Table 1.
Summary of the biological evaluations results.
| Compound | Source | Antibacterial (Positive Control Value) | Cytotoxic (Positive Control Value) |
|---|---|---|---|
| JBIR-99 (45a) | marine sponge-derived fungus Tritirachium sp. Sp081112MEf2 and marine fungus Engyodontium album Strain LF069 |
Staphylococcus epidermidis IC50 0.21 ± 0.09 μM (chloramphenicol IC50 1.8 ± 0.04 μM) Staphylococcus aureus IC50 0.25 ± 0.07 μM (chloramphenicol IC50 2.9 ± 0.5 μM) |
NIH 3T3 IC50 13.2 ± 2.7 μM (amoxifen citrate IC50 16.5 ± 0.2 μM) |
| Engyodontochone B (45b) | marine fungus Engyodontium album Strain LF069 |
Staphylococcus epidermidis IC50 0.22 ± 0.03 μM (chloramphenicol IC50 1.8 ± 0.04 μM) Staphylococcus aureus IC50 0.24 ± 0.04 μM (chloramphenicol IC50 2.9 ± 0.5 μM) |
NIH 3T3 IC50 14.4 ± 2.6 μM (amoxifen citrate IC50 16.5 ± 0.2 μM) |
| JBIR-97/98 (46a) | marine sponge-derived fungus Tritirachium sp. Sp081112MEf2 and marine fungus Engyodontium album Strain LF069 |
Staphylococcus epidermidis IC50 0.20 ± 0.04 μM (chloramphenicol IC50 1.8 ± 0.04 μM) Staphylococcus aureus IC50 0.19 ± 0.02 μM (chloramphenicol IC50 2.9 ± 0.5 μM) |
NIH 3T3 IC50 14.0 ± 1.1 μM (amoxifen citrate IC50 16.5 ± 0.2 μM) |
| Engyodontochone A (46b) | marine fungus Engyodontium album Strain LF069 |
Staphylococcus epidermidis IC50 0.19 ± 0.04 μM (chloramphenicol IC50 1.8 ± 0.04 μM) Staphylococcus aureus IC50 0.17 ± 0.02 μM (chloramphenicol IC50 2.9 ± 0.5 μM) |
NIH 3T3 IC50 11.0 ± 1.6 μM (amoxifen citrate IC50 16.5 ± 0.2 μM) |
| Compound (8) | marine fungus Talaromyces islandicus EN-501 found in red alga Laurencia okamurai |
Escherichia coli MIC 32 μg/mL (chloramphenicol MIC 1 μg/mL) Pseudomonas aeruginosa MIC 32 μg/mL (chloramphenicol MIC 4 μg/mL) Staphylococcus aureus MIC > 64 μg/mL (chloramphenicol MIC 2 μg/mL) Vibrio alginolyticus MIC 32 μg/mL (chloramphenicol MIC 0.5 μg/mL) Vibrio harveyi MIC 32 μg/mL (chloramphenicol MIC 2 μg/mL) Vibrio parahaemolyticus MIC 32 μg/mL (chloramphenicol MIC 2 μg/mL) |
|
| Aspergixanthone A (20) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 1.80 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone B (21) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 >10.0 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone C (22) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 3.3 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 2.8 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 3.6 μM (cisplatin IC50 1.1 μM) HeLa IC50 2.9 μM (cisplatin IC50 0.82 μM) A-549 IC50 3.2 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone E (23) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 > 10.0 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone F (24) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 9.8 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 2.7 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 3.6 μM (cisplatin IC50 1.1 μM) HeLa IC50 1.7 μM (cisplatin IC50 0.82 μM) A-549 IC50 1.1 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone D (26) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus
