reduction in systemic arterial blood pressure and heart rate were observed in normotensive albino rats (for blood pressure-8.5–77.2% for 5–180 min; for heart
rate-6–63% at a concentration range of 0.05–10.0 mg/kg i.v of 9) and cats (at a
concentration range of 0.025–10.0 mg/kg i.v of 9). In vivo neuromuscular activity
screening revealed that 9 (5–20 mg/kg, i.p.) depressed (23–81%) the twitches of the
cat anterior soleus or tibialis muscle preparation induced by indirect electrical
stimulation. At a concentration range of 10–100 µg/mL of 9, spontaneously beating
atria isolated from the guinea pig reduced the amplitude and rate of contractions.
However, in the electrically driven left atria, the force of contraction was also
reduced. In the isolated smooth muscles, a depression in the amplitude of the
spontaneous myogenic contractions was observed with the administration of 9 (10–
100 µg/mL).
14.3.4.2 Antiarthritic Effect
Okai and Carroll isolated 39 from the petroleum ether extract of A. boonei root
barks and evaluated its antiarthritic effect in complete Freund’s adjuvant (CFA)induced arthritic Wistar rats (Kweifio Okai and Carroll 1993). At the treatment
periods, 66 mg/kg body weight of 39 was administered orally in every 48 h from
32 to 40 days of post-adjuvant. Ankle and paw diameters remained unchanged
among the treatment and control groups. Among the various biochemical parameters, alkaline phosphatase (U/L), spleen weight (g%) were altered during the
arthritic conditions (control-265 U/L and 0.19 g%, respectively; arthritic rats-219
U/L and 0.22 g%, respectively). However, treatment with 39 returned the increase
in spleen weight (0.20 g%) and the reduction in serum alkaline phosphatase (272 U/
L).
In another study, Okai et al. investigated the antiarthritic effects of a-amyrin
palmitate (215, Fig. 14.41) in complete Freund’s adjuvant (CFA)-induced arthritic
Wistar rats (Kweifio Okai et al. 1995). However, in the study, acute and chronic
arthritic conditions were identified and evaluated for the effects of 215. During the
acute phase, the ipsilateral ankle swelling was rapidly increased from 60% (11 days
after CFA induction) to 94% (19 days after CFA induction). In the chronic phase,
the percent swelling was similar from 32 to 50 days. Treatment of 215 prevented
the percentage swelling rate by 34% in acute arthritic conditions. Higher blood
granulocyte and serum hyaluronate were observed in the acute conditions of
arthritis with the control groups (1292–9827 Â 10
6 /L and 181–287 µg/L). In
chronic conditions also these biochemical parameters were increased from the
control groups (Blood granulocytes from 668 to 2287 Â 10
6 /L and Serum hyaluronate from 100 to 277 µg/L). However, 215 treatment results in declined biochemical parameters (For acute condition: blood granulocytes-5681 Â 10
6
/L and
Serum hyaluronate-149 µg/L; for chronic conditions: blood granulocytes—
1813 Â 10
6 /L and Serum hyaluronate—147 µg/L).
502
A. T. Paul et al.
rate-6–63% at a concentration range of 0.05–10.0 mg/kg i.v of 9) and cats (at a
concentration range of 0.025–10.0 mg/kg i.v of 9). In vivo neuromuscular activity
screening revealed that 9 (5–20 mg/kg, i.p.) depressed (23–81%) the twitches of the
cat anterior soleus or tibialis muscle preparation induced by indirect electrical
stimulation. At a concentration range of 10–100 µg/mL of 9, spontaneously beating
atria isolated from the guinea pig reduced the amplitude and rate of contractions.
However, in the electrically driven left atria, the force of contraction was also
reduced. In the isolated smooth muscles, a depression in the amplitude of the
spontaneous myogenic contractions was observed with the administration of 9 (10–
100 µg/mL).
14.3.4.2 Antiarthritic Effect
Okai and Carroll isolated 39 from the petroleum ether extract of A. boonei root
barks and evaluated its antiarthritic effect in complete Freund’s adjuvant (CFA)induced arthritic Wistar rats (Kweifio Okai and Carroll 1993). At the treatment
periods, 66 mg/kg body weight of 39 was administered orally in every 48 h from
32 to 40 days of post-adjuvant. Ankle and paw diameters remained unchanged
among the treatment and control groups. Among the various biochemical parameters, alkaline phosphatase (U/L), spleen weight (g%) were altered during the
arthritic conditions (control-265 U/L and 0.19 g%, respectively; arthritic rats-219
U/L and 0.22 g%, respectively). However, treatment with 39 returned the increase
in spleen weight (0.20 g%) and the reduction in serum alkaline phosphatase (272 U/
L).
In another study, Okai et al. investigated the antiarthritic effects of a-amyrin
palmitate (215, Fig. 14.41) in complete Freund’s adjuvant (CFA)-induced arthritic
Wistar rats (Kweifio Okai et al. 1995). However, in the study, acute and chronic
arthritic conditions were identified and evaluated for the effects of 215. During the
acute phase, the ipsilateral ankle swelling was rapidly increased from 60% (11 days
after CFA induction) to 94% (19 days after CFA induction). In the chronic phase,
the percent swelling was similar from 32 to 50 days. Treatment of 215 prevented
the percentage swelling rate by 34% in acute arthritic conditions. Higher blood
granulocyte and serum hyaluronate were observed in the acute conditions of
arthritis with the control groups (1292–9827 Â 10
6 /L and 181–287 µg/L). In
chronic conditions also these biochemical parameters were increased from the
control groups (Blood granulocytes from 668 to 2287 Â 10
6 /L and Serum hyaluronate from 100 to 277 µg/L). However, 215 treatment results in declined biochemical parameters (For acute condition: blood granulocytes-5681 Â 10
6
/L and
Serum hyaluronate-149 µg/L; for chronic conditions: blood granulocytes—
1813 Â 10
6 /L and Serum hyaluronate—147 µg/L).
502
A. T. Paul et al.