing antioxidant power (FRAP) (6.84 ± 1.12
mmol Fe2+/g extract), DPPH radical scavenging (IC50: 203.60 ± 7.28 μg/mL), and Trolox
equivalent antioxidant capacity (TEAC) (1.01 ± 0.01 mmol TE/g extract) assays. This
contrasted with C. nutans which showed lower antioxidant activities owing to its lower TPC
and TFC. Correlation analysis revealed significant correlations (p < 0.05, r = 0.915 - 0.985)
between both TPC and TFC in S. crispus and antioxidant activities. However, only TPC of C.
nutans showed a significant correlation with FRAP values (r = 0.934). Further tentative
identification of the constituents in the extracts using HPLC-ESI-QToF-MS/MS revealed the
existence of 20 polyphenolic compounds in both S. crispus and C. nutans, which were likely
responsible for their antioxidant activities. In addition, 15 polyphenolic compounds classified
as chalcones, isoflavanoids, flavones, and flavonols have not been previously reported in both
species. The methanolic extracts of both species yielded a higher content of antioxidants, with
S. crispus offering a richer source of dietary antioxidants as compared to C. nutans. However,
further study is needed to identify their bioactivities in relation to their bioactive components.

Matched MeSH terms: Flavones
Rational discovery of dengue type 2 non-competitive inhibitors

Heh CH, Othman R, Buckle MJ, Sharifuddin Y, Yusof R, Rahman NA

Chem Biol Drug Des, 2013 Jul;82(1):1-11.
PMID: 23421589 DOI: 10.1111/cbdd.12122

Various works have been carried out in developing therapeutics against dengue. However, to date, no effective vaccine or anti-dengue agent has yet been discovered. The development of protease inhibitors is considered as a promising option, but most previous works have involved competitive inhibition. In this study, we focused on rational discovery of potential anti-dengue agents based on non-competitive inhibition of DEN-2 NS2B/NS3 protease. A homology model of the DEN-2 NS2B/NS3 protease (using West Nile Virus NS2B/NS3 protease complex, 2FP7, as the template) was used as the target, and pinostrobin, a flavanone, was used as the standard ligand. Virtual screening was performed involving a total of 13 341 small compounds, with the backbone structures of chalcone, flavanone, and flavone, available in the ZINC database. Ranking of the resulting compounds yielded compounds with higher binding affinities compared with the standard ligand. Inhibition assay of the selected top-ranking compounds against DEN-2 NS2B/NS3 proteolytic activity resulted in significantly better inhibition compared with the standard and correlated well with in silico results. In conclusion, via this rational discovery technique, better inhibitors were identified. This method can be used in further work to discover lead compounds for anti-dengue agents.

Matched MeSH terms: Flavones/pharmacology; Flavones/therapeutic use; Flavones/chemistry*
Differentiation of Ficus deltoidea varieties and chemical marker determination by UHPLC-TOFMS metabolomics for establishing quality control criteria of this popular Malaysian medicinal herb

Afzan A, Kasim N, Ismail NH, Azmi N, Ali AM, Mat N, et al.

Metabolomics, 2019 Mar 04;15(3):35.
PMID: 30830457 DOI: 10.1007/s11306-019-1489-2

BACKGROUND: Ficus deltoidea Jack (Moraceae) is a plant used in Malaysia for various diseases including as a supplement in diabetes management. Morphology distinction of the 7 main varieties (var. angustifolia, var. bilobata, var. deltoidea, var. intermedia, var. kunstleri, var. motleyana and var. trengganuensis) is challenging due to the extreme leaf heterophylly and unclear varietal boundaries, making it difficult for quality control of F. deltoidea products.
OBJECTIVE: We aimed to compare the phytochemical composition of 7 varieties growing in different conditions at various geographical locations. We also aimed to establish the quality control markers for the authentication of these varieties.
METHODS: We applied untargeted UHPLC-TOFMS metabolomics to discriminate 100 leaf samples of F. deltoidea collected from 6 locations in Malaysia. A genetic analysis on 21 leaf samples was also performed to validate the chemotaxonomy differentiation.
RESULTS: The PCA and HCA analysis revealed the existence of 3 chemotypes based on the differentiation in the flavonoid content. The PLS-DA analysis identified 15 glycosylated flavone markers together with 1 furanocoumarin. These markers were always consistent for the respective varieties, regardless of the geographical locations and growing conditions. The chemotaxonomy differentiation was in agreement with the DNA sequencing. In particular, var. bilobata accession which showed divergent morphology was also differentiated by the chemical fingerprints and genotype.
CONCLUSION: Chemotype differentiation based on the flavonoid fingerprints along with the proposed markers provide a powerful identification tool to complement morphology and genetic analyses for the quality control of raw materials and products from F. deltoidea.

