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Anti-malarial activity of 6-(8'Z-pentadecenyl)-salicylic acid from Viola websteri in mice.

Chung IM, Seo SH, Kang EY, Park WH, Moon HI - Malar. J. (2009)

Bottom Line: Petroleum ether extracts of Viola websteri Hemsl (Violaceae) were reported to have anti-plasmodial activity against Plasmodium falciparum in vitro, with this activity being largely attributable to 6-(8'Z-pentadecenyl)-salicylic acid (6-SA).The possible 'repository' activity of 6-SA was assessed using the method described by Peters.In the present study, 6-SA was found to have anti-malarial activity in vivo, when tested against P. berghei in mice. 6-SA at 5, 10 and 25 mg/kg x day exhibited a significant blood schizontocidal activity in four-day early infections, repository evaluations and established infections with a significant mean survival time comparable to that of the standard drug, chloroquine (5 mg/kg.day). 6-SA possesses a moderate anti-malarial activity that could be exploited for malaria therapy.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Diagnostics, College of Korean Medicine, Dongguk University, Gyeong-Ju 780-714, South Korea. himun68@daum.net

ABSTRACT

Background: Petroleum ether extracts of Viola websteri Hemsl (Violaceae) were reported to have anti-plasmodial activity against Plasmodium falciparum in vitro, with this activity being largely attributable to 6-(8'Z-pentadecenyl)-salicylic acid (6-SA).

Methods: The schizontocidal activity of 6-SA on early Plasmodium berghei infections was evaluated in a four-day test. The possible 'repository' activity of 6-SA was assessed using the method described by Peters. The median lethal dose (LD50) of 6-SA, when given intraperitoneally, was also determined using uninfected ICR mice and the method of Lorke.

Results: In the present study, 6-SA was found to have anti-malarial activity in vivo, when tested against P. berghei in mice. 6-SA at 5, 10 and 25 mg/kg x day exhibited a significant blood schizontocidal activity in four-day early infections, repository evaluations and established infections with a significant mean survival time comparable to that of the standard drug, chloroquine (5 mg/kg.day).

Conclusion: 6-SA possesses a moderate anti-malarial activity that could be exploited for malaria therapy.

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Related in: MedlinePlus

Effect of 6-SA on established Plasmodium berghei infection in mice. The experimental hosts were infected on day 0 and 'treated' orally, with saline containing 0.5% Tween-80, 6-SA at 5, 10 or 25 mg/kg·day or chloroquine at 5 mg/kg·day, on days 3–7.
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Figure 2: Effect of 6-SA on established Plasmodium berghei infection in mice. The experimental hosts were infected on day 0 and 'treated' orally, with saline containing 0.5% Tween-80, 6-SA at 5, 10 or 25 mg/kg·day or chloroquine at 5 mg/kg·day, on days 3–7.

Mentions: In both the four-day test and the test of repository activity, oral 6-SA produced dose-dependent chemosuppression (Table 1), with even the lowest dose tested (5 mg/kg·day) causing significant reductions in parasitaemia (P < 0.05). The highest dose of 6-SA tested (25 mg/kg·day) did not do well enough compared with the lowest dose tested (5 mg/kg·day), and did not quite reach the level of chemosuppression seen with the drugs used as positive controls–chloroquine at 5 mg/kg·day) or pyrimethamine at 1.2 mg/kg·day (Table 1). In the mice that were treated only from 72 hours post-infection, daily oral doses of 6-SA or chloroquine led to gradual reductions in parasitaemia over time, whereas the parasitaemias in the negative-control mice increased with time (Figure 2). All the mice administered with 6-SA showed a gradual decrease in body weight from day 7, but this weight loss lasted only for a few days, after which these mice gained weight daily. Mice in the negative-control group lost weight daily during the follow-up period. One of the five mice administered with 10 mg/kg·day 6-SA died before day 29 (on day 22), as did three of the five mice treated with 5 mg/kg·day (on days 18, 19 and 25) and all five of the negative-control mice (on days 11~18). None of the mice given the highest dose of 6-SA and none of those given chloroquine died during the follow-up period. The mean survival times of the mice administered 5, 10 or 25 mg/kg·day 6-SA, chloroquine and saline containing 0.5% Tween-80 were 24.0, 27.6, 30.0, 30.0 and 15 days, respectively. The mice still alive on day 29 (all of which had been treated with 6-SA or chloroquine) were aparasitaemic. In the tests of activity against established infections, the highest tested doses of 6-SA appeared as effective as chloroquine in terms of the day-7 parasitaemias (Figure 2) and day-29 survival.


