Table 2.
Biological activities of chaetomugilins and chaetoviridines.
| Compound Name | Biological Activity | Assay, Organism, or Cell Line | Biological Results | Positive Control | Refs. |
|---|---|---|---|---|---|
| Chaetomugilin 106B-6 XXVIII (1) | Cytotoxicity | MTT/P388 | 32.0 µM (IC50) | 5-FU 1.7 µM (IC50) | [37,58] |
| MTT/HL-60 | 51.8 µM (IC50) | 5-FU 2.7 µM (IC50) | [37,58] | ||
| MTT/L1210 | 67.1 µM (IC50) | 5-FU 1.1 µM (IC50) | [37,58] | ||
| MTT/KB | 58.8 µM (IC50) | 5-FU 7.7 µM (IC50) | [37,58] | ||
| Chaetomugilin A (2) | Cytotoxicity | MTT/P388 | 8.7 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 7.3 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| MTT/HL-60 | 6.4 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] | ||
| MTT/K562 | 11.1 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/BEL-7402 | 17.9 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/HCT-116 | 6.1 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HeLa | 20.3 µM (IC50) | Adriamycin 0.6 µM (IC50) | [22] | ||
| SRB/L-02 | 15.2 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/MGC-803 | 15.3 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HO8910 | 12.1 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/SH-SY5Y | 23.4 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/NCI-H1975 | 18.3 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/U87 | 27.1 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] | ||
| SRB/MDA-MB-231 | 22.7 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| 11-Epi-chaetomugilin A (4) | Cytotoxicity | MTT/P388 | 88.9 µM (IC50) | 5-FU 1.7 µM (IC50) | [35] |
| MTT/HL-60 | 66.7 µM (IC50) | 5-FU 2.7 µM (IC50) | [35] | ||
| MTT/P388 | 88.9 µM (IC50) | 5-FU 1.7 µM (IC50) | [37,58] | ||
| MTT/HL-60 | 66.7 µM (IC50) | 5-FU 2.7 µM (IC50) | [37,58] | ||
| MTT/L1210 | 80.2 µM (IC50) | 5-FU 1.1 µM (IC50) | [37,58] | ||
| Chaetomugilin B (6) | Cytotoxicity | MTT/P388 | 18.7 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 16.5 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| Chaetomugilin C (7) | Cytotoxicity | MTT/P388 | 3.6 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 2.7 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| MTT/HL-60 | 6.6 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] | ||
| MTT/K562 | 12.3 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/BEL-7402 | 16.8 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/HCT-116 | 5.7 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HeLa | 13.2 µM (IC50) | Adriamycin 0.6 µM (IC50) | [22] | ||
