5-Hydroxy-3-vinyl-2(5H)-furanone -a New Inhibitor of Human Synovial Phospholipase A2 and Platelet Aggregation from Fermentations of a Calyptella Species (Basidiomycetes)

1995 ◽  
Vol 50 (5-6) ◽  
pp. 403-409 ◽  
Author(s):  
Kirsten Lorenzen ◽  
Timm Anke ◽  
Silvia Konetschny-Rapp ◽  
Werner Scheuer
Keyword(s):  
Platelet Aggregation ◽  
Phospholipase A2 ◽  
Antimicrobial Activities ◽  
Selective Inhibitor ◽  
Phospholipase A ◽  
Spectroscopic Methods

Abstract 5-Hydroxy-3-vinyl-2(5H)-furanone, a potent and selective inhibitor of human synovial phospholipase A2 was isolated from fermentations of a Calyptella species. Its structure as identified by spectroscopic methods is identical to PA 147, an antibiotic previously isolated from a streptomycete. 5-hydroxy-3-vinyl-2(5H)-furanone inhibits the aggregation of human and bovine platelets stimulated by different inducers and exhibits weak antimicrobial activities.

scholarly journals Inhibition of phospholipase A2, platelet aggregation and egg albumin induced rat paw oedema as anti-inflammatory effect of Peltophorun pterocarpus stem-bark

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Osmund Chukwuma Enechi ◽  
Emmanuel Sunday Okeke ◽  
Ogochukwu Emmanuel Awoh ◽  
Charles Obinwanne Okoye ◽  
Chinaza Kyrian Odo
Keyword(s):  
Platelet Aggregation ◽  
Acute Toxicity ◽  
Phospholipase A2 ◽  
Phospholipase A ◽  
Phytochemical Analysis ◽  
Dependent Manner ◽  
Egg Albumin ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw

Abstract Background Most medicinal plants presently employed in traditional medicine are used without scientific evidence, thereby suggesting a need to explore efficient and reliable investigations of their potential. We, therefore, conducted the present study to ascertain the efficacy of flavonoid-rich extract of Peltophorum pterocarpum sterm-bark in the treatment and management of inflammatory disorders as employed in folk medicine. Materials and methods Flavonoid-rich extract of Peltophorum pterocarpum sterm-bark and a total of fifty-five (55) Wistar rats were used for this study. Eighteen (18) mice were used for toxicity testing, and the phytochemical analysis was done using the Trease and Evans method, while the acute toxicity was done using Lorke’s method. In vivo anti-inflammatory study was done using the egg albumin-induced paw oedema method, while the in vitro anti-inflammatory studies were performed for the extract using phospholipase A2 inhibition and calcium chloride-induced platelet aggregation assays. Results The phytochemical analysis revealed that the extract of Peltophorum pterocarpum sterm-bark contains tannins, terpenoids, steroids, phenols, alkaloids, flavonoids, glycosides, and saponins ranging from 0.307 ± 0.02 to 1279.567 ± 149.868. The acute toxicity test of the extract showed no toxicity up to 5000 mg/kg body weight. In the systemic oedema of the rat paw, scalar doses of the extract significantly (p < 0.05) suppressed the development of paw oedema induced by egg albumin, particularly with the Indomethacin (1.77 ± 0.41) when compared with the control (5.50 ± 0.26). However, varying doses of the extract significantly (p < 0.05) inhibited phospholipase A2 activity and CaCl2-Induced platelet aggregation in a concentration, dose, and time-dependent manner, in comparison to prednisolone. Conclusion These results indicate that the extract exhibited anti-inflammatory potential, and the mechanism of this activity has a promising ability to inhibit phospholipase A2 activity and platelet aggregation in rats inflicted with paw oedema.

Mechanism of Inhibitory Action on Platelet Activation of a Phospholipase A2 Isolated from Lachesis muta (Bushmaster) Snake Venom

1997 ◽  
Vol 78 (05) ◽  
pp. 1372-1380 ◽  
Author(s):  
André L Fuly ◽  
Olga L T Machado ◽  
Elias W Alves ◽  
Célia R Carlinis
Keyword(s):  
Platelet Aggregation ◽  
Enzymatic Activity ◽  
Phospholipase A2 ◽  
Inhibitory Activity ◽  
Thermal Inactivation ◽  
Anticoagulant Activity ◽  
Gel Filtration ◽  
Apparent Molecular Weight ◽  
Crude Venom ◽  
Lachesis Muta

SummaryCrude venom from Lachesis muta exhibited procoagulant, proteolytic and phospholipase A2 activities. A phospholipase A2, denoted LM-PLA2 was purified from L. muta venom to homogeneity, through a combination of chromatographic steps involving gel-filtration on Sephacryl S-200 HR and reverse phase chromatography on a C2/C18 column. LM-PLA2 presented a single polypeptide chain with an isoelectric point at pH 4.7 and apparent molecular weight of 17 kDa. Partial aminoacid sequence indicated a high degree of homology for LM-PLA2 with other PLA2 from different sources.LM-PLA2 displayed a potent enzymatic activity as measured by indirect hemolysis of red blood cells but it was neither lethal when injected i.p. into mice nor did it present anticoagulant activity. Furthermore, LM-PLA2 displayed a moderate inhibitory activity on the aggregation of rabbit platelets induced by low levels of ADP, thrombin and arachidonate. In contrast, platelet aggregation induced by high doses of collagen was strongly inhibited by LM-PLA2 as well as ATP-release. Treatment of the protein with p-bromophenacyl bromide or 2-mercapto-ethanol, as well as thermal inactivation studies, suggested that the platelet inhibitory effect of LM-PLA2 is dependent on its enzymatic activity. Thus, the platelet inhibitory activity of LM-PLA2 was shown to be dependent on the hydrolysis of plasma phospholipids and/or lipoproteins, most probably those rich in phosphatidylcholine. Surprisingly, lyso-phosphatidylcholine released by LM-PLA2 from plasma was shown to preferentially inhibited collagen-induced platelet aggregation, in contrast to other PLA2s, whose plasma hydrolytic products indistinctly affect platelet’s response to several agonists.

