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Fulltext Anti-inflammatory effects of Polygonum minus (Huds) extract (Lineminus™) in in-vitro enzyme assays and carrageenan induced paw edema

George A, Chinnappan S, Chintamaneni M, Kotak C V, Choudhary Y, Kueper T, et al.

BMC Complement Altern Med, 2014;14:355.
PMID: 25252832 DOI: 10.1186/1472-6882-14-355

The study was aimed to evaluate the anti-inflammatory activity of ethanolic and aqueous extracts of Polygonum minus (Huds) using in vitro and in vivo approaches.

Matched MeSH terms: Lipoxygenase/analysis; Lipoxygenase/metabolism
Fulltext Ardisia crispa roots inhibit cyclooxygenase and suppress angiogenesis

Hamsin DE, Hamid RA, Yazan LS, Taib CN, Yeong LT

BMC Complement Altern Med, 2014;14:102.
PMID: 24641961 DOI: 10.1186/1472-6882-14-102

In our previous studies conducted on Ardisia crispa roots, it was shown that Ardisia crispa root inhibited inflammation-induced angiogenesis in vivo. The present study was conducted to identify whether the anti-angiogenic properties of Ardisia crispa roots was partly due to either cyclooxygenase (COX) or/and lipoxygenase (LOX) activity inhibition in separate in vitro studies.

Matched MeSH terms: Lipoxygenase/metabolism
Fulltext In-vitro and in-vivo validation of ethnopharmacological uses of methanol extract of Isodon rugosus Wall. ex Benth. (Lamiaceae)

Janbaz KH, Arif J, Saqib F, Imran I, Ashraf M, Zia-Ul-Haq M, et al.

BMC Complement Altern Med, 2014 Feb 22;14:71.
PMID: 24559094 DOI: 10.1186/1472-6882-14-71

BACKGROUND: Isodon rugosus is used in folk Pakistan traditional practices to cure ailments related to gastrointestinal, respiratory and cardiovascular problems. Present study was undertaken to validate these folkloric uses.
METHODS: A crude methanol extract of the aerial parts of Isodon rugosus (Ir.Cr.) was used for both in vitro and in vivo experiments. The plant extract was tested on isolated rabbit jejunum preparations for possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract. Acetylcholinesterase and butyrylcholinesterase inhibitory activities of Ir.Cr were also determined as well as its antioxidant activity. The in vivo antiemetic activity of the extract was evaluated by using the chick emesis model, while the analgesic and antipyretic activities were conducted on albino mice.
RESULTS: The application of the crude extract of I. rugosus to isolated rabbit jejunum preparations exhibited relaxant effect (0.01-0.3 mg/ml). The Ir.Cr also relaxed K+(80 m M)-induced spastic contractions in isolated rabbit jejunum preparations and shifted the Ca+2 concentration response curves towards right (0.01-0.3 mg/ml). Similarly, the extract, when applied to the isolated rabbit tracheal preparations relaxed the carbachol (1 μM)--as well as K+ (80 mM)-induced contractions in a concentration range of 0.01-1.0 mg/ml. Moreover, it also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 μM)- and K+ (80 mM)-induced contractions in isolated rabbit aorta preparations. The Ir.Cr (80 mg/kg) demonstrated antipyretic activity on pyrogen-induced pyrexia in rabbits as compared to aspirin as standard drug. The Ir.Cr also exhibited anti-oxidant as well as inhibitory effect on acetyl- and butyryl-cholinesterase and lipoxygenase (0.5 mg/ml).
CONCLUSIONS: The observed relaxant effect on isolated rabbit jejunum, trachea and aorta preparations caused by Ir.Cr is possibly to be mediated through Ca+2 channel blockade and therefore may provided scientific basis to validate the folkloric uses of the plant in the management of gastrointestinal, respiratory and cardiovascular ailments. The observed antioxidant activity as well as the lipoxygenase inhibitory activity may validate its traditional use in pain and inflammations.