Matched MeSH terms: Flavones
Mechanism of vasorelaxation induced by 3'-hydroxy-5,6,7,4'-tetramethoxyflavone in the rats aortic ring assay

Tan CS, Yam MF

Naunyn Schmiedebergs Arch Pharmacol, 2018 06;391(6):561-569.
PMID: 29552696 DOI: 10.1007/s00210-018-1481-9

Previous studies have demonstrated that 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (TMF) content in Orthosiphon stamineus fractions correlate with its vasorelaxation activity. Even with the availability of previous studies, there is still very little information on the vasorelaxation effect of TMF, and few scientific studies have been carried out. Therefore, the present study was designed to investigate the vasorelaxation activity and mechanism of action of the TMF. The vasorelaxation activity and the underlying mechanisms of TMF were evaluated on thoracic aortic rings isolated from Sprague Dawley rats. TMF caused the relaxation of aortic rings with endothelium pre-contracted with phenylephrine. However, the vasorelaxant effect of TMF was significantly decreased in PE-primed endothelium-denuded and potassium chloride-primed endothelium-intact aortic rings. In the presence of Nω-nitro-L-arginine methyl ester, methylene blue, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, indomethacin, tetraethylammonium, 4-aminopyridine, barium chloride, atropine and propranolol, the relaxation stimulated by TMF was significantly reduced. TMF was also found to reduce Ca2+ release from sarcoplasmic reticulum (via IP3R) and block calcium channels (VOCC). The present study demonstrates the vasorelaxant effect of TMF involves NO/sGC/cGMP and prostacyclin pathways, calcium and potassium channels and muscarinic and beta-adrenergic receptors.

Matched MeSH terms: Flavones/pharmacology*
Fulltext Cudraflavone C Induces Tumor-Specific Apoptosis in Colorectal Cancer Cells through Inhibition of the Phosphoinositide 3-Kinase (PI3K)-AKT Pathway

Soo HC, Chung FF, Lim KH, Yap VA, Bradshaw TD, Hii LW, et al.

PLoS One, 2017;12(1):e0170551.
PMID: 28107519 DOI: 10.1371/journal.pone.0170551

Cudraflavone C (Cud C) is a naturally-occurring flavonol with reported anti-proliferative activities. However, the mechanisms by which Cud C induced cytotoxicity have yet to be fully elucidated. Here, we investigated the effects of Cud C on cell proliferation, caspase activation andapoptosis induction in colorectal cancer cells (CRC). We show that Cud C inhibits cell proliferation in KM12, Caco-2, HT29, HCC2998, HCT116 and SW48 CRC but not in the non-transformed colorectal epithelial cells, CCD CoN 841. Cud C induces tumor-selective apoptosis via mitochondrial depolarization and activation of the intrinsic caspase pathway. Gene expression profiling by microarray analyses revealed that tumor suppressor genes EGR1, HUWE1 and SMG1 were significantly up-regulated while oncogenes such as MYB1, CCNB1 and GPX2 were down-regulated following treatment with Cud C. Further analyses using Connectivity Map revealed that Cud C induced a gene signature highly similar to that of protein synthesis inhibitors and phosphoinositide 3-kinase (PI3K)-AKT inhibitors, suggesting that Cud C might inhibit PI3K-AKT signaling. A luminescent cell free PI3K lipid kinase assay revealed that Cud C significantly inhibited p110β/p85α PI3K activity, followed by p120γ, p110δ/p85α, and p110α/p85α PI3K activities. The inhibition by Cud C on p110β/p85α PI3K activity was comparable to LY-294002, a known PI3K inhibitor. Cud C also inhibited phosphorylation of AKT independent of NFκB activity in CRC cells, while ectopic expression of myristoylated AKT completely abrogated the anti-proliferative effects, and apoptosis induced by Cud C in CRC. These findings demonstrate that Cud C induces tumor-selective cytotoxicity by targeting the PI3K-AKT pathway. These findings provide novel insights into the mechanism of action of Cud C, and indicate that Cud C further development of Cud C derivatives as potential therapeutic agents is warranted.

