Investigation of the Possible Anti-angiogenic Activity of Iraqi Scabiosa palaestina L. Using Ex Vivo Rat Aorta Ring Assay

2021 ◽  
Vol 12 (4) ◽  
pp. 249
Author(s):  
AMJED KHAMEES ◽  
ENAS KHADIM ◽  
HAYDER SAHIB
2012 ◽  
Vol 7 (9) ◽  
pp. 1934578X1200700
Author(s):  
Kenn Foubert ◽  
Annelies Breynaert ◽  
Mart Theunis ◽  
Rita Van Den Bossche ◽  
Guido R.Y. De Meyer ◽  
...  

Angiogenesis, in which a vascular network is established from pre-existing vessels, is a complex multistep process. Mechanisms underlying angiogenesis can be investigated using a variety of in vitro, ex vivo and in vivo approaches. Evaluation of several promising plants and plant metabolites, including terpenoids, revealed promising anti-angiogenic activity. Since the maesasaponins displayed anti-angiogenic activity in the chick chorioallantoic membrane (CAM) assay, their activity was further investigated in several test systems. The rat aorta ring assay was compared with the placental vein assay and then selected for the ex vivo investigation of the saponins. Besides their effect on the viability of HUVEC, the anti-angiogenic capacity of the compounds was also investigated in an in vivo zebrafish assay. The activity of the saponins in the viability assay was more pronounced than in the rat aorta ring assay and similar to the effect observed in the CAM assay. The use of different test systems, however, implies different results in the case of saponins.


Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5683
Author(s):  
Megan L. Peach ◽  
Shaunna L. Beedie ◽  
Cindy H. Chau ◽  
Matthew K. Collins ◽  
Suzana Markolovic ◽  
...  

Due to its antiangiogenic and anti-immunomodulatory activity, thalidomide continues to be of clinical interest despite its teratogenic actions, and efforts to synthesize safer, clinically active thalidomide analogs are continually underway. In this study, a cohort of 27 chemically diverse thalidomide analogs was evaluated for antiangiogenic activity in an ex vivo rat aorta ring assay. The protein cereblon has been identified as the target for thalidomide, and in silico pharmacophore analysis and molecular docking with a crystal structure of human cereblon were used to investigate the cereblon binding abilities of the thalidomide analogs. The results suggest that not all antiangiogenic thalidomide analogs can bind cereblon, and multiple targets and mechanisms of action may be involved.


2009 ◽  
Vol 5 (6) ◽  
pp. 370-376 ◽  
Author(s):  
A.F.A. Aisha ◽  
K.M. Abu-Salah ◽  
Y. Darwis ◽  
A.M.S. Abdul Maji

1981 ◽  
Author(s):  
K U Weithmann ◽  
A G Hoechst

Aortas from rats, treated with 5-20 mg/kg of pentoxifylline (pof), penbutolol, prenylamine, clofibric acid or nicotinic acid showed, ex vivo, a significantly higher release of acid labile PGI2-like anti-aggregatory activity compared to controls. This activity could be suppressed by pre-treatment with 2 mg/kg Indomethacin. When incubated with rat aortas in vitro, pof showed a similar stimulatory effect on PGI2-like release, whereas clofibric-and nicotinic acid had no significant effect in this system. Pof and all other drugs mentioned above in therapeutical concentrations had virtually no effect on induced aggregation of human platelets in vitro. However, in the presence of small amounts PGI2 in vitro, inhibition of aggregation and platelet cyclic AMP are enhanced synergistically above the effects of PGI2 and pof individually.We conclude from these experiments that therapeutic doses of all drugs in our study stimulate in vivo the release of PGI2-like activity from vessel walls, thus inhibiting platelet aggregation in vivo. The primary site of action of pof seems to be the vessel wall, whereas the effect of clofibric acid and nicotinic acid on the vessel walls seem to be secondary. The elevation of platelet cyclic AMP levels which generally parallels PGI2-induced inhibition of aggregation might be further enhanced by pof known as an inhibitor of platelet cyclic AMP phosphodiesterase, thus explaining the observed synergistic effects between PGI2 and pof.