| SRB/L-02 | 9.1 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/MGC-803 | 9.6 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HO8910 | 8.8 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/SH-SY5Y | 19.4 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/NCI-H1975 | 12.1 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/U87 | 17.6 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] | ||
| SRB/MDA-MB-231 | 26.6 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| Chaetomugilin D (8) | Cytotoxicity | MTT/P388 | 7.5 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 6.8 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| Phytotoxic activity | Lettuce seed germination bioassay/Root growth inhibition | 24.2 ppm (IC50) | - | [51] | |
| Lettuce seed germination bioassay/Shoot growth inhibition | 27.8 ppm (IC50) | - | [51] | ||
| Antimicrobial | Microplate assay/Vibrio vulnificus | 32.4 µg/mL (MIC) | Erythromycin 2.0 µg/mL (MIC) | [25] | |
| Microplate assay/Vibrio rotiferianus | 15.3 µg/mL (MIC) | Erythromycin 3.9 µg/mL (MIC) | [25] | ||
| Microplate assay/MRSA 1 | 32.2 µg/mL (MIC) | Chloramphenicol 7.6 µg/mL (MIC) | [25] | ||
| Microplate assay/MRSA 2 | 32.4 µg/mL (MIC) | Chloramphenicol 7.5 µg/mL (MIC) | [25] | ||
| Seco-chaetomugilin D (9) | Cytotoxicity | MTT/P388 | 38.6 µM (IC50) | 5-FU 1.7 µM (IC50) | [48] |
| MTT/HL-60 | 47.2 µM (IC50) | 5-FU 2.7 µM (IC50) | [48] | ||
| MTT/L1210 | 53.6 µM (IC50) | 5-FU 3.0 µM (IC50) | [48] | ||
| MTT/KB | 47.2 µM (IC50) | 5-FU 6.0 µM (IC50) | [48] | ||
| Chaetomugilin E (11) | Cytotoxicity | MTT/P388 | 15.7 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 13.2 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| Inhibition TNF-α | TNF-α activated NF-kB assay | 11.6 µM (IC50) | TPCK 3.8 µM (IC50) BAY-11 2.0 µM (IC50) |
[56] | |
| Inhibition NO | Nitrite assay | 5.8 µM (IC50) | L-NMMA 25.1 µM (IC50) | [56] | |
| Chaetomugilin F (13) | Cytotoxicity | MTT/P388 | 3.3 µM (IC50) | 5-FU 1.7 µM (IC50) | [38,40] |
| MTT/HL-60 | 1.3 µM (IC50) | 5-FU 2.7 µM (IC50) | [38,40] | ||
| Inhibition TNF-α | TNF-α activated NF-kB assay | 5.1 µM (IC50) | TPCK 3.8 µM (IC50) BAY-11, 2.0 µM (IC50) |
[56] | |
| Inhibition NO | Nitrite assay | 1.9 µM (IC50) | L-NMMA 25.1 µM (IC50) | [56] | |
| Chaetomugilin G (14) | Cytotoxicity | MTT/P388 | 24.1 µM (IC50) | 5-FU 1.7 µM (IC50) | [38] |
| MTT/HL-60 | 19.8 µM (IC50) | 5-FU 2.7 µM (IC50) | [38] | ||
| MTT/P388 | 24.1 µM (IC50) | 5-FU 1.7 µM (IC50) | [41] | ||
| MTT/HL-60 | 19.8 µM (IC50) | 5-FU 2.7 µM (IC50) | [41] | ||
| MTT/L1210 | 123.6 µM (IC50) | 5-FU 3.0 µM (IC50) | [41] | ||
| MTT/KB | 137.8 µM (IC50) | 5-FU 6.0 µM (IC50) | [41] | ||