Anti-malarial activity of 6-(8'Z-pentadecenyl)-salicylic acid from Viola websteri in mice.

Chung IM, Seo SH, Kang EY, Park WH, Moon HI - Malar. J. (2009)

Effect of 6-SA on established Plasmodium berghei infection in mice. The experimental hosts were infected on day 0 and 'treated' orally, with saline containing 0.5% Tween-80, 6-SA at 5, 10 or 25 mg/kg·day or chloroquine at 5 mg/kg·day, on days 3–7.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2713261&req=5

Figure 2: Effect of 6-SA on established Plasmodium berghei infection in mice. The experimental hosts were infected on day 0 and 'treated' orally, with saline containing 0.5% Tween-80, 6-SA at 5, 10 or 25 mg/kg·day or chloroquine at 5 mg/kg·day, on days 3–7.
Mentions: In both the four-day test and the test of repository activity, oral 6-SA produced dose-dependent chemosuppression (Table 1), with even the lowest dose tested (5 mg/kg·day) causing significant reductions in parasitaemia (P < 0.05). The highest dose of 6-SA tested (25 mg/kg·day) did not do well enough compared with the lowest dose tested (5 mg/kg·day), and did not quite reach the level of chemosuppression seen with the drugs used as positive controls–chloroquine at 5 mg/kg·day) or pyrimethamine at 1.2 mg/kg·day (Table 1). In the mice that were treated only from 72 hours post-infection, daily oral doses of 6-SA or chloroquine led to gradual reductions in parasitaemia over time, whereas the parasitaemias in the negative-control mice increased with time (Figure 2). All the mice administered with 6-SA showed a gradual decrease in body weight from day 7, but this weight loss lasted only for a few days, after which these mice gained weight daily. Mice in the negative-control group lost weight daily during the follow-up period. One of the five mice administered with 10 mg/kg·day 6-SA died before day 29 (on day 22), as did three of the five mice treated with 5 mg/kg·day (on days 18, 19 and 25) and all five of the negative-control mice (on days 11~18). None of the mice given the highest dose of 6-SA and none of those given chloroquine died during the follow-up period. The mean survival times of the mice administered 5, 10 or 25 mg/kg·day 6-SA, chloroquine and saline containing 0.5% Tween-80 were 24.0, 27.6, 30.0, 30.0 and 15 days, respectively. The mice still alive on day 29 (all of which had been treated with 6-SA or chloroquine) were aparasitaemic. In the tests of activity against established infections, the highest tested doses of 6-SA appeared as effective as chloroquine in terms of the day-7 parasitaemias (Figure 2) and day-29 survival.

Bottom Line: Petroleum ether extracts of Viola websteri Hemsl (Violaceae) were reported to have anti-plasmodial activity against Plasmodium falciparum in vitro, with this activity being largely attributable to 6-(8'Z-pentadecenyl)-salicylic acid (6-SA).The possible 'repository' activity of 6-SA was assessed using the method described by Peters.In the present study, 6-SA was found to have anti-malarial activity in vivo, when tested against P. berghei in mice. 6-SA at 5, 10 and 25 mg/kg x day exhibited a significant blood schizontocidal activity in four-day early infections, repository evaluations and established infections with a significant mean survival time comparable to that of the standard drug, chloroquine (5 mg/kg.day). 6-SA possesses a moderate anti-malarial activity that could be exploited for malaria therapy.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Diagnostics, College of Korean Medicine, Dongguk University, Gyeong-Ju 780-714, South Korea. himun68@daum.net

ABSTRACT

Background: Petroleum ether extracts of Viola websteri Hemsl (Violaceae) were reported to have anti-plasmodial activity against Plasmodium falciparum in vitro, with this activity being largely attributable to 6-(8'Z-pentadecenyl)-salicylic acid (6-SA).

Methods: The schizontocidal activity of 6-SA on early Plasmodium berghei infections was evaluated in a four-day test. The possible 'repository' activity of 6-SA was assessed using the method described by Peters. The median lethal dose (LD50) of 6-SA, when given intraperitoneally, was also determined using uninfected ICR mice and the method of Lorke.

Results: In the present study, 6-SA was found to have anti-malarial activity in vivo, when tested against P. berghei in mice. 6-SA at 5, 10 and 25 mg/kg x day exhibited a significant blood schizontocidal activity in four-day early infections, repository evaluations and established infections with a significant mean survival time comparable to that of the standard drug, chloroquine (5 mg/kg.day).

Conclusion: 6-SA possesses a moderate anti-malarial activity that could be exploited for malaria therapy.

Show MeSH
Related in: MedlinePlus