BioMed Research International / 2015 / Article / Tab 1

Review Article

Potential Inhibitors for Isocitrate Lyase of Mycobacterium tuberculosis and Non-M. tuberculosis: A Summary

Table 1

Summary of potential inhibitors for MTB and non-MTB isocitrate lyase (ICL).

NumberPublished yearInhibitorSourceDescriptionTarget ICLInhibitio (IC50)Remarks

11977Itaconate [11, 14] 
Synthetic Succinate analogPseudomonas indigofera = 120Established inhibitor

219823-Nitropropionate [11, 15] 
SyntheticSuccinate analogPseudomonas indigofera = 120Established inhibitor

31990Mycenon [60] 
Mycena sp.FungiAcinetobacter calcoaceticus

Neurospora crassa

Ricinus communis

  

5.2 M 

7.4 M
No information on positive control

419903-Bromopyruvate [11, 16] 
SyntheticGlyoxylate analogEscherichia coli 3 MEstablished inhibitor

52005DNAzyme [41]SyntheticMycobacterium tuberculosis

62006Extract of traditional Chinese medicine [30]Zingiber officinale,
Illicium verum
PlantMycobacterium tuberculosis 47.7 μg/mL
18.2 μg/mL
Positive control
IC50 of itaconate
= 90 g/mL
(good inhibitory)

72007Hydroquinone derivatives [62] 
SyntheticCandida albicans 0.28–1.02 mMPositive control
IC50 of itaconate
= 0.06 mM
(weak inhibitory)

82007Halisulfate 1 [46, 47] 
Hippospongia sp.Marine spongeMagnaporthe grisea 12.6 MNo information on positive control
(high inhibitory)

92007Bromophenols [27] 
Odonthalia corymbifera Red algaeMagnaporthe grisea 2.0–2.8 MPositive control
IC50 of
3-nitropropionate
= 94.2 M
(high inhibitory)

102008Polyoxygenated diterpenes [61]
Phorbas sp.Marine spongeLC50 of
55–140 g/mL
No information on positive control
(weak inhibitory)

112008Meroditerpenoids [48]
Sargassum siliquastrum Brown algaeCandida albicans 50–95 g/mLNo information on positive control
(weak inhibitory)

122008Dihydroxystyrene metabolites [49]
Association of Poecillastra wondoensis and Jaspis sp.Marine spongeCandida albicans 28.7 to >200 μg/mLPositive control
IC50 of itaconate
= 5.8 g/mL
(weak to moderate inhibitory)

132008Sesterterpenoids [50]
Sarcotragus sp.Marine spongeCandida albicans 12.5–19.9 g/mLPositive control
IC50 of Itaconate
= 4.9 g/mL
(moderate to high inhibitory)

142008Sesterterpene sulfates [51]
Dysidea sp.Marine spongeCandida albicans 31.3–33.8 MPositive control IC50 of 3-nitropropionate
= 50.7 M
(high inhibitory)

152009Pthalazinyl derivatives [35]
SyntheticMycobacterium tuberculosis 45–61%
inhibition at 10 M
Positive control
3-nitropropionate has 63.2% inhibition at 100 M

162009Hyrtiosin B [52]
Hyrtios sp.Marine spongeCandida albicans 89 MPositive control
IC50 of
3-nitropropionate
= 50.7 M
(high inhibitory)

172010Phthalazin-4-ylacetamides [36]
SyntheticMycobacterium tuberculosis 40.62–66%
inhibition at 10 M
Positive control
3-nitropropionate has
68.2% inhibition at 100 M

182010Extract of traditional Chinese medicine (I2906) [31]
PlantMycobacterium tuberculosis 134 g/mLControl samples were untreated samples

1920105-Nitro-2-furoic acid hydrazones with furan-2-carbaldehyde [37]
Synthetic Mycobacterium tuberculosis 86.8%
inhibition at 10 mM
Positive control
3-nitropropionate has
63.2% inhibition at 100 M
(good inhibitory)

202010Bromophenols [63]
Synthetic Candida albicans 2.65 MPositive control
IC50 of
3-nitropropionate
= 50.7 μM
(high inhibitory)