| Chaetomugilin H (15) | Cytotoxicity | MTT/P388 | 12.3 µM (IC50) | 5-FU 1.7 µM (IC50) | [38] |
| MTT/HL-60 | 10.3 µM (IC50) | 5-FU 2.7 µM (IC50) | [38] | ||
| MTT/P388 | 12.3 µM (IC50) | 5-FU 1.7 µM (IC50) | [41] | ||
| MTT/HL-60 | 10.3 µM (IC50) | 5-FU 2.7 µM (IC50) | [41] | ||
| MTT/L1210 | 93.3 µM (IC50) | 5-FU 3.0 µM (IC50) | [41] | ||
| MTT/KB | 18.8 µM (IC50) | 5-FU 6.0 µM (IC50) | [41] | ||
| Chaetomugilin I (16) | Cytotoxicity | MTT/P388 | 1.1 µM (IC50) | 5-FU 1.7 µM (IC50) | [37,58,59] |
| MTT/HL-60 | 1.1 µM (IC50) | 5-FU 2.7 µM (IC50) | [37,58,59] | ||
| MTT/L1210 | 1.9 µM (IC50) | 5-FU 1.1 µM (IC50) | [37,58,59] | ||
| MTT/KB | 2.3 µM (IC50) | 5-FU 7.7 µM (IC50) | [37,58,59] | ||
| Inhibition TNF-α | TNF-α activated NF-kB assay | 0.9 µM (IC50) | TPCK 3.8 µM (IC50) BAY-11 2.0 µM (IC50) |
[56] | |
| Inhibition NO | Nitrite assay | 0.3 µM (IC50) | L-NMMA 25.1 µM (IC50) | [56] | |
| 11-Epi-chaetomugilin I (17) | Cytotoxicity | MTT/P388 | 0.7 µM (IC50) | 5-FU 1.7 µM (IC50) | [59] |
| MTT/HL-60 | 1.0 µM (IC50) | 5-FU 2.7 µM (IC50) | [59] | ||
| MTT/L1210 | 1.6 µM (IC50) | 5-FU 1.1 µM (IC50) | [59] | ||
| MTT/KB | 1.2 µM (IC50) | 5-FU 7.7 µM (IC50) | [59] | ||
| Inhibition TNF-α | TNF-α activated NF-kB assay | 0.9 µM (IC50) | TPCK 3.8 µM (IC50) BAY-11 2.0 µM (IC50) |
[56] | |
| Inhibition NO | Nitrite assay | 0.8 µM (IC50) | L-NMMA 25.1 µM (IC50) | [56] | |
| Chaetomugilin J (18) | Phytotoxic activity | Lettuce seed germination bioassay/Root growth inhibition | 22.6 ppm (IC50) | - | [51] |
| Lettuce seed germination bioassay/Shoot growth inhibition | 21.9 ppm (IC50) | - | [51] | ||
| Cytotoxicity | MTT/P388 | 12.6 µM (IC50) | 5-FU 1.7 µM (IC50) | [37,58] | |
| MTT/HL-60 | 12.6 µM (IC50) | 5-FU 2.7 µM (IC50) | [37,58] | ||
| MTT/L1210 | 2.8 µM (IC50) | 5-FU 1.1 µM (IC50) | [37,58] | ||
| MTT/KB | 8.5 µM (IC50) | 5-FU 7.7 µM (IC50) | [37,58] | ||
| Inhibition TNF-α | TNF-α activated NF-kB assay | 7.6 µM (IC50) | TPCK 3.8 µM (IC50) BAY-11 2.0 µM (IC50) |
[56] | |
| Inhibition NO | Nitrite assay | 4.2 µM (IC50) | L-NMMA 25.1 µM (IC50) | [56] | |
| Chaetomugilin K (19) | Cytotoxicity | MTT/P388 | 8.2 µM (IC50) | 5-FU 1.7 µM (IC50) | [58] |
| MTT/HL-60 | 14.1 µM (IC50) | 5-FU 2.7 µM (IC50) | [58] | ||
| MTT/L1210 | 11.2 µM (IC50) | 5-FU 1.1 µM (IC50) | [58] | ||
| MTT/KB | 18.7 µM (IC50) | 5-FU 7.7 µM (IC50) | [58] | ||
| Chaetomugilin L (20) | Cytotoxicity | MTT/P388 | 10.9 µM (IC50) | 5-FU 1.7 µM (IC50) | [58] |
| MTT/HL-60 | 13.1 µM (IC50) | 5-FU 2.7 µM (IC50) | [58] | ||
| MTT/L1210 | 15.6 µM (IC50) | 5-FU 1.1 µM (IC50) | [58] | ||
