Table 2.
Pharmacological activity of lichen tridepsides.
| Tridepside | Botanical Origin | Type of Study | Experimental Model | Activities | Results | References |
|---|---|---|---|---|---|---|
| Gyrophoric acid | Umbilicaria antarctica Frey and I. M. Lamb. | In vitro | PTP1B enzyme activity and kinetic analysis | Antidiabetic Antiobesity |
Inhibition PTP1B activity IC50: 3.6 μM in a non-competitive manner. | [99] |
| Parmelia saxatilis (L.) Ach. | In vitro In silico |
Angiotensin II type-1 receptor (AT1) interaction | Antihypertensive | AT1 antagonist. Calcium influx assay (IC50 29.76 μM). |
[123] | |
| Acarospora fuscata (Nyl.) Th.Fr. | In vitro | Gram-positive bacteria: Bacillus mycoides, Bacillus subtilis Staphylococcus aureus. Gram-negative bacteria: Escherichia coli, Klebsiella pneumoniae. Fungi: Aspergillus flavus, Aspergillus fumigatus, Candida albicans, Penicillium purpurescens and Penicillium verrucosum. |
Antimicrobial | Minimum inhibitory concentration values ranging from 0.019 to 1.25 mg/mL. | [117] | |
| Xanthoparmelia pokornyi (Körb.) O.Blanco, A.Crespo, Elix, D.Hawksw. and Lumbsch | In vitro | Gram-positive bacteria: Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Staphylococcus aureus. Streptococcus faecalis. Gram-negative bacteria: Aeromonas hydrophila, Proteus vulgaris, Yersinia enterocolitica. Fungi: Candida albicans and Candida glabrata. |
Antimicrobial | Active against some bacteria and fungi (A. hydrophila, B. cereus, B. subtilis, L. monocytogenes, P. vulgaris, S. aureus, S. faecalis, Y. enterocolitica, C. albicans and C. glabrata) | [118] | |
| Gyrophoric acid | Acarospora fuscata (Nyl.) Th.Fr. | In vitro | DPPH Superoxide anion radical-scavenging reducing power |
Antioxidant | DPPH (IC50 105.75 µg/mL). Superoxide anion radical (IC50 196.62 µg/mL). Reducing power (1.32 at 1000 µg/mL, 1.12 at 500 µg/mL, 0.71 at 250 µg/mL, 0.39 at 125 µg/mL, and 0.20 at 62.5 µg/mL). |
[117] |
|
Parmelia nepalensis Tayl. Parmelia
tinctorum Nyl. |
In vitro | HaCaT (human keratinocyte cell line) | Antiproliferative | Antiproliferative activity (IC50 value of 1.7 µM). Cytostatic mechanism. |
[76] | |
| Umbilicaria hirsuta (Sw. ex Westr.) Hoffm | In vitro | A2780 (human ovarian carcinoma) HCT-116 p53+/+ and HCT-116 p53−/− (human colon carcinoma) HeLa (human cervix adenocarcinoma) SK-BR-3 (human breast adenocarcinoma) HL-60 (human promyelocytic leukemia) HT-29 (human colon adenocarcinoma) Jurkat (Human T cells lymphocyte leukemia) MCF-7 (Human breast adenocarcinoma) |
Cytotoxic | Effective against A2780, HL-60, and Jurkat cells. Clonogenic ability inhibition of SK-BR-3 cells. A2780 cells accumulation in S-phase at expense of G1/G0-phase. |
[55] | |
| Gyrophoric acid | Umbilicaria hirsuta (Sw. ex Westr.) Hoffm | In vitro | HeLa (human cervix carcinoma) | Cytotoxic | Oxidative stress pathway: ↑ ROS level, DNA oxidation and activity changes of stress/survival proteins as p38MAPK, Erk1/2 and Akt. Apoptosis pathway: ↑ caspase-3 activation, PARP cleavage, PS externalization, and cell cycle changes. |
[17] |
