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Table 1 In vitro activity of Aspidosperma olivaceum extracts and fractions against P. falciparum chloroquine-resistant blood parasites (W2 clone), cytotoxicity (MDL 50 ) to a human hepatoma cell line (HepG2), and selectivity index (SI), the ratio between the MDL 50 and IC 50

From: Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum

Compound* MDL50(μg/mL) IC50(μg/mL)** SI***
[3H]-hypoxanthine Anti-HRPII
Bark extract and fractions
 Crude bark extract 177 ± 4.0 10.6 ± 3.0 9.9 ± 4.5 17
 Acid fraction 330 ± 54.0 6.4 ± 2.3 5.5 ± 2.5 52
 Neutral fraction 20 ± 3.0 2.0 ± 0.2 2.1 ± 0.5 10
 Basic fraction 27 ± 0.0 4.3 ± 2.5 3.8 ± 0.4 <6
 Neutral precipitate (NP) 455 ± 100.0 6.7 ± 3.3 5.0 ± 2.5 68
Leaf extract and fractions     
 Crude leaf extract 904 ± 135.4 7.2 ± 2.3 9.2 ± 5.4 126
 Basic residue 415 ± 98.8 4.5 ± 0.7 2.0 ± 1.5 92
 Acid fraction 441 ± 59.0 8.5 ± 3.5 5.3 ± 1.1 52
Pure substance from extracts*     
 (1) Aspidoscarpine # 301 ± 24.0 5.4 ± 2.5 4.4 ± 0.8 56
 (2) Uleine 52 ± 10.0 7.0 ± 0.0 3.2 ± 1.8 18
 (3) Apparacine 41 ± 2.8 3.0 ± 1.4 3.2 ± 2.7 14
 (5 N-methyl-tetrahydrolivacine 126 ± 6.0 5.7 ± 3.3 4.0 ± 2.8 22
  1. *The steps for the bio-fractionation of the extracts are summarized in Figure 1.
  2. **IC50 = dose inhibiting 50% of parasite growth, evaluated in three or four different experiments for each test.
  3. *** SI = values obtained using the [3H]-hypoxanthine test; toxicity considered present at an SI <10.
  4. #Compound (1) was isolated from the leaves and bark. The compounds are numbered 1, 2, 3, and 5 as in Figure 2; their complete names and structures are listed in Figure 1.