| MTT/KB | 20.1 µM (IC50) | 5-FU 7.7 µM (IC50) | [58] | ||
| Chaetomugilin N (22) | Cytotoxicity | MTT/P388 | 2.3 µM (IC50) | 5-FU 1.7 µM (IC50) | [58] |
| MTT/HL-60 | 2.3 µM (IC50) | 5-FU 2.7 µM (IC50) | [58] | ||
| MTT/L1210 | 10.6 µM (IC50) | 5-FU 1.1 µM (IC50) | [58] | ||
| MTT/KB | 10.6 µM (IC50) | 5-FU 7.7 µM (IC50) | [58] | ||
| Chaetomugilin O (23) | Cytotoxicity | MTT/P388 | 11.1 µM (IC50) | 5-FU 1.7 µM (IC50) | [58] |
| MTT/HL-60 | 11.1 µM (IC50) | 5-FU 2.7 µM (IC50) | [58] | ||
| MTT/L1210 | 10.1 µM (IC50) | 5-FU 1.1 µM (IC50) | [58] | ||
| MTT/KB | 7.2 µM (IC50) | 5-FU 7.7 µM (IC50) | [58] | ||
| Chaetomugilin P (24) | Cytotoxicity | MTT/P388 | 0.7 µM (IC50) | 5-FU 1.7 µM (IC50) | [59] |
| MTT/HL-60 | 1.2 µM (IC50) | 5-FU 2.7 µM (IC50) | [59] | ||
| MTT/L1210 | 1.5 µM (IC50) | 5-FU 1.1 µM (IC50) | [59] | ||
| MTT/KB | 1.8 µM (IC50) | 5-FU 7.7 µM (IC50) | [59] | ||
| Chaetomugilin Q (25) | Cytotoxicity | MTT/P388 | 49.5 µM (IC50) | 5-FU 1.7 µM (IC50) | [59] |
| MTT/HL-60 | 47.2 µM (IC50) | 5-FU 2.7 µM (IC50) | [59] | ||
| MTT/L1210 | 80.2 µM (IC50) | 5-FU 1.1 µM (IC50) | [59] | ||
| Chaetomugilin R (26) | Cytotoxicity | MTT/P388 | 32.0 µM (IC50) | 5-FU 1.7 µM (IC50) | [59] |
| MTT/HL-60 | 51.8 µM (IC50) | 5-FU 2.7 µM (IC50) | [59] | ||
| MTT/L1210 | 67.1 µM (IC50) | 5-FU 1.1 µM (IC50) | [59] | ||
| MTT/KB | 67.1 µM (IC50) | 5-FU 7.7 µM (IC50) | [59] | ||
| Chaetomugilin S (27) | Caspase-3 inhibitory | Caspase-3 enzymatic assay | 20.6 µM (IC50) | Ac-DEVD-CHO 13.7 nM (IC50) | [31] |
| Chaetomugilin T (29) | Cytotoxicity | MTT/P388 | 62.4 µM (IC50) | 5-FU 1.9 µM (IC50) | [43] |
| MTT/HL-60 | 67.2 µM (IC50) | 5-FU 2.3 µM (IC50) | [43] | ||
| Chaetomugilin U (30) | Cytotoxicity | MTT/P388 | 57.4 µM (IC50) | 5-FU 1.9 µM (IC50) | [43] |
| MTT/HL-60 | 57.4 µM (IC50) | 5-FU 2.3 µM (IC50) | [43] | ||
| MTT/L1210 | 94.8 µM (IC50) | 5-FU 2.2 µM (IC50) | [43] | ||
| Chaetoviridin A (31) | Antifungal | Alternaria mali | 33.3 µg/mL (MIC) | - | [61] |
| Botrytis cinerea | 33.3 µg/mL (MIC) | - | [61] | ||
| Colletotrichum gloeosporioides | 33.3 µg/mL (MIC) | - | [61] | ||
| Fusarium oxysporum | 33.3 µg/mL (MIC) | - | [61] | ||
| Phytophthora capsici | 33.3 µg/mL (MIC) | - | [61] | ||
| Phytophthora infestans | 33.3 µg/mL (MIC) | - | [61] | ||
| Pythium ultimum | 1.23 µg/mL (MIC) | - | [61] | ||
| Magnaporthe grisea | 1.23 µg/mL (MIC) | - | [61] | ||
| Sclerotinia sclerotiorum | 97.5 (% inhibition) | - | [73] | ||
| Botrytis cinerea | 69.1 (% inhibition) | - | [73] | ||
| Fusarium graminearum | 77.0 (% inhibition) | - | [73] | ||
| Phytophthora capsici | 60.7 (% inhibition) | - | [73] | ||