2120105-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides [38]
Synthetic Mycobacterium tuberculosis 45.7%
inhibition at 10 mM
Positive control
3-nitropropionate has 68.2% inhibition at 100 M
(good inhibitory)

222010Indole-containing natural compound (analog) [64]
Synthetic Candida albicans 75 MPositive control
IC50 of
3-nitropropionate
= 50 M
(high inhibitory)

232010Isatinyl thiosemicarbazones derivatives [39]
Synthetic Mycobacterium tuberculosis 63.44%
inhibition at 10 mM
Positive control
3-nitropropionate has
65.9% inhibition at 100 mM
(good inhibitory)

242011Brominated resorcinol dimer [65]
SyntheticCandida albicans 28 MPositive control
IC50 of
3-nitropropionate
= 6.0 M
(good inhibitory)

252011Sargachromanols [53]
Sargassum siliquastrum Brown algaeCandida albicans 118.4–172.9 MPositive control
IC50 of
3-nitropropionate
= 34.8 M
(moderate inhibitory)

262011Scalarane sesterterpenes [54]
Hyatella sp.Marine spongeCandida albicans 40.8–55.3 MPositive control IC50 of 3-nitropropionate
= 27.9 M
(weak inhibitory)

272011Suvanine salt [55]
Coscinoderma sp.Marine spongeCandida albicans 5–17 MPositive control IC50
of 3-nitropropionate
= 27.9 M
(moderate inhibitory)

282011Chelerythrine extract [32]Chelidonium majus PlantMycobacterium tuberculosis Expression level decreased 5 fold

292011Mannich base, Ydcm67 [42]
SyntheticMycobacterium tuberculosis 57.4% inhibition at 0.05 mg/mLPositive control oxalic acid has 95.55% inhibition at 0.05 M

302011Peptide inhibitor [43]SyntheticMycobacterium tuberculosis Inhibition rate
38.2–47.92%
Samples contain no peptide inhibitor or ICL in reaction system as controls

3120113-Nitropropionamides derivatives [40]
SyntheticMycobacterium tuberculosis 0.1 MPositive control
IC50 of
3-nitropropionate
= 116.0 M
(good inhibitory)

322012Pyruvate-isoniazid analog with their copper complex [45]
SyntheticMycobacterium tuberculosis Inhibition rate
6–92%
Control docking using pyruvic acid

332012Bahamaolides A (macrolide) [56]
Streptomyces sp.Actinomycete (Actinobacteria)Candida albicans 10.8 MPositive control
IC50 of
3-nitropropionate
= 20.1 M
(high inhibitory)

342012Beta-carboline alkaloid [57]
Synoicum sp.Ascidian
(sea squirt)
Candida albicans 48.2–68.9 MPositive control
IC50 of
3-nitropropionate
= 38.6 M
(weak inhibitory)

352012Sphingolipid [58]
Spirastrella abata Marine spongeCandida albicans 2–87 MPositive control
IC50 of
3-nitropropionate
= 1.0 M
(weak to moderate inhibitory)

362012Thio benzanilide [66]
SyntheticMycobacterium tuberculosis 21–23% inhibition at 10 mol/L Positive control
3-nitropropionate has
25% inhibition at
10–100 mol/L

382012Salicylanilide derivatives [67]
SyntheticMycobacterium tuberculosis 22–59% inhibition at 10–100 mol/LPositive control
3-nitropropionate has
25–67% inhibition
at 10–100 mol/L

392013Tris-aromatic furanones [59]
Synoicum sp.Ascidian
(sea squirt)
Candida albicans 7.62–10.36 MPositive control IC50
of 3-nitropropionate
= 13.91 M
(Good inhibitory)

402013Heptapeptide [44]SyntheticMycobacterium tuberculosis 126 MPositive control
IC50 of
3-nitropropionate
= 50.7 M
(good inhibitory)

Inhibition default unit is IC50 unless other units are mentioned in the table.
Inhibitory potential of potential inhibitors was evaluated by the respective authors.