Strictosamide

Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities.[Pubmed:25589048]

Chem Biol Drug Des. 2015 Oct;86(4):523-30.

A series of novel derivatives of Strictosamide were synthesized and biologically evaluated. 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 mug/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 mug/mL. 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.

Effects of strictosamide on mouse brain and kidney Na+, K+-ATPase and Mg2+-ATPase activities.[Pubmed:18992802]

J Ethnopharmacol. 2009 Jan 12;121(1):117-22.

Present study reports on the general bioactivity of Strictosamide and on its effects on Na(+),K(+)-ATPase and Mg(2+)-ATPase activities of Charles River male mouse. Strictosamide is the main glycoalkaloid of Sarcocephalus latifolius (Rubiaceae) leaves and roots, used as medicinal plant in folk medicine. In this work, we studied the in vitro effects of various concentrations of Strictosamide (0.25, 0.5, 1 or 2 mg/mL) and the in vivo effects of single doses (50, 100 or 200 mg/kg, i.p.) of this compound on kidney and brain Na(+),K(+)-ATPase and Mg(2+)-ATPase activities. Results of general study showed that Strictosamide is slightly toxic to Charles River mouse (LD(50)=723.17 mg/kg), producing CNS depression and kidney toxicity, but the exact mechanism of these effects could not be defined. Strictosamide inhibited the in vitro and in vivo Mg(2+)-ATPase activity on kidney but had nonsignificant effect on brain. Furthermore, Strictosamide had nonsignificant in vitro and in vivo effect on kidney Na(+),K(+)-ATPase activity but produced an in vivo increase of Na(+),K(+)-ATPase activity of brain, these findings suggesting that strictosamine may be related to the induction of alpha(2) isoform of Na(+),K(+)-ATPase and may account for the folk use of Sarcocephalus latifolius root infusion on hypertension.

In vivo anti-inflammatory and analgesic activities of strictosamide from Nauclea officinalis.[Pubmed:25026342]

Pharm Biol. 2014 Nov;52(11):1445-50.

CONTEXT: Strictosamide is the main representative constituent of Nauclea officinalis Pierre ex Pitard (Rubiaceae), which has been used for a long time in China to treat diseases related to infection and inflammation, but its pharmacological activities are not well studied. OBJECTIVE: This work evaluates the anti-inflammatory and analgesic activities of Strictosamide by in vivo experiments. MATERIALS AND METHODS: The anti-inflammatory activity was assessed in mice by models of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema, acetic acid-elevated vascular permeability, and carboxymethylcellulose sodium (CMC-Na)-induced leukocyte migration. The analgesic activity was estimated in mice using acetic acid-induced writhing and hot-plate tests. Compound was injected to mice twice a day for 3 d at doses of 10, 20, and 40 mg/kg. RESULTS: At 20 and 40 mg/kg, Strictosamide obviously decreased the TPA-induced mice ear edema (24.7 and 28.1% inhibition, respectively), and significantly inhibited acetic acid-stimulated peritoneal vascular permeability in mice (23.3 and 33.4% inhibition, respectively). It also significantly decreased the leukocytes in the mice peritoneal cavity induced by CMC-Na at all the tested doses (46.0, 49.1, and 58.7% inhibition, respectively). To acetic acid-induced writhing test in mice, Strictosamide markedly prolonged the pain latency at 20 and 40 mg/kg and decreased the writhing counts at 40 mg/kg (49.7% inhibition). However, it did not obviously improve the pain threshold of mice in hot-plate test. DISCUSSION AND CONCLUSION: Strictosamide may have important effects on inflammation and inflammatory pain. The results provide scientific support for the role of Strictosamide in the use of N. officinalis to treat inflammatory diseases.