new antiplasmodial alkaloids from stephania rotunda lour. () sothavireak bory 1, sok siya bun 2,...
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New antiplasmodial alkaloids from
Stephania rotunda Lour. (កុ�មារពេ�ជ្រ�)
Sothavireak BORY1, Sok Siya BUN2, Béatrice BAGHDIKIAN2,
Valérie MAHIOU2, Nadine AZAS2, Hot BUN2, Evelyne OLLIVIER2.
1 Faculty of Pharmacy, University of Health Sciences-Cambodia.
2 UMR-MD3, Faculty of Pharmacy, Aix-Marseille University, France
Symposium on Biodiversity and Health
17-18 November 2014
2
INTRODUCTION
30 medicinal plants
suspected of
antiplasmodial activity
Symposium on Biodiversity and Health
17-18 November 2014
3
INTRODUCTION
Stephania rotunda Lour.
ពេកុ�មារពេ�ជ្រ�
Extract of tuber:
IC50 < 5 µg/mL
Stephania rotunda presents the most interesting antiplasmodial activity.
Symposium on Biodiversity and Health
17-18 November 2014
4
OBJECTIVES
Isolation and identification of the unknown alkaloids observed
on HPLC chromatograms for the different extracts,
Evaluation of the antiplasmodial activity of alkaloids from the
extracts of Stephania rotunda.
min0 5 10 15 20 25 30 35
mAU
0
25
50
75
100
125
150
175
DAD1 A, Sig=282,4 Ref=360,100 (STEPH\080109000001.D)
8.7
58
11
.48
4
15
.39
7
17
.38
5
24
.71
2
28
.21
4
31
.07
6
36
.53
0
min0 5 10 15 20 25 30 35
mAU
0
10
20
30
40
50
DAD1 A, Sig=282,4 Ref=360,100 (STEPH\080110000000.D)
2.5
86
4.7
46
8.0
89
10
.16
0
13
.09
6
15
.70
2
17
.31
8
20
.06
4
24
.76
5 28
.30
5
Symposium on Biodiversity and Health
17-18 November 2014
5
MATERIALS AND METHODS Plant material
Intrumentation
HPLC FC MS NMR
Phytochemistry:
Antiplasmodial activity: W2 Strain of Plasmodium falciparum
- IC50
- SI
Plants preparation
Herbarium specimens
Plants powder
Symposium on Biodiversity and Health
17-18 November 2014
RESULTS & DISCUSSION
6
Phytochimical study: HPLC, MS, 1D and 2D NMR
N
OCH3
OCH3
O
O
O NCH3
HCH3
H
ONH3CO
H3CO
OCH3
OCH3
N
H3CO
H3CO
OCH3
OCH3
Cepharanthine
Xylopinine Tetrahydropalmatine
min0 5 10 15 20 25 30 35
mAU
0
10
20
30
40
50
DAD1 A, Sig=282,4 Ref=360,100 (STEPH\080110000000.D)
2.5
86
4.7
46
8.0
89
10
.16
0
13
.09
6
15
.70
2
17
.31
8
20
.06
4
24
.76
5
28
.30
5
NCH3
O
O
Roemerine
N+
H3CO
H3CO
OCH3
OCH3
Pseudopalmatine
Palmatine
Symposium on Biodiversity and Health
17-18 November 2014
7
RESULTS & DISCUSSION
Phytochimical study: HPLC, MS, 1D and 2D NMR
NCH3
O
O
OCH3
H3CO
NCH3
O
O
OCH3
Stephanine
min0 5 10 15 20 25 30 35
mAU
0
25
50
75
100
125
150
175
DAD1 A, Sig=282,4 Ref=360,100 (STEPH\080109000001.D)
8.7
58
11
.48
4
15
.39
7
17
.38
5
24
.71
2
28
.21
4
31
.07
6
36
.53
0
Vireakine
Symposium on Biodiversity and Health
17-18 November 2014
RESULTS & DISCUSSION
In vitro antiplasmodial activity
8Symposium on Biodiversity and Health
17-18 November 2014
RESULTS & DISCUSSION
9Symposium on Biodiversity and Health
17-18 November 2014
C X T P CHL ART
C Additive Additive Synergism Additive
X Additive Synergism
T Additive Synergie Additive Additive Additive
P Additive Antagonism Additive
CHL Synergie Additive Antagonism
ART Additive Additive Additive
X : xylopinine, C : cepharanthine, T : tetrahydropalmatine, P: palmatine,
CHL: chloroquine, ART: artesunate.
In vitro antiplasmodial activity: Isobologram study
CONCLUSION
10
8 major alkaloids have been isolated and identified,
Vireakine is identified as a new compound,
Pseudopalmatine, stephanine and vireakine are described for the first time in the plant.
Phytochemical study:
Pseudopalmatine, cepharanthine, stephanine and vireakine are the most active compounds,
Isobologram: 2 synergistic effects and 1 antagonistic effect,
In vitro antiplasmodial activity:
This results justify the use of Stephania rotunda as
traditional medicine for the treatment of malaria.
Select the most promising drug-candidates for further
investigations.
Symposium on Biodiversity and Health
17-18 November 2014
11
2010
2012
2013
2014
2014
2010
Symposium on Biodiversity and Health
17-18 November 2014
12
THANK YOU FOR YOUR ATTENTION
Symposium on Biodiversity and Health
17-18 November 2014
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