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Study on Acetylcholinesterase Inhibitory, Anti-inflammatory and Antioxidant Activities of Holarrhena antidysenterica Bark
| Content Provider | Semantic Scholar |
|---|---|
| Author | Mukem, Sunthorn |
| Copyright Year | 2011 |
| Abstract | The investigation of chemical constituents of Holarrhena antidysenterica bark, family Apocynaceae led to the isolation of four steroidal alkaloids including, conessine (1), isoconessimine (2), conessimine (3), and N-3-methylholarrhimine (4) and one coumarin, scopoletin (5). The steroidal alkaloids and coumarin were subjected to acetylchlolinesterase inhibitory activity showed higher inhibitory activity with IC50 values in the range of 0.12-20.08 μM and a coumarin with an IC50 73.50 μM. The kinetic analyses of acetylchlolinesterase inhibitory activity of steroidal alkaloids suggested the steroidal alkaloid inhibit in competitive manner. Among steroidal alkaloid, 3 showed the best activity with IC50 of 0.12 ± 0.03 μM. The molecular docking of 3 found that it can form hydrogen bonding with Gly-118. This may answer why 3 is more active. Furthermore, all compounds were studied on anti-inflammatory activity using NO production assay in murine macrophage like RAW 264.7. The results found that 2 at concentration 30 μM showed inhibition of NO production 43.6 %, however it has cytotoxicity in murine macrophage at concentration of 100 μM. All these compounds have no antioxidant activity. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://kb.psu.ac.th/psukb/bitstream/2016/10390/1/356362.pdf |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