| Fusarium moniliforme | 59.2 (% inhibition) | - | [73] | ||
| 5′-Epi-chaetoviridin A (33) | Cytotoxicity | SRB assay/HepG-2 | 35.3 µM (IC50) | Camptothecin 32.3 µM (IC50) | [72] |
| 7,5′- Bis-epi-chaetoviridin A (34) |
Caspase-3 inhibitory | Caspase-3 enzymatic assay | 10.9 µM (IC50) | Ac-DEVD-CHO 13.7 nM (IC50) | [31] |
| N-glutarylchaetoviridin A (35) | Cytotoxicity | MTT/HL-60 | 10.3 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] |
| MTT/K562 | 20.3 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/BEL-7402 | 23.9 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| Chaetoviridin B (37) | Antifungal | Pythium ultimum | 33.3 µg/mL (MIC) | - | [61] |
| Magnaporthe grisea | 33.3 µg/mL (MIC) | - | [61] | ||
| Chaetoviridin B (38) | α-Glucosidase inhibiory | Spectrophotometric assay | 6.328 µM (IC50) | Acarbose 54.74 µM (IC50) | [47] |
| N-Glutarylchaetoviridin C (42) | Cytotoxicity | MTT/HL-60 | 11.1 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] |
| MTT/K562 | 11.7 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/BEL-7402 | 10.9 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/HCT-116 | 11.3 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HeLa | 22.1 µM (IC50) | Adriamycin 0.6 µM (IC50) | [22] | ||
| SRB/L-02 | 18.2 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/MGC-803 | 6.6 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| SRB/HO8910 | 9.7 µM (IC50) | Adriamycin 0.4 µM (IC50) | [22] | ||
| SRB/NCI-H1975 | 11.2 µM (IC50) | Adriamycin 0.3 µM (IC50) | [22] | ||
| SRB/U87 | 18.3 µM (IC50) | Adriamycin 0.1 µM (IC50) | [22] | ||
| SRB/MDA-MB-231 | 13.2 µM (IC50) | Adriamycin 0.2 µM (IC50) | [22] | ||
| Chaetoviridin E (44) | Cytotoxicity | SRB assay/BC1 | 5.6 µg/mL (IC50) | Ellipticine 0.26 µg/mL (IC50) | [60] |
| Cytotoxicity | SRB assay/NCl-H187 | 3.5 µg/mL (IC50) | Ellipticine 0.32 µg/mL (IC50) | [60] | |
| Cytotoxicity | SRB assay/HepG-2 | 40.6 µM (IC50) | Camptothecin 32.3 µM (IC50) | [72] | |
| Antimalarial |
Microculture radioisotope assay/P. falciparum (K1, MDR) | 2.9 µg/mL (IC50) | - | [60] | |
| 7-Epi-chaetoviridin E (45) | Caspase-3 inhibitory | Caspase-3 enzymatic assay | 7.9 µM (IC50) | Ac-DEVD-CHO 13.7 nM (IC50) | [31] |
| Chaetoviridin F (47) | Cytotoxicity | SRB assay/NCl-H187 | 4.5 µg/mL (IC50) | Ellipticine 0.32 µg/mL (IC50) | [60] |
| Cytotoxicity | MTT/P388 | 46.0 µM (IC50) | 5-FU 1.9 µM (IC50) | [43] | |
| MTT/HL-60 | 39.1 µM (IC50) | 5-FU 2.3 µM (IC50) | [43] | ||
| MTT/L1210 | 43.7 µM (IC50) | 5-FU 2.2 µM (IC50) | [43] | ||
| MTT/KB | 34.5 µM (IC50) | 5-FU 20.6 µM (IC50) | [43] |