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. 2015 Jan 8;2015:895453. doi: 10.1155/2015/895453

Table 1.

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

Number Published year Inhibitor Source Description Target ICL Inhibition* (IC50) Remarks
1 1977 Itaconate [11, 14] 
Inline graphic
Synthetic Succinate analog Pseudomonas indigofera K i = 120 Established inhibitor

2 1982 3-Nitropropionate [11, 15] 
Inline graphic
Synthetic Succinate analog Pseudomonas indigofera K i = 120 Established inhibitor

3 1990 Mycenon [60] 
Inline graphic
Mycena sp. Fungi Acinetobacter calcoaceticus

Neurospora crassa

Ricinus communis

  

5.2 μM 

7.4 μM
No information on positive control

4 1990 3-Bromopyruvate [11, 16] 
Inline graphic
Synthetic Glyoxylate analog Escherichia coli 3 μM Established inhibitor

5 2005 DNAzyme [41] Synthetic Mycobacterium tuberculosis

6 2006 Extract of traditional Chinese medicine [30] Zingiber officinale,
Illicium verum
Plant Mycobacterium tuberculosis 47.7 μg/mL
18.2 μg/mL
Positive control
IC50 of itaconate
= 90 μg/mL
(good inhibitory)

7 2007 Hydroquinone derivatives [62] 
Inline graphic
Synthetic Candida albicans 0.28–1.02 mM Positive control
IC50 of itaconate
= 0.06 mM
(weak inhibitory)

8 2007 Halisulfate 1 [46, 47] 
Inline graphic
Hippospongia sp. Marine sponge Magnaporthe grisea 12.6 μM No information on positive control
(high inhibitory)

9 2007 Bromophenols [27] 
Inline graphic
Odonthalia corymbifera Red algae Magnaporthe grisea 2.0–2.8 μM Positive control
IC50 of
3-nitropropionate
= 94.2 μM
(high inhibitory)

10 2008 Polyoxygenated diterpenes [61]
Inline graphic
Phorbas sp. Marine sponge LC50 of
55–140 μg/mL
No information on positive control
(weak inhibitory)

11 2008 Meroditerpenoids [48]
Inline graphic
Sargassum siliquastrum Brown algae Candida albicans 50–95 μg/mL No information on positive control
(weak inhibitory)

12 2008 Dihydroxystyrene metabolites [49]
Inline graphic
Association of Poecillastra wondoensis and Jaspis sp. Marine sponge Candida albicans 28.7 to >200 μg/mL Positive control
IC50 of itaconate
= 5.8 μg/mL
(weak to moderate inhibitory)

13 2008 Sesterterpenoids [50]
Inline graphic
Sarcotragus sp. Marine sponge Candida albicans 12.5–19.9 μg/mL Positive control
IC50 of Itaconate
= 4.9 μg/mL
(moderate to high inhibitory)

14 2008 Sesterterpene sulfates [51]
Inline graphic
Dysidea sp. Marine sponge Candida albicans 31.3–33.8 μM Positive control IC50 of 3-nitropropionate
= 50.7 μM
(high inhibitory)

15 2009 Pthalazinyl derivatives [35]
Inline graphic
Synthetic Mycobacterium tuberculosis 45–61%
inhibition at 10 μM
Positive control
3-nitropropionate has 63.2% inhibition at 100 μM

16 2009 Hyrtiosin B [52]
Inline graphic
Hyrtios sp. Marine sponge Candida albicans 89 μM Positive control
IC50 of
3-nitropropionate
= 50.7 μM
(high inhibitory)

17 2010 Phthalazin-4-ylacetamides [36]
Inline graphic
Synthetic Mycobacterium tuberculosis 40.62–66%
inhibition at 10 μM
Positive control
3-nitropropionate has
68.2% inhibition at 100 μM

18 2010 Extract of traditional Chinese medicine (I2906) [31]
Inline graphic
Plant Mycobacterium tuberculosis 134 μg/mL Control samples were untreated samples

19 2010 5-Nitro-2-furoic acid hydrazones with furan-2-carbaldehyde [37]
Inline graphic
Synthetic Mycobacterium tuberculosis 86.8%
inhibition at 10 mM
Positive control
3-nitropropionate has
63.2% inhibition at 100 μM
(good inhibitory)

20 2010 Bromophenols [63]
Inline graphic
Synthetic Candida albicans 2.65 μM Positive control
IC50 of
3-nitropropionate
= 50.7 μM
(high inhibitory)