Matched MeSH terms: Flavones/pharmacology*
Fulltext Evaluation of anti-bacterial and anti-oxidant potential of andrographolide and echiodinin isolated from callus culture of Andrographis paniculata Nees

Arifullah M, Namsa ND, Mandal M, Chiruvella KK, Vikrama P, Gopal GR

Asian Pac J Trop Biomed, 2013 Aug;3(8):604-10; discussion 609-10.
PMID: 23905016 DOI: 10.1016/S2221-1691(13)60123-9

To evaluate the anti-bacterial and anti-oxidant activity of andrographolide (AND) and echiodinin (ECH) of Andrographis paniculata.

Matched MeSH terms: Flavones/pharmacology*
Fulltext Platelet-activating factor (PAF) antagonistic activity of a new biflavonoid from Garcinia nervosa var. pubescens King

Jalil J, Jantan I, Ghani AA, Murad S

Molecules, 2012 Sep 10;17(9):10893-901.
PMID: 22964504 DOI: 10.3390/molecules170910893

The methanol extract of the leaves of Garcinia nervosa var. pubescens King, which showed strong inhibitory effects on platelet-activating factor (PAF) receptor binding, was subjected to bioassay-guided isolation to obtain a new biflavonoid, II-3,I-5, II-5,II-7,I-4',II-4'-hexahydroxy-(I-3,II-8)-flavonylflavanonol together with two known flavonoids, 6-methyl-4'-methoxyflavone and acacetin. The structures of the compounds were elucidated by spectroscopic methods. The compounds were evaluated for their ability to inhibit PAF receptor binding to rabbit platelets using ³H-PAF as a ligand. The biflavonoid and acacetin showed strong inhibition with IC₅₀ values of 28.0 and 20.4 µM, respectively. The results suggest that these compounds could be responsible for the strong PAF antagonistic activity of the plant.

Matched MeSH terms: Flavones/pharmacology; Flavones/chemistry
Fulltext Lamiaceae: An Insight on Their Anti-Allergic Potential and Its Mechanisms of Action

Sim LY, Abd Rani NZ, Husain K

Front Pharmacol, 2019;10:677.
PMID: 31275149 DOI: 10.3389/fphar.2019.00677

The prevalence of allergic diseases such as asthma, allergic rhinitis, food allergy and atopic dermatitis has increased dramatically in recent decades. Conventional therapies for allergy can induce undesirable effects and hence patients tend to seek alternative therapies like natural compounds. Considering the fact above, there is an urgency to discover potential medicinal plants as future candidates in the development of novel anti-allergic therapeutic agents. The Lamiaceae family, or mint family, is a diverse plant family which encompasses more than 7,000 species and with a cosmopolitan distribution. A number of species from this family has been widely employed as ethnomedicine against allergic inflammatory skin diseases and allergic asthma in traditional practices. Phytochemical analysis of the Lamiaceae family has reported the presence of flavonoids, flavones, flavanones, flavonoid glycosides, monoterpenes, diterpenes, triterpenoids, essential oil and fatty acids. Numerous investigations have highlighted the anti-allergic activities of Lamiaceae species with their active principles and crude extracts. Henceforth, this review has the ultimate aim of compiling the up-to-date (2018) findings of published scientific information about the anti-allergic activities of Lamiaceae species. In addition, the botanical features, medicinal uses, chemical constituents and toxicological studies of Lamiaceae species were also documented. The method employed for data collection in this review was mainly the exploration of the PubMed, Ovid and Scopus databases. Additional research studies were obtained from the reference lists of retrieved articles. This comprehensive summarization serves as a useful resource for a better understanding of Lamiaceae species. The anti-allergic mechanisms related to Lamiaceae species are also reviewed extensively which aids in future exploration of the anti-allergic potential of Lamiaceae species.