Matched MeSH terms: Lipoxygenase Inhibitors/pharmacology; Lipoxygenase Inhibitors/therapeutic use
Effects of iridoids on lipoxygenase and hyaluronidase activities and their activation by beta-glucosidase in the presence of amino acids

Ling SK, Tanaka T, Kouno I

Biol Pharm Bull, 2003 Mar;26(3):352-6.
PMID: 12612446

Enzyme inhibitory activities of 14 iridoids previously obtained from two Malaysian medicinal plants, Saprosma scortechinii and Rothmannia macrophylla, were evaluated in vitro using soybean lipoxygenase and bovine testis hyaluronidase. Most of the iridoids, including asperulosidic acid, paederosidic acid, and an epimeric mixture of gardenogenins A and B, did not show any effect on the enzyme activities, except for the bis-iridoids, which inhibited the lipoxygenase activity with their IC(50) values of approximately 1.3 times that of a known inhibitor, fisetin. Structural modification of asperulosidic acid and paederosidic acid through enzymatic hydrolysis by beta-glucosidase resulted in their inhibition towards the enzyme activities, and these activities were enhanced by the presence of some amino acids (lysine, leucine or glutamic acid) or ammonium acetate. Mixtures of gardenogenins A and B; isomers of non-glucosidic iridoids, incubated with amino acid or ammonium acetate did not show any inhibitory effect on the enzyme activities during the 6 h incubation period, except for lysine where spontaneous reaction between the iridoids and amino acid resulted in the inhibition of lipoxygenase activity. The results from these biomimetic reactions suggested that the iridoid aglycons and the intermediates formed by these reactive species could inhibit the enzyme activities, and thus substantiate previous reports that the formation of iridoidal aglycons is a prerequisite for the iridoid glycosides to demonstrate some of the biological activities. In addition, the results also indicated that it is worthwhile to further explore these intermediates as potential anti-inflammatory agents.

Matched MeSH terms: Lipoxygenase/metabolism*
Pharmacological evaluation and docking studies of α,β-unsaturated carbonyl based synthetic compounds as inhibitors of secretory phospholipase A₂, cyclooxygenases, lipoxygenase and proinflammatory cytokines

Bukhari SN, Lauro G, Jantan I, Bifulco G, Amjad MW

Bioorg Med Chem, 2014 Aug 1;22(15):4151-61.
PMID: 24938495 DOI: 10.1016/j.bmc.2014.05.052

Arachidonic acid and its metabolites have generated high level of interest among researchers due to their vital role in inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as synergistic anti-inflammatory effect. A series of novel α,β-unsaturated carbonyl based compounds were synthesized and evaluated for their inhibitory activity on secretory phospholipase A₂ (sPLA₂), cyclooxygenases (COX), soybean lipoxygenase (LOX) in addition to proinflammatory cytokines comprising IL-6 and TNF-α. Six α,β-unsaturated carbonyl based compounds (2, 3, 4, 12, 13 and 14) exhibited strong inhibition of sPLA₂ activity, with IC₅₀ values in the range of 2.19-8.76 μM. Nine compounds 1-4 and 10-14 displayed inhibition of COX-1 with IC₅₀ values ranging from 0.37 to 1.77 μM (lower than that of reference compound), whereas compounds 2, 10, 13 and 14 strongly inhibited the COX-2. The compounds 10-14 exhibited strong inhibitory activity against LOX enzyme. All compounds were evaluated for the inhibitory activities against LPS-induced TNF-α and IL-6 release in the macrophages. On the basis of screening results, five active compounds 3, 4, 12, 13 and 14 were found strong inhibitors of TNF-α and IL-6 release in a dose-dependent manner. Molecular docking experiments were performed to clarify the molecular aspects of the observed COX and LOX inhibitory activities of the investigated compounds. Present findings increases the possibility that these α,β-unsaturated carbonyl based compounds might serve as beneficial starting point for the design and development of improved anti-inflammatory agents.

