Problem statement: Dregea genus (Asclepiadaceae) is well known for the rich of steroid pregnane contents and these plants are famous for the potential to be applied as alternative biological activities. Dregea volubilis is the only species of Dregea genus in Thailand. The chemical and biological investigations of this plant are interesting to bioassay-guided fractionation, particularly chondroprotective effect. Approach: The research was carried out to extract, isolate, purify and elucidate structure of the active compound from the roots Dregea volubilis. Both of the solvent extracts and isolated compound were evaluated with kinds of chondroprotection. i.e., S-GAG), HA, UA and production of matrix metalloproteinase-2 (MMP-2). Results: Polyoxypregnane glycoside (PGG) or 12-0-benzoyl-8, 11-ditigloyl-3β, 8β, 11α, 12β, 14β-pentahydroxy-pregn-14-ol, 20-one,-3-0-methyl-β-D-allopyranosyl (1→4)-β-D-thevetopyranoside was isolated from the active ethyl acetate extract of the roots Dregea volubilis. The spectroscopic techniques were provided for success in structure determination. In addition, a new compound was the most powerful to biological activities. Chondroprotective effect of PPG on the degradation of sulfated glycosaminoglycan (S-GAG), hyaluronan (HA), uronic acid (UA) and production of matrix metalloproteinase-2 (MMP-2) in interleukin-1β (IL-1β)-stimulated porcine articular cartilage were also assessed. PGG was interestingly effective in reducing IL-1β induced S-GAG, HA release from cartilage explant and MMP-2 activity. Furthermore, PPG can reverse effect of IL-1β-reduced the levels of uronic acid remaining in cartilage tissue. Conclusion: The PGG was possessed a potent chondroprotective activity using the IL-1β stimulated cartilage explant model. Therefore, it is possible to use this compound as a new pharmacological agent for the management of degenerative joint diseases.
Interleukin-1β (IL-1β) induces the expression of matrix metalloproteinases (MMPs) implicated in cartilage and joint degradation in osteoarthritis (OA) and rheumatoid arthritis (RA). Polyoxypregnane glycoside (PPG), active compound was identified from Dregea volubilis extract by chemical analysis, shown to exert chondroprotective effects in cartilage explant models. However, no studies have been undertaken for the molecular investigation of whether PPG constituents protect the human articular chondrocyte (HAC). In the present studies, HAC was co-treated with IL-1β and PPG. The expression of MMPs, type II collagen, phosphorylation of mitogen-activated protein kinases (MAPKs) and NF-κB signaling pathway were determined by Western immunoblotting. PPG (6.25-25 μM) decreased the IL-1β-induced HA release from chondrocyte to culture medium. The mode of action of PPG was likely mediated through inhibiting expression of MMP-1, -3 and -13 in the medium, which was associated with the inhibition of mRNA expression. PPG had no effect on IL-1β-induced phosphorylation of MAPK pathway. Conversely, PPG decreased phosphorylation of IκB kinase and IκBα degradation. Taken together, these results indicate that PPG may inhibit cartilage degradation in OA and may also be used as nutritional supplement for maintaining joint integrity and function.
Goniothalamus (Annonaceae) is well known for the rich of styryllactone contents and these plants are famous for the potential to be applied as alternative biological activities. The chemical and biological investigations of Goniothalamus tapis is tested for anticancer activities. The research was processioned to extract, isolate, purify and elucidate structure from the leaves and twigs of G. tapis. The isolated compound was evaluated with cytotoxic activity. Goniothalamin was isolated from ethyl acetate extract of G. tapis and the spectroscopic techniques were used for structure elucidation. In addition, goniothalamin was the most powerful to cytotoxic activity which was the first reported for this specie. The goniothalamin was possessed a potent cytotoxicity. Therefore, it is possible to use this compound as a pharmacological agent.
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