Matched MeSH terms: Flavones
Fulltext Flavonoids as Natural Anti-Inflammatory Agents Targeting Nuclear Factor-Kappa B (NFκB) Signaling in Cardiovascular Diseases: A Mini Review

Choy KW, Murugan D, Leong XF, Abas R, Alias A, Mustafa MR

Front Pharmacol, 2019;10:1295.
PMID: 31749703 DOI: 10.3389/fphar.2019.01295

Cardiovascular diseases (CVDs) such as angina, hypertension, myocardial ischemia, and heart failure are the leading causes of morbidity and mortality worldwide. One of the major transcription factors widely associated with CVDs is nuclear factor-kappa B (NFκB). NFκB activation initiates the canonical and non-conical pathways that promotes activation of transcription factors leading to inflammation, such as leukocyte adhesion molecules, cytokines, and chemokines. Flavonoids are bioactive polyphenolic compounds found abundantly in various fruits, vegetables, beverages (tea, coffee), nuts, and cereal products with cardiovascular protective properties. Flavonoids can be classified into six subgroups based on their chemical structures: flavanones, flavones, flavonols, flavan-3-ols, isoflavones, and anthocyanidins. As NFκB inhibitors, these flavonoids may modulate the expression of pro-inflammatory genes leading to the attenuation of the inflammatory responses underlying various cardiovascular pathology. This review presents an update on the anti-inflammatory actions of flavonoids via inhibition of NFκB mechanism supporting the therapeutic potential of these natural compounds in various CVDs.

Matched MeSH terms: Isoflavones; Flavones
Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells

Phan CW, Sabaratnam V, Bovicelli P, Righi G, Saso L

Biofactors, 2016 Nov 12;42(6):591-599.
PMID: 27193378 DOI: 10.1002/biof.1296

Negletein has been shown to have therapeutic potential for inflammation-associated diseases, but its effect on neurite outgrowth is still unknown. The present study showed that negletein alone did not trigger PC12 cells to differentiate and extend neurites. When compared with the cells in the untreated control, a significant (P

Matched MeSH terms: Flavones/pharmacology*
Luteolin and apigenin derived glycosides from Alphonsea elliptica abrogate LPS-induced inflammatory responses in human plasma

Attiq A, Jalil J, Husain K, Mohamad HF, Ahmad A

J Ethnopharmacol, 2021 Jul 15;275:114120.
PMID: 33857595 DOI: 10.1016/j.jep.2021.114120

ETHNOPHARMACOLOGICAL RELEVANCE: Numerous Alphonsea species including Alphonsea elliptica (mempisang) leaves and fruits are indigenously used in inflammatory conditions such as postpartum swelling and rheumatism in southeast Asian countries. In our previous in-vitro findings, A. elliptica methanol extract exhibited platelet-activating factor inhibition, suggesting the presence of phyto-constituents with anti-inflammatory potential.
AIM OF THE STUDY: However, so far there is no literature available on the anti-inflammatory activity of this species. Henceforth, based on the above background and our previous laboratory findings, we hypothesize that phytoconstituents of A. elliptica could possess anti-inflammatory potential against inflammatory mediators including prostaglandin-E2 (PGE2), cyclooxegenase-2 (COX-2) and cytokines (IL-1β and IL-6).
MATERIALS AND METHODS: Vacuum and column chromatography techniques were employed for the isolation of phytoconstituents. The structure elucidation was carried out using HRESI-MS, 1H and 13C-NMR analysis and compared with the published literature. For cytotoxicity analysis, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was performed on peripheral blood mononuclear cells. In-vitro anti-inflammatory activities were evaluated against the levels of PGE2, COX-2, IL-1β and IL-6 in lipopolysaccharide (LPS)-induced human plasma using enzyme-linked immunosorbent assay and radioimmunoassay.
RESULTS: Unprecedentedly, chromatographic purification of methanolic leaves extract afforded five flavones namely vitexin, isovitexin, orientin, isoorientin, schaftoside with three flavanols; kaempferol, myricetin and rutin from A elliptica. In cell viability analysis, isolates did not present cytotoxicity up to 50 μM. In anti-inflammatory evaluation, orientin and isoorientin exhibited strong (≥70%), while isovitexin and vitexin produced strong to moderate (50-69%) PGE2, COX-2, IL-1β and IL-6 inhibition at 25 and 50 μM. Isoorientin, orientin, isovitexin, and vitexin showed significant (p