Matched MeSH terms: Lipoxygenase/metabolism; Lipoxygenase/chemistry*; Lipoxygenase Inhibitors/chemical synthesis; Lipoxygenase Inhibitors/pharmacology; Lipoxygenase Inhibitors/chemistry*
Bioassay-guided identification of an anti-inflammatory prenylated acylphloroglucinol from Melicope ptelefolia and molecular insights into its interaction with 5-lipoxygenase

Shaari K, Suppaiah V, Wai LK, Stanslas J, Tejo BA, Israf DA, et al.

Bioorg Med Chem, 2011 Nov 1;19(21):6340-7.
PMID: 21958738 DOI: 10.1016/j.bmc.2011.09.001

A bioassay-guided investigation of Melicope ptelefolia Champ ex Benth (Rutaceae) resulted in the identification of an acyphloroglucinol, 2,4,6-trihydroxy-3-geranylacetophenone or tHGA, as the active principle inhibiting soybean 15-LOX. The anti-inflammatory action was also demonstrated on human leukocytes, where the compound showed prominent inhibitory activity against human PBML 5-LOX, with an IC(50) value of 0.42 μM, very close to the effect produced by the commonly used standard, NDGA. The compound concentration-dependently inhibited 5-LOX product synthesis, specifically inhibiting cysteinyl leukotriene LTC(4) with an IC(50) value of 1.80 μM, and showed no cell toxicity effects. The anti-inflammatory action does not seem to proceed via redox or metal chelating mechanism since the compound tested negative for these bioactivities. Further tests on cyclooxygenases indicated that the compound acts via a dual LOX/COX inhibitory mechanism, with greater selectivity for 5-LOX and COX-2 (IC(50) value of 0.40 μM). The molecular features that govern the 5-LOX inhibitory activity was thus explored using in silico docking experiments. The residues Ile 553 and Hie 252 were the most important residues in the interaction, each contributing significant energy values of -13.45 (electrostatic) and -5.40 kcal/mol (electrostatic and Van der Waals), respectively. The hydroxyl group of the phloroglucinol core of the compound forms a 2.56Å hydrogen bond with the side chain of the carboxylate group of Ile 553. Both Ile 553 and Hie 252 are crucial amino acid residues which chelate with the metal ion in the active site. Distorting the geometry of these ligands could be the reason for the inhibition activity shown by tHGA. The molecular simulation studies supported the bioassay results and served as a good model for understanding the way tHGA binds in the active site of human 5-LOX enzyme.

Matched MeSH terms: Arachidonate 5-Lipoxygenase/metabolism*; Lipoxygenase Inhibitors/isolation & purification*; Lipoxygenase Inhibitors/pharmacology; Lipoxygenase Inhibitors/chemistry
Synthesis of furocoumarin-stilbene hybrids as potential multifunctional drugs against multiple biochemical targets associated with Alzheimer's disease

Agbo EN, Gildenhuys S, Choong YS, Mphahlele MJ, More GK

Bioorg Chem, 2020 08;101:103997.
PMID: 32554280 DOI: 10.1016/j.bioorg.2020.103997

A series of furocoumarin-stilbene hybrids has been synthesized and evaluated in vitro for inhibitory effect against acetylcholinesterase (AChE), butyrylcholinestarase (BChE), β-secretase, cyclooxygenase-2 (COX-2), and lipoxygenase-5 (LOX-5) activities including free radical-scavenging properties. Among these hybrids, 8-(3,5-dimethoxyphenyl)-4-(3,5-dimethoxystyryl)furochromen-2-one 4h exhibited significant anticholinesterase activity and inhibitory effect against β-secretase, COX-2 and LOX-5 activities. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and an in vitro cell-based antioxidant activity assay involving lipopolysaccharide induced reactive oxygen species production revealed that 4h has capability of scavenging free radicals. Molecular docking into AChE, BChE, β-secretase, COX-2 and LOX-5 active sites has also been performed.

