| In vitro: |
| Chem Biol Drug Des. 2015 Oct;86(4):523-30. | | Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities.[Pubmed: 25589048] | A series of novel derivatives of strictosamide were synthesized and biologically evaluated.
METHODS AND RESULTS:
Most of the new compounds exhibited improved activities than the parent compound strictosamide. Among them, compounds Ib and If possessed antiviral activities against influenza A virus (A/Jinan/15/90) with IC50 values of 4.12 and 12.35 μg/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 μg/mL.
CONCLUSIONS:
Both compounds IIc and IId had moderate antiproliferative effects against five human cancer cell lines. The preliminary structure-activity relationships were also concluded. This study provides a promising new template with potential antiviral activity. | | Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology, 2014(7):1558-64. | | Experimental Research on Effect of Strictosamide Injection on Cardiovascular System.[Reference: WebLink] | This study was aimed to investigate the effects of high-dose strictosamide injection on cardiovascular system of anesthetized beagle dogs and to examine the inhibition of strictosamide on ion channels in vitro.
METHODS AND RESULTS:
Indexes such as changes of systolic blood pressure(Sys), diastolic blood pressure(Dia), mean blood pressure(MBP), heart rate(HR), PR, QRS, QT, QTcb and QTcv at different time points before and after strictosamide injection in dogs were monitored by the polygraph system. The inhibition of strictosamide at different concentrations on hERG potassium channel in CHO-hERG cells and Nav1.5 sodium channel in HEK-293-Nav1.5 cells were measured by whole-cell patch-clamp method. The results showed that compared with the blank control group, Sys, Dia, MBP and HR were obviously declined 15 min after medication in the strictosamide(60, 18 mg·kg-1) group and the vehicle-control group(containing tween-80)(P 0.05). After medication, all indexes were recovered. Compared to the vehicle-control group, there were no significant differences at different time points in each medication groups. Compared with the blank control group and before medication, the QT interval, QTcb and QTcv were significantly prolonged 15 min after medication in the strictosamide(60, 18, 6 mg·kg-1) group and the vehicle-control group(P 0.05). When medication stopped, indexes were recovered at certain level. Compared with the vehicle-control group, there were no significant differences of QT interval, QTcb and QTcv of each medication group at different time points(P 0.05). The inhibition of strictosamide on hERG potassium channel and Nav1.5 sodium channel were weak with IC50 values of560.8 μM and 900 μM, respectively, which were far greater than the positive controls.
CONCLUSIONS:
It was concluded that single, high-dose intravenous injection of strictosamide may lead to a lower blood pressure, a slower heart rate and a prolongation on the QT interval in beagle dogs, which returned to basal levels when medication stopped. It was speculated that the reduction of blood pressure and the slowing of heart rate were related to tween-80 contained in the vehicle control group. No significant inhibitory effects were detected on hERG potassium channel and Nav1.5 sodium channel in vitro, which suggested that other mechanisms may be involved in strictosamide-induced QT interval prolongation in animals. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