Matched MeSH terms: Flavones
Fulltext Computational Approach Towards Exploring Potential Anti-Chikungunya Activity of Selected Flavonoids

Seyedi SS, Shukri M, Hassandarvish P, Oo A, Shankar EM, Abubakar S, et al.

Sci Rep, 2016 Apr 13;6:24027.
PMID: 27071308 DOI: 10.1038/srep24027

Chikungunya virus (CHIKV) is a mosquito-borne alphavirus that causes chikungunya infection in humans. Despite the widespread distribution of CHIKV, no antiviral medication or vaccine is available against this virus. Therefore, it is crucial to find an effective compound to combat CHIKV. We aimed to predict the possible interactions between non-structural protein 3 (nsP) of CHIKV as one of the most important viral elements in CHIKV intracellular replication and 3 potential flavonoids using a computational approach. The 3-dimensional structure of nsP3 was retrieved from the Protein Data Bank, prepared and, using AutoDock Vina, docked with baicalin, naringenin and quercetagetin as ligands. The first-rated ligand with the strongest binding affinity towards the targeted protein was determined based on the minimum binding energy. Further analysis was conducted to identify both the active site of the protein that reacts with the tested ligands and all of the existing intermolecular bonds. Compared to the other ligands, baicalin was identified as the most potential inhibitor of viral activity by showing the best binding affinity (-9.8 kcal/mol). Baicalin can be considered a good candidate for further evaluation as a potentially efficient antiviral against CHIKV.

Matched MeSH terms: Flavones
Modulation of vascular reactivity in normal, hypertensive and diabetic rat aortae by a non-antioxidant flavonoid

Ajay M, Achike FI, Mustafa MR

Pharmacol Res, 2007 May;55(5):385-91.
PMID: 17317209

In this study, we report the effects of a non-antioxidant flavonoid flavone on vascular reactivity in Wistar-Kyoto (WKY) rat isolated aortae. Whether flavone directly modulates vascular reactivity in spontaneously hypertensive rat (SHR) and streptozotocin-induced diabetic-WKY rat isolated aortae was also determined. Thoracic aortic rings were mounted in organ chambers and exposed to various drug treatments in the presence of flavone (10 microM) or its vehicle (DMSO), which served as control. Pretreatment with flavone enhanced relaxant effects to endothelium-dependent vasodilator acetylcholine (ACh) and attenuated contractile effects to alpha(1)-receptor agonist phenylephrine (PE) in WKY aortae compared to those observed in control aortic rings. Flavone had no effect on relaxations to ACh in WKY aortae incubated with either L-NAME or methylene blue, but enhanced relaxations to ACh in WKY aortae incubated with indomethacin or partially depolarized with KCl. Relaxations to ACh are totally abolished in both control or flavone pretreated endothelium-denuded WKY aortae. Flavone attenuated the inhibition by beta-NADH of ACh-induced relaxation in WKY aortae, but it had no significant effect on the transient contractions induced by beta-NADH nor the pyrogallol-induced abolishment of ACh-induced relaxation in WKY aortae. Flavone enhanced endothelium-independent relaxation to sodium nitroprusside (SNP) in both endothelium-intact and -denuded WKY aortae. Flavone enhanced relaxation to ACh and SNP as well as attenuated contractile effects to PE in SHR and diabetic aortae, a finding similar to that observed in normal WKY aortae. From these results, we conclude that flavone modulates vascular reactivity in normal as well as hypertensive and diabetic aortae. These effects of flavone results probably through enhanced bioactivity of nitric oxide released from the endothelium.

Matched MeSH terms: Flavones

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