Matched MeSH terms: Lipoxygenase Inhibitors/pharmacology
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1

Ahmad W, Kumolosasi E, Jantan I, Bukhari SN, Jasamai M

Chem Biol Drug Des, 2014 Jun;83(6):670-81.
PMID: 24406103 DOI: 10.1111/cbdd.12280

Arachidonic acid and its metabolites have generated a heightened interest due to their significant role in inflammation. Inhibiting the enzymes involved in arachidonic acid metabolism has been considered as the synergistic anti-inflammatory effect. A series of novel curcumin diarylpentanoid analogues were synthesized and evaluated for their inhibitory effects on activity of secretory phospholipase A2 , cyclooxygenases, soybean lipo-oxygenase as well as microsomal prostaglandin E synthase-1. Among the curcumin analogues, compounds 3, 6, 9, 12, and 17 exhibited strong inhibition of secretory phospholipase A2 activity, with IC50 values ranging from 5.89 to 11.02 μm. Seven curcumin analogues 1, 3, 6, 7, 9, 11, and 12 showed inhibition of cyclooxygenases-2 with IC50 values in the range of 46.11 to 94.86 μm, which were lower than that of curcumin. Compounds 3, 6, 7, 12, and 17 showed strong inhibition of lipo-oxygenase enzyme activity. Preliminary screening of diarylpentanoid curcumin analogues for microsomal prostaglandin E synthase-1 activity revealed that four diarylpentanoid curcumin analogues 5, 6, 7, and 13 demonstrated higher inhibition of microsomal prostaglandin E synthase-1 activity with IC50 ranging from 2.41 to 4.48 μm, which was less than that of curcumin. The present results suggest that some of these diarylpentanoid analogues were able to inhibit the activity of these enzymes. This raises the possibility that diarylpentanoid analogues of curcumin might serve as useful starting point for the design of improved anti-inflammatory agents.

Matched MeSH terms: Lipoxygenase/metabolism*
Fulltext Inflammation Drives Alzheimer's Disease: Emphasis on 5-lipoxygenase Pathways

Siddiqui A, Akhtar S, Shah Z, Othman I, Kumari Y

Curr Neuropharmacol, 2021;19(6):885-895.
PMID: 32972344 DOI: 10.2174/1570159X18666200924122732

It is a known fact that inflammation affects several physiological processes, including the functioning of the central nervous system. Additionally, impairment of lipid mechanisms/pathways have been associated with a number of neurodegenerative disorders and Alzheimer's Disease (AD) is one of them. However, much attention has been given to the link between tau and beta- amyloid hypothesis in AD pathogenesis/prognosis. Increasing evidences suggest that biologically active lipid molecules could influence the pathophysiology of AD via a different mechanism of inflammation. This review intends to highlight the role of inflammatory responses in the context of AD with the emphasis on biochemical pathways of lipid metabolism enzyme, 5-lipoxygenase (5- LO).

Matched MeSH terms: Arachidonate 5-Lipoxygenase*
Fulltext Studies of synthetic chalcone derivatives as potential inhibitors of secretory phospholipase A2, cyclooxygenases, lipoxygenase and pro-inflammatory cytokines

Jantan I, Bukhari SN, Adekoya OA, Sylte I

Drug Des Devel Ther, 2014;8:1405-18.
PMID: 25258510 DOI: 10.2147/DDDT.S67370

Arachidonic acid metabolism leads to the generation of key lipid mediators which play a fundamental role during inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as a synergistic anti-inflammatory effect with enhanced spectrum of activity. A series of 1,3-diphenyl-2-propen-1-one derivatives were investigated for anti-inflammatory related activities involving inhibition of secretory phospholipase A2, cyclooxygenases, soybean lipoxygenase, and lipopolysaccharides-induced secretion of interleukin-6 and tumor necrosis factor-alpha in mouse RAW264.7 macrophages. The results from the above mentioned assays exhibited that the synthesized compounds were effective inhibitors of pro-inflammatory enzymes and cytokines. The results also revealed that the chalcone derivatives with 4-methlyamino ethanol substitution seem to be significant for inhibition of enzymes and cytokines. Molecular docking experiments were carried out to elucidate the molecular aspects of the observed inhibitory activities of the investigated compounds. Present findings increase the possibility that these chalcone derivatives might serve as a beneficial starting point for the design and development of improved anti-inflammatory agents.

