Anti-inflammatory activity in vitro and in vivo

In a study by Xiong et al.,1999, verbascoside was found to have nitric oxide radical scavenging

activity, which possibly contributes to its anti-inflammatory effect. Seven phenylethanoids, including

acteoside (verbascoside) at the concentration of 100–200 mM reduced (6.3–62.3%) nitrite

accumulation in lipopolysaccharide (0.1 μg/ml) stimulated J774.1 cells. At 200 mM, they inhibited by

32.2–72.4% nitrite accumulation induced by lipopolysaccharide (0.1 μg/ml)/ interferon-γ (100 U/ml) in

mouse peritoneal exudate macrophages. Furthermore, verbascoside inhibited formation of the 5-

lipoxygenase product 5-HETE and leucotriene B4 in human polymorphonuclear leukocytes.

Verbascoside (acteoside) had strong radical scavenging actions (Kimura et al., 1987).

Verbascoside’s anti-inflammatory activity was evaluated by the carrageenin-induced paw oedema test

in the rat. Verbascoside administered orally at 150 mg/kg inhibited carrageenan-induced rat paw

oedema by 94% after 3 hours (p<0.02), compared to 40% inhibition by indometacin at 10 mg/kg

(p<0.01) (Schapoval et al., 1998).

Furthermore, verbascoside was found to have anti-inflammatory effect against Dgalactosamin/lipopolysaccharide-induced

hepatitis in mice (Xiong et al., 1999).

A study done by Murai et al., 1995 showed that verbascoside had inhibitory effects on arachidonic acid

induced mouse ear oedema. 20 μl of arachidonic acid (100 mg) dissolved in acetone (1 ml) was

delivered to both the inner and outer surfaces of each of the right and left ears of mice. Verbascoside

inhibited oedema by 6% at 1 mg/ear, and 14% at 3 mg/ear (p<0.05).

Cardiovascular activity in vitro and in vivo

In isolated, perfused rat hearts (Langendorff model) verbacoside (1 mM) increased heart rate by 37%,

the force of contraction by 9% and coronary perfusion rate by 68%. Verbascoside significantly

increased chronotropism (p=0.010), inotropism (p=0.016) an coronary perfusion rate (p=0.016) when

tested against the competitive α-adrenergic blocker phentolamine (1 μM) (Pennacchio et al., 1999).

It has been reported that verbascoside increased perfused rat heart rate (Pennacchio et al., 1999).

However, verbascoside (acteoside) administered intravenously to normotensive pentothal

anaesthetised rats exhibited a dose-dependent decrease in systolic, diastolic and mean arterial blood

pressure; the median effective dose of 10 mg/kg reduced mean arterial blood pressure by 39% for 2-3

minutes, while heart rate also decreased (Ahmad and Rizwani, 1995).

Analgesic activity in vivo

Verbascoside (acteoside) exhibited analgesia on acetic acid-induced writhing and on tail pressure pain

in mice after oral administration of 300 mg/kg and 100 mg/kg, respectively. Verbascoside also caused

weak sedation by prolongation of pentobarbital-induced anesthesia and the depression of locomotion

enhanced by metamphetamine (Nakamura et al., 1997).

Antitumour activity in vivo

Verbascoside inhibited proliferation of human gastric adenocarcinoma MGc80-3 cell line by 53.2%

(p<0.001) at 20 μmol/l. When the verbascoside-treated cells were inoculated subcutaneously into

BALB/C nude mice, the rate of tumour development decreased by 75% compared to that of animals

receiving untreated cells. These effects were thought to be related to antioxidant properties of

verbascoside (Li et al., 1997).