Characterisation and antimalarial activities of metabolites from leaves of Anonidium mannii By GP Makoni Supervisor: Prof RW Krause 42 nd Annual SACI
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Characterisation and antimalarial activities of metabolites from leaves of
Anonidium mannii
ByGP Makoni
Supervisor: Prof RW Krause
42nd Annual SACI Conference 2015 KZN
2 December 2015
Malaria: The case
2
Malaria: Drug target area
3
Bioassays• Antimalarial• Cytotoxicity• Microbial
Evaluate• Active secondary
metabolites in Anonidium mannii
Identify
• New drugs• Scaffolds
Add value
• Ethno-medicinal uses
Validate
Objectives of
Research
4
Anonidium mannii• Belongs to the Annonaceae
family and is native to Cameroon.
• Ethno medicinal uses include:
1. Malaria
2. Gonorrhoea
3. Dysentery
4. Cancer
5. Skin inflammation5
MethodologySolvent extraction
1:1 DCM: MeOH
VLCGradient elution
CCActive fractions
AntimalarialCell cytotoxicity &
anticancer
Microbial assays
Bioassay
6
Structure elucidation
2D NMR
1D NMR
MS
FTIR
MP
CHNS
COSY
HSQC HMBC
NOESY
1H NMR
13CNMR
DEPT135Structure
elucidation
77
Results%
via
bilit
y
Cytotoxicity and pLDH comparison
8
pLDH
Cell cytotoxicity
Suggested structures
AM1C yield 1.94% or 0.09% AM2C 1.06% & 0.05%
AM3C 0.33% &0.02%9
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 22
2421
27
26
25
23
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 2224
26
27
28
29
30
2325
21
12
34
56
7
89
10
11
1213
14 15
16
1718
1920
21
22
23
24
25
26
29
30
31
27
28
32
33
HO
AM1C 1HNMR
10
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 2224
26
27
28
29
30
2325
21
AM1C 13CNMR
11
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 2224
26
27
28
29
30
2325
21
AM1C COSY
12
H20
H20
H21
H21
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 2224
26
27
28
29
30
2325
21
AM1C HMBC
C9
H7H14
H12 H18
HO
OH
12
34
56
7
8109
11
14
13
15
16
1712
18
19 20 2224
26
27
28
29
30
2325
21
13
Conclusion & comments
• Antimalarial screening has shown that there are metabolites in Anonidium mannii that are active against malaria.
• Work is still in progress to further investigate the cytotoxic fraction for their anti-cancer activities.
• Structural elucidation is still in progress for the other pure metabolites extracted.
• SAR & absolute configuration are still under consideration.
14
Acknowledgements
• My supervisor: Prof. R Krause
• Dr X Siwe Noundou
• Rhodes University Chemistry Dept
• Rhodes Sandisa Imbewu Fund
THANK YOU
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