Matched MeSH terms: Lipoxygenase/metabolism; Lipoxygenase Inhibitors/chemical synthesis; Lipoxygenase Inhibitors/pharmacology*; Lipoxygenase Inhibitors/chemistry
Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood

Ahmad S, Israf DA, Lajis NH, Shaari K, Mohamed H, Wahab AA, et al.

Eur J Pharmacol, 2006 May 24;538(1-3):188-94.
PMID: 16650843

Some chalcones, such as hydroxychalcones have been reported previously to inhibit major pro-inflammatory mediators such as nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and reactive oxygen species production by suppressing inducible enzyme expression via inhibition of the mitogen-activated protein kinase (MAPK) pathway and nuclear translocation of critical transcription factors. In this report, the effects of cardamonin (2',4'-dihydroxy-6'-methoxychalcone), a chalcone that we have previously isolated from Alpinia rafflesiana, was evaluated upon two cellular systems that are repeatedly used in the analysis of anti-inflammatory bioactive compounds namely RAW 264.7 cells and whole blood. Cardamonin inhibited NO and PGE(2) production from lipopolysaccharide- and interferon-gamma-induced RAW cells and whole blood with IC(50) values of 11.4 microM and 26.8 microM, respectively. Analysis of thromboxane B(2) (TxB(2)) secretion from whole blood either stimulated via the COX-1 or COX-2 pathway revealed that cardamonin inhibits the generation of TxB(2) via both pathways with IC(50) values of 2.9 and 1.1 microM, respectively. Analysis of IC(50) ratios determined that cardamonin was more COX-2 selective in its inhibition of TxB(2) with a ratio of 0.39. Cardamonin also inhibited the generation of intracellular reactive oxygen species and secretion of TNF-alpha from RAW 264.7 cells in a dose responsive manner with IC(50) values of 12.8 microM and 4.6 microM, respectively. However, cardamonin was a moderate inhibitor of lipoxygenase activity when tested in an enzymatic assay system, in which not a single concentration tested was able to cause an inhibition of more than 50%. Our results suggest that cardamonin acts upon major pro-inflammatory mediators in a similar fashion as described by previous work on other closely related synthetic hydroxychalcones and strengthens the conclusion of the importance of the methoxyl moiety substitution on the 4' or 6' locations of the A benzene ring.

Matched MeSH terms: Lipoxygenase/metabolism
Bioactivity-guided fractionation of the lipoxygenase and cyclooxygenase inhibiting constituents from Chisocheton polyandrus Merr

Chan KY, Mohamad K, Ooi AJ, Imiyabir Z, Chung LY

Fitoterapia, 2012 Jul;83(5):961-7.
PMID: 22565147 DOI: 10.1016/j.fitote.2012.04.018

Lipoxygenase (LOX)-inhibiting compounds from the leaves of Chisocheton polyandrus Merr. were isolated in this study using a bioactivity-guided fractionation technique. Two dammarane triterpenoids, dammara-20,24-dien-3-one (1) (IC(50)=0.69±0.07 μM) and 24-hydroxydammara-20,25-dien-3-one (2) (IC(50)=1.11±0.38 μM), were isolated and identified based on the soybean LOX assay. Dammara-20,24-dien-3-one (1) exhibited dual inhibition of both human 5-LOX (IC(50)=24.27±2.92 μM) and cyclooxygenase-2 (COX-2) (IC(50)=3.17±0.90 μM), whereas 24-hydroxydammara-20,25-dien-3-one (2) did not exhibit any significant inhibitory effects. This report is the first to detail the inhibition of LOX and COX by both C. polyandrus and its isolated compounds.

Matched MeSH terms: Lipoxygenase/metabolism; Lipoxygenase Inhibitors/isolation & purification; Lipoxygenase Inhibitors/pharmacology*
Anti-inflammatory trends of new benzimidazole derivatives

Bukhari SN, Lauro G, Jantan I, Fei Chee C, Amjad MW, Bifulco G, et al.

Future Med Chem, 2016 Oct;8(16):1953-1967.
PMID: 27654499

In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A2, lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages.