2004 ◽  
Vol 486 (2) ◽  
pp. 201-207 ◽  
Author(s):  
Ivan S de la Lande ◽  
Tracey E Siebert ◽  
Catherine L Bennett ◽  
Irene Stafford ◽  
John D Horowitz

1995 ◽  
Vol 73 (8) ◽  
pp. 1203-1207 ◽  
Author(s):  
Bahjaf Al-Ani ◽  
Mahmoud Saifeddine ◽  
Morley D. Hollenberg

We have studied the actions of the proteinase-activated-receptor-2 (PAR2)-activating polypeptide, SLIGRL-NH2 (SLI-NH2), in rat aorta and in gastric longitudinal muscle preparations. In the phenylephrine-precontracted aorta preparation, SLI-NH2 caused an endothelium-dependent relaxation that mimicked the action of low concentrations (0.5 U/mL) of trypsin and that was blocked by the nitric oxide synthase inhibitor Nω-nitro-L-arginine methyl ester. In endothelium-free aorta ring preparations, SLI-NH2 caused neither a relaxation nor a contraction. In the gastric longitudinal muscle preparation, SLI-NH2 caused a transient contraction that mimicked the action of trypsin (0.5 U/mL) and that was sensitive to inhibitors of cyclooxygenase (indomethacin) and tyrosine kinase (genistein). Further, using a reverse-transcriptase – polymerase chain reaction (RT–PCR) approach we detected, in both assay tissues, mRNA for the rat PAR2 receptor, and we ascertained, using a cloned receptor cDNA obtained from a rat intestinal cDNA library, that the putative N-terminal activating peptide sequence of the rat PAR2 receptor (SLIGRL) is identical with the one previously cloned from murine tissue. We concluded that, like the thrombin receptor, the PAR2 receptor may play a pathophysiologic role in the regulation of vascular and gastric smooth muscle contractility.Key words: thrombin, proteinase-activated receptor 2, protease, smooth muscle.


2014 ◽  
Vol 64 (2) ◽  
pp. 233-245 ◽  
Author(s):  
José A. S. Luis ◽  
Thiago M. De Aquino ◽  
Bruno F. Lira ◽  
Petrônio F. A. Filho ◽  
Marcus T. Scotti ◽  
...  

Abstract Seven new compounds have been synthetized in satisfactory yields (51-78 %) through the treatment of mesoionic 1,3-thiazolium-5-thiolate (4a-d) and 1,3,4-thiadiazolium- 5-thiolate (10a,b) with chloroacetic acid or methyl iodide: 1,3,4-thiadiazolium-5-methylthio- (11) and 5-thioacetate (12). The structure of the title compounds was elucidated by elemental analysis, IR, 1H and 13C NMR spectroscopy. The newly synthesized compounds 5a, 6a, 11 and 12 were evaluated for their ex vivo spasmolytic potential on four isolated smooth muscles (rat aorta and uterus, guinea pig ileum and trachea) and compared with scopolamine. Some of the compounds exhibited potent spasmolytic activity equal to or stronger than scopolamine


2010 ◽  
Vol 20 (3) ◽  
pp. 219-223
Author(s):  
F. Cilurzo ◽  
P. Minghetti ◽  
F. Selmin ◽  
I.E. Cupone ◽  
C.G.M. Gennari ◽  
...  
Keyword(s):  
Ex Vivo ◽  

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 251
Author(s):  
Imran Ahmad Khan ◽  
Musaddique Hussain ◽  
Shahzada Khurram Syed ◽  
Malik Saadullah ◽  
Ali M. Alqahtani ◽  
...  

Plumeria rubra (L.) is a traditional folkloric medicinal herb used to treat cardiovascular disorders. The present investigation was methodically planned to investigate the pharmacological foundations for the therapeutic effectiveness of P. rubra in cardiovascular illnesses and its underlying mechanisms. Ex vivo vaso-relaxant effects of crude leaf extract of P. rubra were observed in rabbit aorta ring preparations. Hypotensive effects were measured using pressure and force transducers connected to the Power Lab data acquisition system. Furthermore, P. rubra displayed cardioprotective properties in rabbits when they were exposed to adrenaline-induced myocardial infarction. In comparison to the intoxicated group, the myocardial infarction model showed decreased troponin levels, CK-MB, LDH, ALT, ALP, AST, and CRP, as well as necrosis, apoptosis, oedema, and inflammatory cell enrollment. P. rubra has revealed good antioxidant properties and prolonged the noradrenaline intoxicated platelet adhesion. Its anticoagulant, vasorelaxant, and cardioprotective effects in both in vivo and ex vivo investigations are enabled by blocking L-type calcium channels, lowering adrenaline, induced oxidative stress, and tissue tear, justifying its therapeutic utility in cardiovascular disorders.


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