scholarly journals New Haloterpenes from the Marine Red Alga Laurencia papillosa: Structure Elucidation and Biological Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 35
Author(s):  
Mohamed Shaaban ◽  
Ghada S. E. Abou-El-Wafa ◽  
Christopher Golz ◽  
Hartmut Laatsch
Keyword(s):  
Biological Activity ◽  
Crude Extract ◽  
Structure Elucidation ◽  
Antimicrobial Activities ◽  
Red Alga ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Chemical Structures ◽  
Terpene Derivatives

Analysis of the air-dried marine red alga Laurencia papillosa, collected near Ras-Bakr at the Suez gulf (Red Sea) in Egypt delivered five new halogenated terpene derivatives: aplysiolic acid (1), 7-acetyl-aplysiol (2), aplysiol-7-one (3), 11,14-dihydroaplysia-5,11,14,15-tetrol (5a), and a new maneonene derivative 6, named 5-epi-maneolactone. The chemical structures of these metabolites were characterized employing spectroscopic methods, and the relative and absolute configurations were determined by comparison of experimental and ab initio-calculated NMR, NOE, ECD, and ORD data, and by X-ray diffraction of 2 and 6. The antimicrobial activities of the crude extract and compounds 1–3, 5a and 6 were studied.

A novel selective inhibitor to thrombin-induced platelet aggregation purified from the leech Whitmania pigra

2016 ◽  
Vol 473 (1) ◽  
pp. 349-354 ◽  
Author(s):  
Xuan Liu ◽  
Caihui Wang ◽  
Xue Ding ◽  
Xiaodong Liu ◽  
Qian Li ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Selective Inhibitor ◽  
Whitmania Pigra

Retinol induces platelet aggregation via activation of phospholipase A2

1988 ◽  
Vol 154 (3) ◽  
pp. 1075-1080 ◽  
Author(s):  
Tohru Nakano ◽  
Kohji Hanasaki ◽  
Saichi Matsumoto ◽  
Hitoshi Arita
Keyword(s):  
Platelet Aggregation ◽  
Phospholipase A2

Cell surface lipids and adhesion. I. The effects of lysophosphatidyl compounds, phospholipase A2 and aggregation-inhibiting protein

1975 ◽  
Vol 18 (3) ◽  
pp. 347-356
Author(s):  
A.S. Curtis ◽  
J. Campbell ◽  
F.M. Shaw
Keyword(s):  
Cell Adhesion ◽  
Fatty Acid ◽  
Cell Surface ◽  
Phospholipase A2 ◽  
Low Temperatures ◽  
Phospholipase A ◽  
Phospholipase Activity ◽  
Surface Lipids ◽  
Parallel Effect ◽  
Inhibiting Protein

Aggregation-inhibiting protein (AIP: Curtis & Greaves, 1965), which diminishes the adhesiveness of cells, particularly at low temperatures, is identified in the present paper as phospholipase A2 (EC. 3.1.1.4). Our reasons for this identification are because phospholipase activity parallels AIP activity on cell adhesion, and because various inhibitors and sera act in a parallel manner on adhesion in the presence of AIP or phospholipase. We suggest that the enzyme acts on adhesion by producing lysolecithin and other lysolipids in the plasmalemma. Addition of lysolipids diminishes cell adhesion in a manner similar to phospholipase A. Incubation of cells in Hanks' medium at 37 degrees C has a parallel effect. Conditions which would be expected to stimulate reacylation of lysolipids in the plasmalemma, i.e. incubation of cells in the external presence of CoA, ATP and a fatty acid, lead to a recovery or maintenance of adhesion after or during Hanks' incubation at 37 degrees C. All these results suggest that lipid components of the cell, probably in the plasmalemma, are of importance in adhesion. The results are discussed in relation to the long-standing controversy about the effects of low temperatures and trypsinization on cell adhesion, for phospholipase treatment of cells affects adhesion in a manner similar to trypsinization.

Mariannaeapyrone -a New Inhibitor of Thromboxane A2 Induced Platelet Aggregation

2001 ◽  
Vol 56 (1-2) ◽  
pp. 106-110 ◽  
Author(s):  
Kerstin Fabian ◽  
Timm Anke ◽  
Olov Sterner
Keyword(s):  
Platelet Aggregation ◽  
Chemical Structure ◽  
Thromboxane A2 ◽  
Human Platelets ◽  
Selective Inhibitor ◽  
Spectroscopic Techniques ◽  
Fungal Metabolite ◽  
Antimicrobial Effects ◽  
The Common ◽  
Induced Aggregation

Abstract Mariannaeapyrone ((E)-2-(1,3,5,7-tetramethyl-5-nonenyl)-3,5-dimethyl-6-hydroxy-4H-pyran-4-one) is a new fungal metabolite isolated from fermentations of the common mycophilic deuteromycete Mariannaea elegans. The chemical structure of the 4-pyrone was determined by spectroscopic techniques. Mariannaeapyrone is a selective inhibitor of the thromboxane A2 induced aggregation of human platelets, whereas only weak cytotoxic and antimicrobial effects could be observed.

Sign in / Sign up

Export Citation Format

Share Document