Bacillus anthraci Salmonella typhi Enterobacter aerogenes |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 > 10.0 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone G (28) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus MIC 0.78 μg/mL Bacillus anthraci MIC 12.5 μg/mL Salmonella typhi MIC 6.13 μg/mL Enterobacter aerogenes MIC 6.13 μg/mL |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 > 10.0 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone H (29) | marine fungus Aspergillus sp. ZA-01 |
Micrococcus lysodeikticus MIC 6.13 μg/mL Bacillus anthraci MIC 12.5 μg/mL Salmonella typhi MIC 6.13 μg/mL Enterobacter aerogenes MIC 6.13 μg/mL |
MDA-MB-231 IC50 > 10.0 μM (cisplatin IC50 1.3 μM) MCF-7 IC50 > 10.0 μM (cisplatin IC50 0.97 μM) MGC-803 IC50 > 10.0 μM (cisplatin IC50 1.1 μM) HeLa IC50 > 10.0 μM (cisplatin IC50 0.82 μM) A-549 IC50 > 10.0 μM (cisplatin IC50 0.74 μM) |
| Aspergixanthone I (27) | marine fungus Aspergillus sp. ZA-01 |
Vibrio anguillarum MIC 1.56 µM (ciprofloxacin MIC 0.312 µM) Vibrio parahemolyticus MIC 1.56 µM (ciprofloxacin MIC 0.078 µM) Vibrio alginolyticus MIC 3.12 µM (ciprofloxacin MIC 0.625 µM) |
|
| Aspergixanthone J (30) | marine fungus Aspergillus sp. ZA-01 |
Vibrio anguillarum MIC 6.25 µM (ciprofloxacin MIC 0.312 µM) Vibrio parahemolyticus MIC 25 µM (ciprofloxacin MIC 0.078 µM) Vibrio alginolyticus MIC 25 µM (ciprofloxacin MIC 0.625 µM) |
|
| Aspergixanthone K (31) | marine fungus Aspergillus sp. ZA-01 |
Vibrio anguillarum MIC 3.12 µM (ciprofloxacin MIC 0.312 µM) Vibrio parahemolyticus MIC 25.0 µM (ciprofloxacin MIC 0.078 µM) Vibrio alginolyticus MIC 12.5 µM (ciprofloxacin MIC 0.625 µM) |
|
| Citreamicin θ A (32) | marine Streptomyces sp. |
Staphylococcus haemolyticus UST950701-004 MIC 0.5 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus UST950701-005 MIC 1.0 μg/mL (penicillin G MIC 0.25 μg/mL, streptomycin MIC 8.0 μg/mL) Bacillus subtillis 769 MIC 0.25 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus ATCC43300 MIC 0.25 μg/mL (penicillin G MIC > 50 μg/mL, streptomycin MIC > 50 μg/mL) |
HeLa IC50 0.055 μg/mL (cisplatin IC50 18.14 μg/mL) |
| Citreamicin θ B (33) | marine Streptomyces sp. |
Staphylococcus haemolyticus UST950701-004 MIC 0.5 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus UST950701-005 MIC 1.0 μg/mL (penicillin G MIC 0.25 μg/mL, streptomycin MIC 8.0 μg/mL) Bacillus subtillis 769 MIC 0.25 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus ATCC43300 MIC 0.25 μg/mL (penicillin G MIC > 50 μg/mL, streptomycin MIC > 50 μg/mL) |
HeLa IC50 0.072 μg/mL (cisplatin IC50 18.14 μg/mL) |
| Citreaglycon A (35) | marine Streptomyces sp. |
Staphylococcus haemolyticus UST950701-004 MIC 8.0 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus UST950701-005 MIC 16.0 μg/mL (penicillin G MIC 0.25 μg/mL, streptomycin MIC 8.0 μg/mL) Bacillus subtillis 769 MIC 8.0 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus ATCC43300 MIC 8.0 μg/mL (penicillin G MIC > 50 μg/mL, streptomycin MIC > 50 μg/mL) |
HeLa IC50 > 40 μg/mL (cisplatin IC50 18.14 μg/mL) |
| Dehydrocitreaglycon A (36) | marine Streptomyces sp. |