21 2010 5-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides [38]
Inline graphic
Synthetic Mycobacterium tuberculosis 45.7%
inhibition at 10 mM
Positive control
3-nitropropionate has 68.2% inhibition at 100 μM
(good inhibitory)

22 2010 Indole-containing natural compound (analog) [64]
Inline graphic
Synthetic Candida albicans 75 μM Positive control
IC50 of
3-nitropropionate
= 50 μM
(high inhibitory)

23 2010 Isatinyl thiosemicarbazones derivatives [39]
Inline graphic
Synthetic Mycobacterium tuberculosis 63.44%
inhibition at 10 mM
Positive control
3-nitropropionate has
65.9% inhibition at 100 mM
(good inhibitory)

24 2011 Brominated resorcinol dimer [65]
Inline graphic
Synthetic Candida albicans 28 μM Positive control
IC50 of
3-nitropropionate
= 6.0 μM
(good inhibitory)

25 2011 Sargachromanols [53]
Inline graphic
Sargassum siliquastrum Brown algae Candida albicans 118.4–172.9 μM Positive control
IC50 of
3-nitropropionate
= 34.8 μM
(moderate inhibitory)

26 2011 Scalarane sesterterpenes [54]
Inline graphic
Hyatella sp. Marine sponge Candida albicans 40.8–55.3 μM Positive control IC50 of 3-nitropropionate
= 27.9 μM
(weak inhibitory)

27 2011 Suvanine salt [55]
Inline graphic
Coscinoderma sp. Marine sponge Candida albicans 5–17 μM Positive control IC50
of 3-nitropropionate
= 27.9 μM
(moderate inhibitory)

28 2011 Chelerythrine extract [32] Chelidonium majus Plant Mycobacterium tuberculosis Expression level decreased 5 fold

29 2011 Mannich base, Ydcm67 [42]
Inline graphic
Synthetic Mycobacterium tuberculosis 57.4% inhibition at 0.05 mg/mL Positive control oxalic acid has 95.55% inhibition at 0.05 M

30 2011 Peptide inhibitor [43] Synthetic Mycobacterium tuberculosis Inhibition rate
38.2–47.92%
Samples contain no peptide inhibitor or ICL in reaction system as controls

31 2011 3-Nitropropionamides derivatives [40]
Inline graphic
Synthetic Mycobacterium tuberculosis 0.1 μM Positive control
IC50 of
3-nitropropionate
= 116.0 μM
(good inhibitory)

32 2012 Pyruvate-isoniazid analog with their copper complex [45]
Inline graphic
Synthetic Mycobacterium tuberculosis Inhibition rate
6–92%
Control docking using pyruvic acid

33 2012 Bahamaolides A (macrolide) [56]
Inline graphic
Streptomyces sp. Actinomycete (Actinobacteria) Candida albicans 10.8 μM Positive control
IC50 of
3-nitropropionate
= 20.1 μM
(high inhibitory)

34 2012 Beta-carboline alkaloid [57]
Inline graphic
Synoicum sp. Ascidian
(sea squirt)
Candida albicans 48.2–68.9 μM Positive control
IC50 of
3-nitropropionate
= 38.6 μM
(weak inhibitory)

35 2012 Sphingolipid [58]
Inline graphic
Spirastrella abata Marine sponge Candida albicans 2–87 μM Positive control
IC50 of
3-nitropropionate
= 1.0 μM
(weak to moderate inhibitory)

36 2012 Thio benzanilide [66]
Inline graphic
Synthetic Mycobacterium tuberculosis 21–23% inhibition at 10 μmol/L Positive control
3-nitropropionate has
25% inhibition at
10–100 μmol/L

38 2012 Salicylanilide derivatives [67]
Inline graphic
Synthetic Mycobacterium tuberculosis 22–59% inhibition at 10–100 μmol/L Positive control
3-nitropropionate has
25–67% inhibition
at 10–100 μmol/L

39 2013 Tris-aromatic furanones [59]
Inline graphic
Synoicum sp. Ascidian
(sea squirt)
Candida albicans 7.62–10.36 μM Positive control IC50
of 3-nitropropionate
= 13.91 μM
(Good inhibitory)

40 2013 Heptapeptide [44] Synthetic Mycobacterium tuberculosis 126 μM Positive control
IC50 of
3-nitropropionate
= 50.7 μM
(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.