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. 2024 Feb 23;22(3):101. doi: 10.3390/md22030101

Table 3.

Antitumor activity of compounds from minority orders in lung cancer.

Sponge Compounds Chemical Class Methods of Production Cell Line (NSCLC/SCLC) IC50 In Vivo * Molecular Mechanism Ref.
Iotrochota purpurea itampolin A derivative (52) Brominated tyrosine alkaloid Chemical synthesis A549 (NSCLC) 0.66 μM (48 h) Decreased expression of phospho-p38 [48]
Mycale henscheli peloruside A (53) Polyketide Isolation and chemical synthesis (both methods) NR NR (H460 xenografts) Dose-dependent decrease in tumor growth, with TGI values of 88% at 5 mg/kg and 99% at 10 mg/kg, with no deaths. (A549 Xenografts) TGI ranging from 51% to 74% [49]
Phakellia fusca phakellistatin 17 (54), phakellistatin 18 (55), phakellistatin 18 analog 1 (56), and phakellistatin 18 analog 2 (57) Proline-rich cyclopeptides Chemical synthesis A549 (NSCLC) 54: >100 μM
55: 72.42 μM
56: 67.53 μM
57: 79.71 μM
(72 h)
NR [50]
Jaspis stellifera stellettin B (Stel B) (58) Isomalabaricane triterpene Isolation A549 (NSCLC) 0.022 μM
(48 h)
Targeting PI3K/Akt/mTOR pathway. Induction of G1 arrest (↑p27 and ↓cyclin D1), apoptosis (↑PARP cleavage and ↑ROS generation), and autophagy (↑LC3B II/I, ↑Atg5, and ↓p62). [51]
Raspailia bouryesnaultae raspailol (59), raspadiene (60), kerlinic acid (61), kerlinic acid methyl ester (62), annonene (63), and 6-hydroxyannonene (64) Clerodane diterpenes Isolation A549 (NSCLC) 59: 24.12 μM
60: 100.3 μM
61: 66.22 μM
62: 20.63 μM
63: 143.7 μM
64: 24.52 μM
(48 h)
NR [54]
Acanthodendrilla sp. (S)- acanthodendrilline (65) and (R)- acanthodendrilline (66) Bromotyrosine alkaloid Chemical synthesis H292 (NSCLC) 65: 58.5 ± 6.7 μM
66: 173.5 ± 24.7 μM
(72 h)
NR [55]
Chondrosia corticata halichondramide (67), jaspisamide A (68), neohalichondramide (69), halishigamide D (70), and (19Z)-halichondramide (71) Oxazole-containing macrolide Isolation A549 (NSCLC) 67: 0.045 μM
68: 32.63 μM
69: 3.73 μM
70: 1.65 μM
71: 0.024 μM
(72 h)
G2/M cell cycle arrest (↑p53, ↑GADD45α, ↓cyclin B1, ↓cyclin A, ↓CDC2, and ↓CDC25C) and suppression of the Akt/mTOR signaling pathway (71). [56]
Ianthella basta bastadin-6 (72), bastadin-9 (73), bastadin-16 (74), methyl-[2-hydroxyimino-3-(4-hydroxyphenyl)]-propionate (75), methyl-[2-hydroxyimino-3-(3,5-dibromo-4-hydroxyphenyl)]-propionate (76), norbromohemibastadin-1 (77), L-tyrosine-tyramide A (78), and 5,5′-dibromohemibastadin-1 (79) Bastadins 7274: Isolation
48: Chemical synthesis
A549 (NSCLC) 72: 3 μM
73: 7 μM
74: 8 μM
7578: >100 μM
79: 68 μM
(72 h)
NR [57]
NR alkaloid analogs with 2-amino-1H-imidazole core Alkaloid Chemical synthesis A549 (NSCLC) 14.15–43.72 μM (72 h) Inhibition of tumor growth in A549 xenograft models. [58]

* in vivo in lung cancer; not reported, NR; tumor growth inhibition, TGI; non-small-cell lung cancer, NSCLC; non-tumoral, NT; phosphatidylinositol 3-kinase, PI3K; protein kinase B, Akt; serine/threonine-protein kinase mTOR, mTOR; cyclin-dependent kinase inhibitor 1B, p27; poly (ADP-ribose) polymerase, PARP; reactive oxygen species, ROS; microtubule-associated proteins 1A/1B light chain 3B, LC3B; autophagy-related 5, Atg5; tumor protein P53, p53; growth arrest and DNA damage inducible alpha, GADD45α; cyclin-dependent kinase-1, CDC2; cell division cycle 25C, CDC25C; no in vivo evaluation in lung cancer, ✗; in vivo evaluation in lung cancer, ✓; increase, ↑; decrease, ↓.