Further, anti-inflammatory activities of these alkaloids (20, 24, and 30) were
screened by xylene-induced ear edema and the carrageenan-induced air pouch
model. In xylene-induced ear edema, early-stage inflammation resulted in edematisation of the ear. Aspirin resulted in 45.7% inhibition in the edematisation. 20 at
10 mg/kg, i.g. and i.p. resulted in 41.9 and 41.5% inhibition. Although the i.g.
administration of 24 (5 mg/kg) and 30 (8 mg/kg) did not result in good inhibition, i.
p. administration exhibited significant inhibition on the edematisation (40.3 and
42.0%, respectively). In the carrageenan-induced air pouch model, various biochemical parameters raised from inflammatory responses were measured.
Prostaglandin E 2 (PGE 2 ), superoxide dismutase (SOD), nitric oxide (NO), and
malondialdehyde (MDA) were measured as the biochemical markers for the
inflammation. The screened alkaloids lowered the MDA levels in serum, reduced
NO production, and increased levels of SOD in exudate. The results indicated that
these alkaloids inhibited the lipid peroxidation and served as a free radical scavenging property by the antioxidant enzymes enhancement. Further, a decreased
level of PGE 2 in exudates suggested the ability of these alkaloids to interfere with
the COX pathways of arachidonic acid metabolism.
Sultana et al. isolated ten triterpenoid derivatives (32–41) from the ethanolic
extract of A. scholaris aerial parts (Fig. 14.5) and evaluated the anti-inflammatory
potential of newly isolated phytochemical, nighascholarene (34), ursane type
triterpenoid methyl ester (100 mg/kg), by carrageenan-induced paw edema test in
Wistar rats (Sultana et al. 2019). Compound 34 resulted in 44% inhibition in the
paw edema, while indomethacin resulted in 85% inhibition (positive control).
Table 14.3 Anti-inflammatory activities of various alkaloids from A. scholaris
Compound (at 100 µM)
COX-I
Inhibition (%)
COX-II
Inhibition (%)
5-LOX
Inhibition (%)
Alkaloids fraction
a
54.3
63.3
57.3
6
53.3
90.7
38.4
12
45.8
95.7
79.9
14
43.1
95.9
<0
19
44.7
96.4
79.5
24
44.7
92.0
31.0
25
38.5
91.1
57.3
27
47.0
95.6
<0
29
60.8
90.4
69.5
SC-560
61.3
–
–
NS-398
–
97.1
–
Zileuton
–
–
83.1
a At 300 µg/mL
14 Pharmaceutical Application of Bio-actives …
471
screened by xylene-induced ear edema and the carrageenan-induced air pouch
model. In xylene-induced ear edema, early-stage inflammation resulted in edematisation of the ear. Aspirin resulted in 45.7% inhibition in the edematisation. 20 at
10 mg/kg, i.g. and i.p. resulted in 41.9 and 41.5% inhibition. Although the i.g.
administration of 24 (5 mg/kg) and 30 (8 mg/kg) did not result in good inhibition, i.
p. administration exhibited significant inhibition on the edematisation (40.3 and
42.0%, respectively). In the carrageenan-induced air pouch model, various biochemical parameters raised from inflammatory responses were measured.
Prostaglandin E 2 (PGE 2 ), superoxide dismutase (SOD), nitric oxide (NO), and
malondialdehyde (MDA) were measured as the biochemical markers for the
inflammation. The screened alkaloids lowered the MDA levels in serum, reduced
NO production, and increased levels of SOD in exudate. The results indicated that
these alkaloids inhibited the lipid peroxidation and served as a free radical scavenging property by the antioxidant enzymes enhancement. Further, a decreased
level of PGE 2 in exudates suggested the ability of these alkaloids to interfere with
the COX pathways of arachidonic acid metabolism.
Sultana et al. isolated ten triterpenoid derivatives (32–41) from the ethanolic
extract of A. scholaris aerial parts (Fig. 14.5) and evaluated the anti-inflammatory
potential of newly isolated phytochemical, nighascholarene (34), ursane type
triterpenoid methyl ester (100 mg/kg), by carrageenan-induced paw edema test in
Wistar rats (Sultana et al. 2019). Compound 34 resulted in 44% inhibition in the
paw edema, while indomethacin resulted in 85% inhibition (positive control).
Table 14.3 Anti-inflammatory activities of various alkaloids from A. scholaris
Compound (at 100 µM)
COX-I
Inhibition (%)
COX-II
Inhibition (%)
5-LOX
Inhibition (%)
Alkaloids fraction
a
54.3
63.3
57.3
6
53.3
90.7
38.4
12
45.8
95.7
79.9
14
43.1
95.9
<0
19
44.7
96.4
79.5
24
44.7
92.0
31.0
25
38.5
91.1
57.3
27
47.0
95.6
<0
29
60.8
90.4
69.5
SC-560
61.3
–
–
NS-398
–
97.1
–
Zileuton
–
–
83.1
a At 300 µg/mL
14 Pharmaceutical Application of Bio-actives …
471