| Acarospora fuscata (Nyl.) Th.Fr. | In vitro | A549 (human lung carcinoma cell line), Fem-x (malignant melanoma cell line), K562 (chronic myelogeneous leukemia cell line) LS174 (human colon carcinoma cell line) |
Cytotoxic | Weak activity against A549 and LS174 (IC50 151.51 and 151.65 µg/mL). Moderate cytotoxic effect against Fem-x and K562 cells (IC50 64.01 and 78.45 µg/mL). Apoptosis of sub-G1 phase in malignant cells. Reduction percentage of cells in G0/G1 and S-G2/Mphases of the cell cycle. |
[117] | |
| Ochrolechia deceptionis Hue. | In vitro | A375 (melanoma cancer cell line) | Cytotoxic | Low activity. | [58] | |
| - | In vitro | Primary cultures of rat hepatocytes | Cytotoxic | Inactive. | [119] | |
| Umbilicaria hirsuta (Sw. ex Westr.) Hoffm | In vitro | Calf thymus DNA | DNA-interacting agents | Topoisomerase I inhibition (25 μM). | [61] | |
| - | In vitro | Second and third instar larvae of the mosquito Culiseta longiareolata | Larvicidal activity | LC (50) values: 0.41 ppm, LC (90) values: 1.93 ppm. | [39] | |
| Xanthoparmelia pokornyi (Körb.) O.Blanco, A.Crespo, Elix, D.Hawksw. and Lumbsch | In vitro | HaCaT (human keratinocyte cell line) | Photoprotective | Prevention of cytotoxic, apoptotic, and cytoskeleton alterative effects of 2.5 J/cm2 UVB. | [121] | |
| Gyrophoric acid | Lasallia pustulata (L.) Méra | In vitro | DPPH assay NBT assay Human keratinocytes HaCaT cell line |
Photoprotective | DPPH (IC50 25 µg/mL) Good PF-UVA candidate (SPF > 5). |
[120] |
| - | In vitro | (UVA)-treated dermal fibroblasts | Photoprotective | Anti-aging effects. Upregulated mRNA levels of COL1A1/COL3A1/SOD2 genes and type I collagen protein levels. ↓MMP1 mRNA and protein expression levels. |
[122] | |
| Lasallia pustulata (L.) Méra | In vitro | MM98 (Malignant mesothelioma cell line) A431 (vulvar carcinoma cell line) HaCaT (human keratinocyte cell line) |
Wound healing | Strong wound closure effects. Better results combined with (+)-usnic acid. |
[89] | |
| Tenuiorin acid | Peltigera leucophlebia (Nyl.) Gyeln. | In vitro | Calcium-stimulated porcine leucocytes. T-47D (human cancer breast cell line) WIDR (human cancer colon cell line) PANC-1 (human cancer pancreas cell line) |
Antiproliferative | Moderate 5-lipoxygenase inhibition (IC50 values of 41.6 μM). Moderate/weak antiproliferative effects on PANC-1 and WIDR cells (ED50 87.9 and 95.9 μM, respectively) and weak activity against T-47D cells (ED50 152.6 μM). |
[22] |
| Umbilicaria antarctica Frey and I. M. Lamb. | In vitro In silico |
ThT fluorescence assay Docking studies |
Neuroprotective | Tau inhibitor (IC50 100 µM). | [124] | |
| Trivaric acid | - | In silico | Docking and ITC studies | Antidiabetic | PTP1b inhibition by blocking its active site. | [126] |
| - | In vitro | PTP1b inhibition assay Human liver HepG2 cancer cell line |
Antidiabetic | ↑ PTP1B inhibitory activity. IR/IRS/Akt/GLUT2 pathway stimulation. ↑ Glucose consumption |
[125] | |
| Trivaric acid | - | In vivo | Diabetic mice model | Antidiabetic | ↓ insulin resistance ↓ leptin resistance. Improve lipid profile and weight control. |
[125] |
| - | In vitro | Human leukocyte elastase assay | Anti-inflammatory | Potent human leukocyte elastase inhibitory activity (IC50 of 1.8 µM). | [127] |