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Anti-inflammatory effects of the gorgonian Pseudopterogorgia elisabethae collected at the Islands of Providencia and San Andrés (SW Caribbean).

Correa H, Valenzuela AL, Ospina LF, Duque C - J Inflamm (Lond) (2009)

Bottom Line: Finally, because the PsG, PsP and seco-PsK did not exhibit any NO scavenger activity, they should inhibit the inducible Nitric Oxide Synthase (iNOS) or other routes that influence this enzyme.All results presented contribute to demonstrate that the compounds isolated in this work from P. elisabethae are promising molecules with an interesting anti-inflammatory activity profile.Additionally, the results obtained could provide preliminary insights towards their structure-activity relationship.

View Article: PubMed Central - HTML - PubMed

Affiliation: Departamento de Química, Universidad Nacional de Colombia, Cra, 30 N degrees 45 -03, Bogotá D,C, Colombia. lfospinag@unal.edu.co.

ABSTRACT

Background: We are reporting for the first time the in vivo anti-inflammatory activity of extracts and fractions, and in vitro anti-inflammatory activity of pure compounds, all isolated from Pseudopterogorgia elisabethae collected at the Providencia (chemotype 1) and San Andrés (chemotype 2) Islands (SW Caribbean).

Methods: Extracts from P. elisabethae were fractionated on silica gel to yield fractions: F-1 (pseudopterosins PsQ, PsS and PsU) and F-2 (amphilectosins A and B, PsG, PsK, PsP and PsT and seco-pseudopterosins seco-PsJ and seco-PsK) from chemotype 1, and F-3 (elisabethatrienol, 10-acetoxy-9-hydroxy- and 9-acetoxy-10-hydroxy-amphilecta-8,10,12,14-tetraenes (interconverting mixture) and amphilecta-8(13),11,14-triene-9,10-dione) from chemotype 2. By using preparative RP-HPLC and spectroscopic means, we obtained the pure PsG, PsK, PsP, PsQ, PsS, PsT, PsU, seco-PsK and the interconverting mixture of non-glycosylated diterpenes (IMNGD). The anti-inflammatory properties of extracts and fractions were evaluated using in vivo model "12-O-tetradecanoyl-phorbol-acetate (TPA)-induced mouse ear oedema". The activities of pure compounds and of the IMNGD were evaluated using in vitro assays myeloperoxidase (MPO) release (by human polymorphonuclear neutrophils (PMNs)), nitric oxide release (by J-774 cells) and scavenger activity on NO.

Results: In the in vivo anti-inflammatory assay, extracts and F-3 showed low inhibition levels of inflammation compared to indomethacin, F-1 and F-2. Additionally, we evaluated the MPO release to the inflammation site, and found a marked inhibition of MPO levels by all extracts and fractions, even superior to the inhibition shown by indomethacin.Furthermore, in the MPO in vitro assay, IMNGD, PsQ, PsS, PsT and PsU, exhibited higher inhibition levels compared to dexamethasone and indomethacin. In the NO release in vitro, IMNGD, PsP and PsT were the most potent treatments. Finally, because the PsG, PsP and seco-PsK did not exhibit any NO scavenger activity, they should inhibit the inducible Nitric Oxide Synthase (iNOS) or other routes that influence this enzyme. Alternatively, PsQ, PsS, and PsU did show scavenger activity.

Conclusion: All results presented contribute to demonstrate that the compounds isolated in this work from P. elisabethae are promising molecules with an interesting anti-inflammatory activity profile. Additionally, the results obtained could provide preliminary insights towards their structure-activity relationship.

No MeSH data available.


Related in: MedlinePlus

Effects of pure compounds from P. elisabethae on MPO release in PMNs. Calcium ionophore (1 μM) (A23187)-PMNs (2.5 × 106 cells/well) treated with IMNGD (50 μg/ml), pure compounds (10 μM), dexamethasone (10 μM) and indomethacin (10 μM). Data expressed as mean ± S.E.M., n = 3 (Anova post-test Dunnet: *P < 0.05 and **P < 0.01 respect to control (stimulated cells).
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Figure 4: Effects of pure compounds from P. elisabethae on MPO release in PMNs. Calcium ionophore (1 μM) (A23187)-PMNs (2.5 × 106 cells/well) treated with IMNGD (50 μg/ml), pure compounds (10 μM), dexamethasone (10 μM) and indomethacin (10 μM). Data expressed as mean ± S.E.M., n = 3 (Anova post-test Dunnet: *P < 0.05 and **P < 0.01 respect to control (stimulated cells).

Mentions: Figure 4 shows the percentage of MPO inhibition (released in vitro by human PMNs) by IMNGD (10 μg/ml) and pure compounds (10 μM) isolated from P. elisabethae. IMNGD was the most active treatment in the experiment, exhibiting 92 ± 6% inhibition levels in comparison with indomethacin (57 ± 4%) and dexamethasone (35 ± 1%).


