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INNOSC Theranostics and
Pharmacological Sciences Anticancer activity of cyanobacteria

in fighting cancer makes it a promising candidate for Synechocystis salina, and Nodosilinea sp., are the principal
further study and development [29-34] . sources of this compound . According to Afonso et al.,
[39]
[28]
Bartoloside A has been found to have anticancer effect on
3.2. Cyclic peptides and depsipeptides human osteosarcoma (MG-63), colon carcinoma (RKO),
3.2.1. Dolastatins and human breast cancer (T-47D) cells, with IC values of
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22, 40, and 23 μM, respectively.
Dolastatins represent a group of cyclic and linear peptides,
depsipeptides, and macrolides, containing oxazole 3.5. Linear peptides
heterocycles and thiazole. These peptides are derived
from Symploca sp. Dolastatin 10 and 15 (Figure 4) can 3.5.1. Bisebromoamides
depolymerize microtubules and are also capable of Bisebromoamides are linear peptides (Figure 4) derived
inducing apoptosis by arresting the cell cycle in the G2/M from Lyngbya sp. They are known to impair actin dynamics
phase of various cancer cell lines, including A549, KB, and have demonstrated anticancer properties against
DU-145, and LoVo cells. Their IC values are 0.97, 0.052, various cancer cell lines, including HeLa S3, JFCR39 (a
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0.5, and 0.076 nM, respectively . panel of 39 human cancers) , NRK, 769-P, 786-O kidney
[40]
[9]
cancer cells , and HCT-116 (with EC ranging between
[41]
50
3.2.2. Symplostatin 1 45 and 483 nM) . The compound showed an IC of 40
[42]
50
Symplostatin 1 (Figure 4), a dolastatin 10 analog derived nM against HeLa S3 cells and a GI of 40 nM against
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[40]
from marine cyanobacteria Symploca hydnoides, is shown JFCR39 cells .
to possess potent cytotoxic effects against MDA-MB-435
(breast cancer) and ovarian cancer cell lines (IC50 of 0.15 3.5.2. Carmaphycins
and 0.09 nM, respectively). An in vivo study revealed Extracted from Symploca sp., carmaphycins A and B
that symplostatin 1 can effectively suppress the growth of (Figure 4) are new forms of marine-based epoxyketone
murine mammary 16/C and murine colon 38 cell lines, 20S proteasome inhibitors. These substances have
which took a longer time for the cells to recover from demonstrated strong anticancer effect against NCI-H460,
toxicity . HCT-116, and the NCI-60 cell lines, with a GI range of
[35]
50
1 – 50 nM .
[43]
3.3. Macrolides
3.3.1. Caylobolide 3.6. Depsipeptides
Caylobolides (Figure 4) are macrolides (macrolactones) 3.6.1. Anaenamides
isolated from the Phormidium sp. and L. majuscula. Anaenamides A and B are new geometric isomers
Caylobolide A exhibited cytotoxic properties against HCT- and linear depsipeptides derived from Hormoscilla sp.
116 cells (human colon tumor) with an IC of 9.9 μM , These compounds contain two α-hydroxy acid residues,
[36]
50
while caylobolide B showed anticancer activity against an alkylated-salicylic fragment, and an abnormal
HeLa and HT-29 cells, with IC values of 12.2 and 4.5 μM, α-chlorinated-α,β-unsaturated (E/Z) ester. Anaenamides
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respectively . A and B (Figure 4) were found to have mild anticancer
[37]
properties against the HCT-116 cell line, with IC
3.3.2. Swinholide values of 4.5 and 8.7 μM, respectively . Different from
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[44]
Swinholide is a type of macrolide containing a unique, larger anaenamides A and B, anaenamides C and D possesses
lactone ring structure known as a dimeric 44-membered a primary amide instead of a methyl ester. However,
ring (Figure 4). Swinholide A is derived from Phormidium anaenamides C and D have been demonstrated to display
sp. and has been found to possess anti-cancer properties anticancer effect against HCT-116 cells at an IC of 100
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against fibrosarcoma cells (HT-1080) and H-460, with μM but no cytotoxic activity against human embryonic
IC values of 0.017 μg/mL and between 170 and 910 nM, kidney cells (HEK293) [44,45] .
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respectively [28,38] .
3.7. Linear lipopeptides
3.4. Glycolipids 3.7.1. Almiramides
3.4.1. Bartolosides Almiramides are linear lipopeptides that are highly
Bartoloside (Figure 4) is a newly discovered type of N-methylated. They are derived from Oscillatoria
chlorinated aromatic glycolipid. It is composed of nigroviridis and L. majuscula. Almiramides B and D
mono- and/or di-glycosylated dialkylresorcinols (DARs) (Figure 5) have been found to display strong cytotoxic
with halogenated alkyl moieties. The marine cyanobacteria, effects against MDA-MB-231, with an IC of 13 μM .
[46]
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Volume 7 Issue 1 (2024) 6 https://doi.org/10.36922/itps.1388