Matched MeSH terms: Lipoxygenase
Atrovirinone inhibits pro-inflammatory mediator release from murine macrophages and human whole blood

Syahida A, Israf DA, Permana D, Lajis NH, Khozirah S, Afiza AW, et al.

Immunol Cell Biol, 2006 Jun;84(3):250-8.
PMID: 16509831

Many plant-derived natural compounds have been reported previously to inhibit the production of important pro-inflammatory mediators such as nitric oxide, prostaglandin E2, TNF-alpha and reactive oxygen species by suppressing inducible enzyme expression via inhibition of the mitogen-activated protein kinase pathway and nuclear translocation of critical transcription factors. This study evaluates the effects of atrovirinone [2-(1-methoxycarbonyl-4,6-dihydroxyphenoxy)-3-methoxy-5,6-di-(3-methyl-2-butenyl)-1,4-benzoquinone)], a benzoquinone that we have previously isolated from Garcinia atroviridis, on two cellular systems that are repeatedly used in the analysis of anti-inflammatory bioactive compounds, namely, RAW 264.7 macrophage cells and whole blood. Atrovirinone inhibited the production of both nitric oxide and prostaglandin E2 from LPS-induced and IFN-gamma-induced RAW 264.7 cells and whole blood, with inhibitory concentration (IC)50 values of 4.62 +/- 0.65 and 9.33 +/- 1.47 micromol/L, respectively. Analysis of thromboxane B2 (TXB2) secretion from whole blood stimulated by either the cyclooxygenase (COX)-1 or the COX-2 pathway showed that atrovirinone inhibits the generation of TXB2 by both pathways, with IC50 values of 7.41 +/- 0.92 and 2.10 +/- 0.48 micromol/L, respectively. Analysis of IC50 ratios showed that atrovirinone was more COX-2 selective in its inhibition of TXB2, with a ratio of 0.32. Atrovirinone also inhibited the generation of intracellular reactive oxygen species and the secretion of TNF-alpha from RAW 264.7 cells in a dose-responsive manner, with IC50 values of 5.99 +/- 0.62 and 11.56 +/- 0.04 micromol/L, respectively. Lipoxygenase activity was also moderately inhibited by atrovirinone. Our results suggest that atrovirinone acts on important pro-inflammatory mediators possibly by the inhibition of the nuclear factor-kappaB pathway and also by the inhibition of the COX/lipoxygenase enzyme activity.

Matched MeSH terms: Lipoxygenase/metabolism; Lipoxygenase/chemistry
Fulltext Ipomea aquatica crude extract inhibits lipoxygenase, hyaluronidase and xanthine oxidase activities

Muhammad Helmi Nadri, Kian, Kai Cheng, Pei, Ying Ong, Hong, Yeng L., Nor Zalina Othman, Nur Fashya Musa, et al.

Journal of Academia Universiti Teknologi MARA Negeri Sembilan, 2020;8(2):9-14.
MyJurnal

Ipomea aquatica, locally known as water spinach, is one of the most common vegetable consumed by
Malaysian. Based on previous studies, crude extract and phenolic compounds of I. aquatica exhibited
several biological activities including antioxidant, anti-microbial and anti-proliferative. The presence
of phenolic compounds in I. aquatica may contributed to their ability to inhibit enzymes, chelate
metals and scavenge free radicals. Currently, no study reported on anti-inflammatory activity of I.
aquatica with respect to lipoxygenase, hyaluronidase and xanthine oxidase enzymes. The present
study aims to enhance current knowledge on biological properties of I. aquatica crude extract
particularly on anti-inflammatory activity. Three enzymes that involve in inflammatory pathway were
selected in this study including lipoxygenase, hyaluronidase and xanthine oxidase. I. aquatica was
extracted in methanol and tested for lipoxygenase, hyaluronidase and xanthine oxidase at different
concentrations using direct enzyme inhibition assay. Lipoxygenase, hyaluronidase and xanthine
oxidase inhibitory activities of the methanol crude extract increased with increasing
concentration. Highest inhibition activity against lipoxygenase, hyaluronidase and xanthine oxidase
were observed at a concentration of 1000 µg/ml with inhibition of 87.18%, 95.36% and 78.38%,
respectively. Our finding in this study indicates potential anti-inflammatory activity of I. aquatica
crude extract through inhibition of lipoxygenase, hyaluronidase and xanthine oxidase.

