E. coli (ATCC 35150), P. aeruginosa (ATCC 27853), Salmonella enterica (ATCC
13311). All the isolated compounds (3-hydroxy-11-ursen-28,13-olide (90), 41, 50–
52 and 54) did not exhibit any antibacterial effects in gram-negative bacteria, while
in gram-positive bacteria, 50 and 41 exhibited a moderate potential (Table 14.9).
Further, a synergistic antibacterial effect was observed against B. cereus and S.
aureus by 41 in combination with ampicillin and tetracycline.
14.3.1.4 Nuclear Factor-jB (NF-jB) Inhibitory Activity and b2
Adrenoreceptor (AR) Activation
Hou et al. identified NF-jB inhibitors and b2-AR agonists from an alkaloidal
extract of A. scholaris via microfractionation bioactivity-based ultra-performance
liquid chromatography/mass spectrometry (Hou et al. 2012b). In the study, cytotoxicity of the compounds was determined via the quantities of lactate dehydrogenase (LDH). For the identification of NF-jB inhibition and b2 AR activation,
luciferase reporter assay was used. Preliminary UPLC-MS analysis identified 17
peaks for NF-jB inhibition, while 11 peaks were identified for b2 AR agonist
activity. According to the relative percent content, nine alkaloids, namely, 3, 18, 19,
20, 24, 27, 19(Z)-vallesamine (91), (Z)-alstoscholarine (92), and (E)-alstoscholarine
(93), were screened for individual screening (Fig. 14.19). Compared to control,
these compounds didn’t exhibit a significant level of LDH in the serum (10 or
100 µmol/L). The obtained results indicated that these compounds did not show
any kind of toxicity to the cells. Further, NF-jB inhibition activity of alkaloids in
Table 14.9 Antibacterial
effects of various triterpenoids
from A. scholaris
Compound
Minimum Inhibitory concentrations (µg/mL)
E. faecalis L. monocytogenes B. cereus
50
4
8
16
41
1
2
8
Ampicillin
2
1
128
Tetracycline 4
2
4
19(Z)-Vallesamine (91)
(E)-alstoscholarine (93)
O
O
N
H
N
O
(Z)-alstoscholarine (92)
O
O
N
H
N
O
N
H
N
COOCH 3
HO
Fig. 14.19 Chemical structures of various alkaloids from A. scholaris (91–93)
14 Pharmaceutical Application of Bio-actives …
481
13311). All the isolated compounds (3-hydroxy-11-ursen-28,13-olide (90), 41, 50–
52 and 54) did not exhibit any antibacterial effects in gram-negative bacteria, while
in gram-positive bacteria, 50 and 41 exhibited a moderate potential (Table 14.9).
Further, a synergistic antibacterial effect was observed against B. cereus and S.
aureus by 41 in combination with ampicillin and tetracycline.
14.3.1.4 Nuclear Factor-jB (NF-jB) Inhibitory Activity and b2
Adrenoreceptor (AR) Activation
Hou et al. identified NF-jB inhibitors and b2-AR agonists from an alkaloidal
extract of A. scholaris via microfractionation bioactivity-based ultra-performance
liquid chromatography/mass spectrometry (Hou et al. 2012b). In the study, cytotoxicity of the compounds was determined via the quantities of lactate dehydrogenase (LDH). For the identification of NF-jB inhibition and b2 AR activation,
luciferase reporter assay was used. Preliminary UPLC-MS analysis identified 17
peaks for NF-jB inhibition, while 11 peaks were identified for b2 AR agonist
activity. According to the relative percent content, nine alkaloids, namely, 3, 18, 19,
20, 24, 27, 19(Z)-vallesamine (91), (Z)-alstoscholarine (92), and (E)-alstoscholarine
(93), were screened for individual screening (Fig. 14.19). Compared to control,
these compounds didn’t exhibit a significant level of LDH in the serum (10 or
100 µmol/L). The obtained results indicated that these compounds did not show
any kind of toxicity to the cells. Further, NF-jB inhibition activity of alkaloids in
Table 14.9 Antibacterial
effects of various triterpenoids
from A. scholaris
Compound
Minimum Inhibitory concentrations (µg/mL)
E. faecalis L. monocytogenes B. cereus
50
4
8
16
41
1
2
8
Ampicillin
2
1
128
Tetracycline 4
2
4
19(Z)-Vallesamine (91)
(E)-alstoscholarine (93)
O
O
N
H
N
O
(Z)-alstoscholarine (92)
O
O
N
H
N
O
N
H
N
COOCH 3
HO
Fig. 14.19 Chemical structures of various alkaloids from A. scholaris (91–93)
14 Pharmaceutical Application of Bio-actives …
481