Anti-inflammatory effects of the gorgonian Pseudopterogorgia elisabethae collected at the Islands of Providencia and San Andrés (SW Caribbean).

Correa H, Valenzuela AL, Ospina LF, Duque C - J Inflamm (Lond) (2009)

Effects of pure compounds from P. elisabethae on MPO release in PMNs. Calcium ionophore (1 μM) (A23187)-PMNs (2.5 × 106 cells/well) treated with IMNGD (50 μg/ml), pure compounds (10 μM), dexamethasone (10 μM) and indomethacin (10 μM). Data expressed as mean ± S.E.M., n = 3 (Anova post-test Dunnet: *P < 0.05 and **P < 0.01 respect to control (stimulated cells).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2662832&req=5

Figure 4: Effects of pure compounds from P. elisabethae on MPO release in PMNs. Calcium ionophore (1 μM) (A23187)-PMNs (2.5 × 106 cells/well) treated with IMNGD (50 μg/ml), pure compounds (10 μM), dexamethasone (10 μM) and indomethacin (10 μM). Data expressed as mean ± S.E.M., n = 3 (Anova post-test Dunnet: *P < 0.05 and **P < 0.01 respect to control (stimulated cells).
Mentions: Figure 4 shows the percentage of MPO inhibition (released in vitro by human PMNs) by IMNGD (10 μg/ml) and pure compounds (10 μM) isolated from P. elisabethae. IMNGD was the most active treatment in the experiment, exhibiting 92 ± 6% inhibition levels in comparison with indomethacin (57 ± 4%) and dexamethasone (35 ± 1%).

Bottom Line: Finally, because the PsG, PsP and seco-PsK did not exhibit any NO scavenger activity, they should inhibit the inducible Nitric Oxide Synthase (iNOS) or other routes that influence this enzyme.All results presented contribute to demonstrate that the compounds isolated in this work from P. elisabethae are promising molecules with an interesting anti-inflammatory activity profile.Additionally, the results obtained could provide preliminary insights towards their structure-activity relationship.

View Article: PubMed Central - HTML - PubMed

Affiliation: Departamento de Química, Universidad Nacional de Colombia, Cra, 30 N degrees 45 -03, Bogotá D,C, Colombia. lfospinag@unal.edu.co.

ABSTRACT

Background: We are reporting for the first time the in vivo anti-inflammatory activity of extracts and fractions, and in vitro anti-inflammatory activity of pure compounds, all isolated from Pseudopterogorgia elisabethae collected at the Providencia (chemotype 1) and San Andrés (chemotype 2) Islands (SW Caribbean).

Methods: Extracts from P. elisabethae were fractionated on silica gel to yield fractions: F-1 (pseudopterosins PsQ, PsS and PsU) and F-2 (amphilectosins A and B, PsG, PsK, PsP and PsT and seco-pseudopterosins seco-PsJ and seco-PsK) from chemotype 1, and F-3 (elisabethatrienol, 10-acetoxy-9-hydroxy- and 9-acetoxy-10-hydroxy-amphilecta-8,10,12,14-tetraenes (interconverting mixture) and amphilecta-8(13),11,14-triene-9,10-dione) from chemotype 2. By using preparative RP-HPLC and spectroscopic means, we obtained the pure PsG, PsK, PsP, PsQ, PsS, PsT, PsU, seco-PsK and the interconverting mixture of non-glycosylated diterpenes (IMNGD). The anti-inflammatory properties of extracts and fractions were evaluated using in vivo model "12-O-tetradecanoyl-phorbol-acetate (TPA)-induced mouse ear oedema". The activities of pure compounds and of the IMNGD were evaluated using in vitro assays myeloperoxidase (MPO) release (by human polymorphonuclear neutrophils (PMNs)), nitric oxide release (by J-774 cells) and scavenger activity on NO.

Results: In the in vivo anti-inflammatory assay, extracts and F-3 showed low inhibition levels of inflammation compared to indomethacin, F-1 and F-2. Additionally, we evaluated the MPO release to the inflammation site, and found a marked inhibition of MPO levels by all extracts and fractions, even superior to the inhibition shown by indomethacin.Furthermore, in the MPO in vitro assay, IMNGD, PsQ, PsS, PsT and PsU, exhibited higher inhibition levels compared to dexamethasone and indomethacin. In the NO release in vitro, IMNGD, PsP and PsT were the most potent treatments. Finally, because the PsG, PsP and seco-PsK did not exhibit any NO scavenger activity, they should inhibit the inducible Nitric Oxide Synthase (iNOS) or other routes that influence this enzyme. Alternatively, PsQ, PsS, and PsU did show scavenger activity.

Conclusion: All results presented contribute to demonstrate that the compounds isolated in this work from P. elisabethae are promising molecules with an interesting anti-inflammatory activity profile. Additionally, the results obtained could provide preliminary insights towards their structure-activity relationship.

No MeSH data available.


Related in: MedlinePlus