Matched MeSH terms: Lipoxygenase
Fulltext Neuropharmacological evaluation on four traditional herbs used as nervine tonic and commonly available as Shankhpushpi in India

Sethiya NK, Nahata A, Singh PK, Mishra SH

J Ayurveda Integr Med, 2018 03 09;10(1):25-31.
PMID: 29530454 DOI: 10.1016/j.jaim.2017.08.012

BACKGROUND: Shankhpushpi is an Ayurvedic drug, widely used for its actions on the central nervous system, especially to improve intellect and boost memory. Four botanicals viz. Canscora decussata Schult. (CD), Clitorea ternatea Linn. (CT), Convolvulus pluricaulis Choisy. (CP) and Evolvulus alsinoides Linn. (EA) are considered as sources of Shankhpushpi by Indian practitioners on the basis of their morphological descriptions given in ancient texts.
OBJECTIVE: The present study was undertaken to evaluate the neuropharmacological effect of four herbs commonly identified as source of Shankhpushpi.
MATERIALS AND METHODS: Methanol extracts of all four varieties were tested and evaluated in vitro and in vivo for their neuropharmacological effects. Experiments such as protection against β-amyloid induced neurotoxicity on brain cell line (Neuro 2A), antioxidant potential, AchE (acetylcholinesterase enzyme) inhibition, and 5-LOX (lipoxygenase) enzyme inhibition were conducted for in vitro evaluation. For in vivo evaluation, scopolamine (0.3 mg/kg i.p.) induced memory retrieval using pole climbing apparatus and Morris water maze were performed in rat models.
RESULTS: It was found that protective effects of EA and CD against β-amyloid induced neurotoxicity in Neuro 2A cells were significantly higher than CT and CP. EA proved to be superior than other varieties on the basis of antioxidant activity, AchE inhibitory and LOX inhibitory activities. The preventive activity of EA on scopolamine induced memory retrieval in pole climbing and Morris water maze task in rats was found to be higher than that of CD, CT and CP.
CONCLUSION: EA has remarkable neuropharmacological effect as compared to other three varieties of Shankhpushpi. This effect may be attributed due to the presence of steroids (stigmasterol and betulinic acid), coumarins (scopoletin) and flavonoids (β-carotene and chlorogenic acid). Hence it can be used as a promising lead in development and management of neuronal disorders including Alzheimer's disease.

Matched MeSH terms: Lipoxygenase
Overproduction of lipoxygenase from Pseudomonas aeruginosa in Escherichia coli by auto-induction expression and its application in triphenylmethane dyes degradation

Lu J, Zhang C, Leong HY, Show PL, Lu F, Lu Z

J Biosci Bioeng, 2020 Mar;129(3):327-332.
PMID: 31585857 DOI: 10.1016/j.jbiosc.2019.09.006

In this study, the bacterial lipoxygenase (LOX) gene from Pseudomonas aeruginosa ATCC27853 (pse-LOX) was cloned, sequenced and heterologous expressed in Escherichia coli by auto-induction expression strategy. Production of the recombinant pse-LOX (pse-rLOX) gene up to 23,850 U/mL (264 mg pure protein/L bacterial culture fluid) was observed in the end of this process. To the best of our knowledge, this is the first attempt to manipulate LOX heterologous expression process using auto-induction expression approach, and it is the highest production of recombinant LOX compared with other reports. Subsequently, the resulted pse-rLOX was proved to efficiently degrade triphenylmethane dyes such as malachite green, brilliant green and aniline blue. Generally, an overproduction of the LOX from P. aeruginosa was observed in E. coli, and this recombinant gene is a potential candidate as biocatalyst for triphenylmethane dyes decolorization.

