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. 2020 Jun 29;12(7):1721. doi: 10.3390/cancers12071721

Table 1.

(A) Half-maximal inhibitory concentrations (IC50) of taccalonolides in HeLa cells. (B) Details of in vivo tumor xenograft studies in mice using taccalonolides AF and AJ. IC50 of (C) persin and its analogues, and (D) curcumin, maytansine, combretastatin, noscapine, and quercetin in various cancer cell lines.

(A)
Compound IC50 (μM) Compound IC50 (μM) Compound IC50 (μM) Compound IC50 (μM) Compound IC50 Compound IC50 (μM) References:
[24,26,30,31,32]
Taccalonolide A 5.32 ± 0.23 Taccalonolide N 8.5 ± 0.40 Taccalonolide Z 0.12 ± 0.008 Taccalonolide AD 3.4 ± 0.2 Taccalonolide AO >50 Taccalonolide AN 1.5 ± 0.1
Taccalonolide B 3.12 ± 0.18 Taccalonolide I 49.2 ± 2.8 Taccalonolide AA 0.032 ± 0.002 Taccalonolide AE 5.0 ± 0.2 Taccalonolide AK >50 Paclitaxel 0.0012 ± 0.1
Taccalonolide E 39.5 ± 4.70 Taccalonolide R 13.0 ± 1.0 Taccalonolide AB 2.7 ± 0.1 Taccalonolide AF 0.023 ± 0.003 Taccalonolide AL 34.4 ± 7.5
Taccalonolide H2 0.73 ± 0.02 Taccalonolide T 0.34 ± 0.02 Taccalonolide AC >50 Taccalonolide AJ 0.0042 ± 0.0003 Taccalonolide AM 2.0 ± 0.1
(B)
Compound Xenograft Models Method of Tumor Cell Administration Treatment Strategy/Dose References
Taccalonolide AF and AJ MDA-MB-231 breast cancer intraperitoneal 1. Taccalonolide AF: 2 mg/kg on Days 1, 4, 8
2. Taccalonolide AF: 2.5 mg/kg on Days 1 and 5
3. Taccalonolide AJ: 0.5 mg/kg on Days 1, 3, 5, and 8
[27]
Taccalonolide AF and AJ SCC-4 oral cancer cells subcutaneous 1. Taccalonolide AF: 80 μg on Days 0 and 3
2. Taccalonolide AJ: 40 μg on Days 0 and 3
3. Taccalonolide AJ: 80 μg on Days 0 and 3
[34]
(C)
Breast Cancer Cell Lines Ovarian Cancer Cell Lines Prostate Cancer Cell Lines Leukemia Cell Lines References:
[35,36,37]
Compound (μM) MCF-7 T-47D MDA-MB-468 MDA-MB-157 SK-BR3 Hs578T MDA-MB-231 MCF-10A OVCAR-3 IGROV-1 1A9 A2780 PC-3 LNCaP HL-60
Persin 15.1 ± 1.3 30.3 ± 2.3 25.0 ± 2.8 12.8 ± 1.2 19.7 ± 1.3 32.1 ± 2.3 >39 >39 27.9 ± 4.5 15.6 ± 3.6 13.7 ± 0.6 8.1 ± 1.1 30.0 ± 3.0 22.0 ± 1.8 1.9 ± 0.1
1 17.1 ± 1.7 20.7 ± 3.2 >39 >39 >39 >39 >39 >39 >39 >39 4.1 ± 0.4 8.1 ± 1.4 >39 >39 0.6 ± 0.03
2 >32 18.9 ± 1.3 13.7 ± 0.9 4.0 ± 0.1
3 27.7 ± 5.5 19.4 ± 2.2 2.6 ± 0.4
4 >27 21.2 ± 1.8 7.5 ± 0.2
5 23.8 ± 2.2 34.1 ± 5.3 5.8 ± 0.1
6 29.0 ± 4.2 47.6 ± 3.5 28.4 ± 0.5
7 >21
8 >24
9 20.1 ± 3.6
10 >65 124 ± 20 22.8 ± 1.0
(D)
Breast Cancer Cell Lines Lung Cancer Cell Lines Squamous Carcinoma Cell Lines Lymphoma Cell Lines Ovarian Cancer Cell Line Cervical Cancer Cell Line Leukemia Cell Line Prostate Cancer Cell Line References
Compound MCF7 MDA-MB-231 BT-474 SK-BR3 MDA-MB-435 A594 H1299 H292 NCI-H358M Tu212 Tu686 BJAB OVCAR-8 HeLa HL60 LNCap PC3M
Curcumin (μM) 11.2 6.03 11.6 5.5 6.4 25.0 [38,39,40,41,42]
Maytansine (pM) 30 420 44 270 [43,44,45]
Combretastatin A4 (nM) 2.8 5.3 3.8 8 0.37 0.9 2.1 4.7 [46,47]
Noscapine (μM) 29 69 [48]
Quercetin (μM) 14 1 22 [49]