A comparative study of topical natural ergot alkaloids on the intraocular pressure and aqueous humor dynamics in oclular normotensive and α-chymotrypsin-induced ocular hypertensive rabbits

Puras, Gustavo; Santafé, Juan; Segarra, José; Garrido, Manuel; Melena, José

doi:10.1007/s00417-007-0596-3

Cited by 3 publications

(3 citation statements)

References 37 publications

(44 reference statements)

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“…However, we expect the 0.46 µL/(minϫmm Hg) value to approximate the control outflow conductance of the normal sheep eye. This value is similar to that obtained in eyes of other species, eg, 0.2 to 0.4 µL/(minϫmm Hg) in rabbits 8,[16][17][18][19][20][21] and 0.3 µL/(minϫmm Hg) in humans. 22 As such, it is possible that anecortave reversed the increase in aqueous outflow resistance produced by prednisolone so that outflow conductance in the combined presence of the 2 agents was similar to that in the normal eye.…”

Section: Commentsupporting

confidence: 88%

Suppression of Corticosteroid-Induced Ocular Hypertension in Sheep by Anecortave

Candia¹

2010

Arch Ophthalmol

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Objective: To confirm the ocular hypotensive effects of anecortave acetate on an ovine model for steroid-induced ocular hypertension. Eyes of normal sheep exhibit a robust steroid-induced ocular hypertensive response. Recent observations in an uncontrolled, interventional case series indicated that anecortave elicited hypotensive effects when administered as a sub-Tenon depot in the eyes of a small sample of patients with glaucoma. Methods: Intraocular pressure (IOP) was monitored by Perkins applanation tonometry in 16 normal sheep receiving topically administered prednisolone acetate, 0.5%, in both eyes, 3 times daily, a protocol that doubled IOP within 12 days. Half of the sheep had received a unilateral sub-Tenon injection of anecortave in 1 eye prior to the initiation of the bilateral prednisolone instillations, while the 8 remaining sheep received the unilateral anecortave sub-Tenon depot after the IOP was maximally elevated by the prednisolone instillations. Results: In these 2 sets of experiments, the presence of the anecortave depot suppressed the steroidinduced IOP elevation and reverted the elevated IOP to baseline levels. Measurements of aqueous outflow facility indicated that eyes treated with prednisolone plus anecortave exhibited a 5.8-fold higher outflow facility than the fellow eyes solely exposed to prednisolone, indicating that anecortave prevented the increase in outflow resistance produced by the corticosteroid. Conclusion: Elucidation of the mechanisms of action of anecortave in animal models may prove relevant to the design of novel interventions for the management of primary open-angle glaucoma.

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Section: Commentsupporting

confidence: 88%

Suppression of Corticosteroid-Induced Ocular Hypertension in Sheep by Anecortave

Candia¹

2010

Arch Ophthalmol

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“…In the study, ergocristine, α-ergocriptine, and ergocornine were found to be effective in decreasing the IOP in a dose-dependent fashion, producing an ocular antihypertensive effect. The same group later conducted a comparative evaluation of the effect of these alkaloids on IOP and on aqueous humor dynamics, both in ocular normotensive and in α-chymotrypsin-induced ocular hypertensive rabbits [ 40 ]. The tested molecules decreased both tonographic outflow facility and aqueous humor inflow, which explains the reduction of the IOP in a dose-related fashion for both rabbit models.…”

Section: Role Of Ergot Alkaloids In Reducing Intraocular Pressurementioning

confidence: 99%

Natural Ergot Alkaloids in Ocular Pharmacotherapy: Known Molecules for Novel Nanoparticle-Based Delivery Systems

et al. 2020

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Several pharmacological properties are attributed to ergot alkaloids as a result of their antibacterial, antiproliferative, and antioxidant effects. Although known for their biomedical applications (e.g., for the treatment of glaucoma), most ergot alkaloids exhibit high toxicological risk and may even be lethal to humans and animals. Their pharmacological profile results from the structural similarity between lysergic acid-derived compounds and noradrenalin, dopamine, and serotonin neurotransmitters. To reduce their toxicological risk, while increasing their bioavailability, improved delivery systems were proposed. This review discusses the safety aspects of using ergot alkaloids in ocular pharmacology and proposes the development of lipid and polymeric nanoparticles for the topical administration of these drugs to enhance their therapeutic efficacy for the treatment of glaucoma.

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“…Similarly, antiurease, α -glucosidase, and antilipoxygenase activity is reported in the literature for crude alkaloids from fruit, bark, leaves, and root of Zanthoxylum armatum [ 41 ]. Alkaloids isolated from different plants were also investigated for their α -chymotrypsin inhibitory potential [ 42 – 44 ]. The above reported data support the urease α -chymotrypsin inhibitory activities of our alkaloids 1 – 4 .…”

Section: Resultsmentioning

confidence: 99%

Urease and α-Chymotrypsin Inhibitory Activities and Molecular Docking Studies of Alkaloids Isolated from Medicinal Plant Isatis minima Bunge

Fozia

Ahmad

Haq

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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Phytochemical studies on the alkaloids fraction of the entire plant of Isatis minima Bunge resulted in the alkaloids 1–4 isolation, which were first time isolated from this species. The 1D and 2D NMR spectroscopic data were used to identify their structures, and there was satisfactory compatibility of the data compared to those which were previously published. In the examined compounds 1–4, Isaindigotidione (3) and Isaindigotone (4) were shown as an effective urease inhibitor in such a concentration-dependent way against Jack bean and Bacillus pasteurii urease, with IC50 values 29.03 ± 0.04, 20.04 ± 0.09 and 34.03 ± 0.07, 26.13 ± 0.08 μM, respectively. Compounds 3 and 4 were likewise shown to be an effective inhibitor against α-chymotrypsin, exhibiting IC50 values 16.09 ± 0.07 and 22.01 ± 0.06 μM, correspondingly. The program MOE-Dock was used to perform a molecular docking analysis to confirm probable binding modes of the active complexes of the isolated compounds 1–4 and the crystal structure of urease and α-chymotrypsin enzymes. Compound 3 was the most active, having the highest docking scores against Bacillus pasteurii urease, α-chymotrypsin, and Jack bean (−8.6876), (−7.6647), and (−13.1927) μM, respectively. All four alkaloids (1–4) showed significant urease and protease inhibitory potential and further these activities were confirmed with the help of molecular docking study.

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A comparative study of topical natural ergot alkaloids on the intraocular pressure and aqueous humor dynamics in oclular normotensive and α-chymotrypsin-induced ocular hypertensive rabbits

Cited by 3 publications

References 37 publications

Suppression of Corticosteroid-Induced Ocular Hypertension in Sheep by Anecortave

Suppression of Corticosteroid-Induced Ocular Hypertension in Sheep by Anecortave

Natural Ergot Alkaloids in Ocular Pharmacotherapy: Known Molecules for Novel Nanoparticle-Based Delivery Systems

Urease and α-Chymotrypsin Inhibitory Activities and Molecular Docking Studies of Alkaloids Isolated from Medicinal Plant Isatis minima Bunge

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