Matched MeSH terms: Lipoxygenase/genetics; Lipoxygenase/metabolism*
Mutation study for 9 genes in 23 unrelated patients with autosomal recessive congenital ichthyosis in Japan and Malaysia

Numata S, Teye K, Krol RP, Karashima T, Fukuda S, Matsuda M, et al.

J. Dermatol. Sci., 2015 Apr;78(1):82-5.
PMID: 25766764 DOI: 10.1016/j.jdermsci.2015.02.006
Matched MeSH terms: Arachidonate 12-Lipoxygenase/genetics*
Fulltext Mechanism(s) of action involved in the gastroprotective activity of Muntingia calabura

Zakaria ZA, Balan T, Suppaiah V, Ahmad S, Jamaludin F

J Ethnopharmacol, 2014 Feb 12;151(3):1184-1193.
PMID: 24380736 DOI: 10.1016/j.jep.2013.12.045

ETHNOPHARMACOLOGICAL RELEVANCE: Muntingia calabura L. (Muntingiaceae) is locally known as kerukup siam. Its leaves, flowers, barks and roots have been used traditionally in East Asia and South America to treat various diseases including ulcer-related diseases. The present study aimed to investigate the mechanism(s) of gastroprotective effect of methanol extract of Muntingia calabura leaves (MEMC) using the pylorus ligation induced gastric ulceration in rats.
MATERIALS AND METHODS: Five groups of rats (n=6) were administered orally once daily for 7 days with 8% Tween 80 (negative control), 100 mg/kg ranitidine (positive control), or MEMC (100, 250 or 500 mg/kg), followed by the ulcer induction via ligation of the pyloric part of the rat's stomach. This was followed by the macroscopic analysis of the stomach, evaluation of gastric content parameters, and quantification of mucus content. The antioxidant (measured using the superoxide anion and 2,2-diphenyl-1-picrylhydrazyl (DPPH)-radical scavenging, oxygen radical absorbance capacity (ORAC) and total phenolic content (TPC) assays), anti-inflammatory (evaluated using the in vitro lipoxygenase and xanthine oxidase assays), phytoconstituents and HPLC analysis of MEMC were also carried out.
RESULTS: The MEMC significantly (p<0.05) reduced gastric lesion in this model. Furthermore, the extract also significantly (p<0.01) reduced the volume of gastric content whereas the total acidity was significantly (p<0.05) reduced in the doses of 100 and 500 mg/kg MEMC. Moreover, the mucus content increased significantly (p<0.01) in MEMC-treated rats. The extract also showed high antioxidant and anti-inflammatory activities in all assays tested, and demonstrated the presence of high tannins and saponins followed by flavonoids.
CONCLUSION: The MEMC exerted gastroprotective effect via several mechanisms including the anti-secretory, antioxidant and anti-inflammatory activities. These activities could be attributed to the presence of tannins, saponins and flavonoids (e.g. rutin, quercitrin, fisetin and dihydroquercetin).

Matched MeSH terms: Lipoxygenase/metabolism
Fulltext Thermal inactivation of lipoxygenase in soya bean using superheated steam to produce low beany flavour soya milk

Chong WK, Mah SY, Easa AM, Tan TC

J Food Sci Technol, 2019 Sep;56(9):4371-4379.
PMID: 31478006 DOI: 10.1007/s13197-019-03905-4

Time and temperature parameters of superheated steam (SHS) treatment were optimised using response surface methodology (RSM) for specific lipoxygenase (LOX) activity in soya beans and crude protein content in soya milk. The optimal SHS treatment was obtained at 9.3 min and 119 °C. The predicted values of specific LOX activity and crude protein content by RSM were 0.0098 μmol/(min mg protein) and 3.2%, respectively. These values were experimentally verified to be 0.0081 ± 0.0002 μmol/(min mg protein) and 3.0 ± 0.1%, respectively. Sensory evaluation showed that the beany flavour of soya milk produced from SHS treated soya beans was significantly weaker (P

Matched MeSH terms: Lipoxygenase

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