Cytotoxic Activities of Major Diterpenoid Constituents of Andrographis paniculata. in a Panel of Human Tumor Cell Lines

Figures & data

Figure 1The chemical structures of the diterpenoids of Andrographis paniculata. Nees. Source: Matsuda et al. (1994).

Table 1.. Cytotoxic activity (EC₅₀ values, 72 h) of diterpenoid constituents of A. paniculata. and positive controls against a variety of cell lines.

Cell lines	Andrographolide	14-Deoxyandrographolide	Andrographiside	14-Deoxy-11, 12-didehydroandrographolide	Neoandrographolide	Deoxyandrographiside	14-Deoxy-12-methoxyandrographolide	Vincristine sulfate	Etoposide
1. Caov-3	23.6	ND	ND	ND	ND	ND	ND	3.5	76.2
2. T-47D	13.3	2.8	ND	1.5	18.1	ND	9.9	21.7	1.9
3. Hs-578T	17.3	ND	ND	34.9	ND	ND	26.7	0.002	139.4
4. HepG2	29.4	28.3	ND	11.5	ND	ND	ND	0.340	ND
5. NCI-H23	9.9	26.4	ND	41.8	ND	ND	19.5	0.002	0.14

EC₅₀ values (µg/ml) were derived from the dose-response relationship for 3 independent experiments (n = 9) using GraphPadPrism software.

EC₅₀ from non–dose response curves were derived by 50% interpolation on fit spline point-to-point plots.

ND: Not determined, EC₅₀ values of the compound may be higher than maximum concentration tested, no inhibition or positive growth.

Figure 2The effect of (A) 14-Deoxy-11,12-didehydroandrographolide (EC₅₀ values of 1.520 µg/ml, 72 h) (B) DNase I (1 U/ml), (C) etoposide (EC₅₀ values of 1.9 µg/ml, 72 h), and (D) DMSO 1% (v/v) on T-47D cells as assayed with Deadend™ Colometric Apoptosis Detection System (Promega, USA). Arrows show darkly stained nuclei of T-47D cells indicating DNA fragmentation. No DNA fragmentation was observed in diterpenoid-treated cells. Trypan blue exclusion assay of the T-47D cells treated with 14-Deoxy-11,12-didehydroandrographolide (EC₅₀ values of 1.5 µg/ml, 72 h) for (E) 24 h and (F) 72 h. Arrow shows necrotic cell.

Figure 3The effect of 14-deoxy-11,12-didehydroandrographolide (EC₅₀ values of 1.52 µg/ml, 72 h), on T-47D cell line as stained with Annexin-V-FLUOS™ kit (Roche, Germany). (A and B). The effect of 1% (v/v) DMSO, control vehicle on T-47D cell line. (C) Positive annexin V (thick arrows) and propidium iodide (thin arrows) stained cells were noted. Original magnification × 100 (A) × 400 (B, C).

Matsuda T, Kuroyanagi M, Sugiyama S, Umehara K, Ueno A, Nishi K (1994): Cell differentiation-inducing diterpenes from Andrographis paniculata. Nees. Chem Pharm Bull (Tokyo) 42: 1216–1225. [PUBMED], [INFOTRIEVE], [CSA]

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