Staphylococcus haemolyticus UST950701-004 MIC 8.0 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus UST950701-005 MIC 16.0 μg/mL (penicillin G MIC 0.25 μg/mL, streptomycin MIC 8.0 μg/mL) Bacillus subtillis 769 MIC > 50 μg/mL (penicillin G MIC 0.13 μg/mL, streptomycin MIC 8.0 μg/mL) Staphylococcus aureus ATCC43300 MIC 0.25 μg/mL (penicillin G MIC > 50 μg/mL, streptomycin MIC > 50 μg/mL) |
HeLa IC50 > 40 μg/mL (cisplatin IC50 18.14 μg/mL) |
| Buanmycin (34) | marine Streptomyces sp. |
Staphylococcus aureus MIC 10.5 μΜ (ampicillin MIC 4.5 μΜ) Bacillus subtilis MIC 0.7 μM (ampicillin MIC 1.1 μΜ) Kocuria rhizophila MIC 10.5 μM (ampicillin MIC 0.6 μΜ) Salmonella enterica MIC 0.7 μM (ampicillin MIC 4.5 μΜ) Proteus hauseri MIC 21.1 μM (ampicillin MIC < 0.6 μΜ) |
A-549 IC50 1.7 μΜ (etoposide IC50 0.8 μΜ) HCT-116 IC50 0.9 μM (etoposide IC50 1.9 μΜ) SNU-638 IC50 0.8 μM (etoposide IC50 0.5 μΜ) K-562 IC50 > 100 μM (etoposide IC50 3.1 μΜ) SK-HEP1 IC50 1.9 μM (etoposide IC50 1.1 μΜ) MDA-MB-231 IC50 1.2 μM (etoposide IC50 10.6 μΜ) |
| Compound (7) | marine fungus Phomopsis sp. (No. SK7RN3G1) | Hep-2 IC50 8 μg/mL HepG2 IC50 9 μg/mL |
|
| Versixanthone A (39) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 2.6 μM (doxorubicin hydrochloride IC50 0.02 μM) K562 IC50 7.1 μM (doxorubicin hydrochloride IC50 0.3 μM) A549 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.2 μM) H1975 IC50 11.2 μM (doxorubicin hydrochloride IC50 0.8 μM) 803 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.2 μM) HO-8910 IC50 10.1 μM (doxorubicin hydrochloride IC50 0.5 μM) |
|
| Versixanthone B (40) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 9.9 μM (doxorubicin hydrochloride IC50 0.02 μM) A549 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.2 μM) H1975 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.8 μM) 803 IC50 21.6 μM (doxorubicin hydrochloride IC50 0.2 μM) HO-8910 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.5 μM) |
|
| Versixanthone C (41) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 7.8 μM (doxorubicin hydrochloride IC50 0.02 μM) K562 IC50 18.2 μM (doxorubicin hydrochloride IC50 0.3 μM) A549 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.2 μM) H1975 IC50 25.6 μM (doxorubicin hydrochloride IC50 0.8 μM) HO-8910 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.5 μM) HCT-116 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.2 μM) |
|
| Versixanthone D (42) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 3.3 μM (doxorubicin hydrochloride IC50 0.02 μM) K562 IC50 9.1 μM (doxorubicin hydrochloride IC50 0.3 μM) A549 IC50 12.7 μM (doxorubicin hydrochloride IC50 0.2 μM) H1975 IC50 > 50 μM (doxorubicin hydrochloride IC50 0.8 μM) 803 IC50 9.8 μM (doxorubicin hydrochloride IC50 0.2 μM) HO-8910 IC50 13.9 μM (doxorubicin hydrochloride IC50 0.5 μM) HCT-116 IC50 6.1 μM (doxorubicin hydrochloride IC50 0.2 μM) |
|
| Versixanthone E (43) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 1.6 μM (doxorubicin hydrochloride IC50 0.02 μM) K562 IC50 11.1 μM (doxorubicin hydrochloride IC50 0.3 μM) H1975 IC50 2.7 μM (doxorubicin hydrochloride IC50 0.8 μM) 803 IC50 2.2 μM (doxorubicin hydrochloride IC50 0.2 μM) HO-8910 IC50 2.0 μM (doxorubicin hydrochloride IC50 0.5 μM) |
