Table 2 Pharmacological studies of gossypol: molecular mechanisms and anticancer effects in various cancer models

In vitro

In vivo

HNC cell lines

(CAL-27, FaDu, A253);

BALB/c mice with SALTO cells

5–80 µM (in vitro); intratumoral and oral

(in vivo)

↑apoptosis

autophagy induction

[1]

In vitro

In vivo

Breast cancer cells

(MCF7, MDA-MB-231, MDA-MB-468, ZR-75-1, T47D);

MCF-7 and MDA-MB-468 xenografts in mice

100 µM

(in vitro);

10 mg/kg/day

(in vivo)

decreased cell growth;

↓MDM2, ↓VEGF

apoptosis promotion

[78]

[5]

In vitro

NSCLC cell lines

(H1975)

20 µM

-inhibition of cell proliferation and migration;

caspase-dependent apoptosis

[74]

80 µM

overcoming EGFR-TKIs resistance; targeting EGFRL858R/T790M and YAP/TAZ

[79]

In vitro

Human lung cancer cell lines (H1299, H358)

0.1–50 µM

inhibition of cullin neddylation

[82]

In vitro,

In vivo,  Clinical study

Gastroesophageal cancer cell lines; nude mice with JHESO cell xenografts

10 µM (in vitro);

7.5 mg/kg (in vivo)

growth inhibition; downregulation of YAP1, SOX9; combination treatment synergy

[61]

In vitro

Pancreatic cancer cell lines (BxPC-3, MIA PaCa-2)

200 µM

mitochondrial apoptosis via PERK-CHOP signaling

[32]

In vitro

Hepatoma

(HepG2, Hep3B)

colon carcinoma

(HCT-116, HT-29) cells

5–50 µM

reduced cell viability;

↑caspase 3/7 activity

[41]

In vitro

Human colon cancer cells (COLO 225)

100 µM

reduced cell viability; gene expression modulation

[6]

In vitro

In vivo

Cervical cancer cells

(HeLa, SiHa);

BALB/c AnN nude mice with SiHa cells

10 µM (in vitro);

10–20 mg/kg (in vivo)

inhibition of migration and invasion;

tumor growth reduction

[23]

In vitro

Prostate cancer cells

100 µM

inhibition of androgen formation;

5α-reductase and 3α-hydroxysteroid dehydrogenase inhibition

[7]