|
| Versixanthone F (44) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 2.7 μM (doxorubicin hydrochloride IC50 0.02 μM) K562 IC50 6.7 μM (doxorubicin hydrochloride IC50 0.3 μM) A549 IC50 10.6 μM (doxorubicin hydrochloride IC50 0.2 μM) HO-8910 IC50 20.8 μM (doxorubicin hydrochloride IC50 0.5 μM) HCT-116 IC50 0.7 μM (doxorubicin hydrochloride IC50 0.2 μM) |
|
| Versixanthone G (47) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 13.4 μM K562 IC50 20.9 μM A549 IC50 17.8 μM H1975 IC50 9.8 μM MGC803 IC50 4.6 μM HEK293 IC50 > 50 μM HO-8910 IC50 9.6 μM HCT-116 IC50 16.2 μM |
|
| Versixanthone H (48) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 6.9 μM K562 IC50 22.1 μM A549 IC50 19.2 μM H1975 IC50 5.3 μM MGC803 IC50 6.2 μM HEK293 IC50 > 50 μM HO-8910 IC50 6.9 μM HCT-116 IC50 15.2 μM |
|
| Versixanthone I (49) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 27.8 μM K562 IC50 >50 μM A549 IC50 > 50 μM H1975 IC50 > 50 μM HEK293 IC50 > 50 μM HO-8910 IC50 > 50 μM HCT-116 IC50 > 50 μM |
|
| Versixanthone J (50) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 47.3 μM K562 IC50 > 50 μM A549 IC50 > 50 μM H1975 IC50 > 50 μM HEK293 IC50 > 50 μM HO-8910 IC50 > 50 μM HCT-116 IC50 > 50 μM |
|
| Versixanthone K (51) | fungus Aspergillus versicolor HDN1009 found in soil around a mangrove | HL-60 IC50 49.5 μM K562 IC50 > 50 μM A549 IC50 > 50 μM H1975 IC50 49.5 μM MGC803 IC50 > 50 μM HEK293 IC50 > 50 μM HO-8910 IC50 > 50 μM HCT-116 IC50 > 50 μM |
IC50 = The concentration causing 50% inhibition of cell survival; MIC = minimum inhibitory concentration; ACC-MESO-1 = human malignant pleural mesothelioma cell line; A-549, human lung cancer; BEL-7402 = human hepatocellular carcinoma cell line; C-A120 = doxorubicin-selected derivative ABCC1-overexpressing cell line; GLC-82 = human lung cancer cell line; H460 = human lung cancer cell line; H1975 = human lung cancer cell line; HCT-15, human colon cancer; HCT-116 = human colorectal carcinoma cell line; HEK-293 = human embryonic kidney cell line; HeLa = Human cervical cancer cell line; Hep-2 = Human Epidermoid carcinoma; HepG2 = Human liver cancer cell line; HL-60 = human leukemia cell line; HO-8910 = human ovarian cancer cell line; K562 = leukemia cell line; KB = human oral epidermoid carcinoma cell line; KB-3-1 = human epidermoid carcinoma cell line; KBv200 = vincristine-selected derivative ABCB1-overexpressing cell line; MCF-7 = Breast adenocarcinoma cell line; MCF-7/Adr = doxorubicin-selected derivative ABCB1-overexpressing cell line; MDA-MB-231 = human breast cancer cell line; MGC-803 = Gastric mucinous adenocarcinoma cell line; NIH-3T3 = mouse fibroblasts cell line; S1 = human colon carcinoma cell line; S1-M1-80 = mitoxantrone-selected derivative ABCG2-overexpressing cell line; SK-HEP1 = human liver cancer cell line; SK-MEL-2, human skin cancer; SK-OV-3, human ovarian cancer; SNU-638 = human gastric cancer cell line; XF- 498, human CNS cancer.