Table 4.
Chemical compounds isolated from different parts of Aster flaccidus and their biological activities.
S. No | Compounds | Parts used | Dose | Bioactivity | Mechanism | Models | IC50/ID50/p-values |
---|---|---|---|---|---|---|---|
1 | 2-O-β-d-glucopyranoside-vicodiol | Aerial [58] | |||||
2 | 10-O-β-d-glucopyranoside-oplopanone | ||||||
3 | α-spinasterol | 5–100 μg/mL | Anticholinesterase activity [62] | Inhibited the acetylcholinesterase enzyme (obtained from brain homogenate) activity | NA | IC50 value, 44.19 ± 2.59 μg/mL | |
3–100 μM | Anti-inflammatory [60] | Suppressed the LPS-induced expression of COX-1 and COX-2 activities expressed in prostaglandin levels (in ng/mL) | Male Swiss mice | IC50 value, 16.17 μM (COX-1 inhibition) and 7.8 μM (COX-2 inhibition) | |||
40 μM | Anti-inflammatory [68] | Significantly suppressed the production of NO, PGE2, TNF, and IL-1β by LPS-stimulated cells through ERK pathway-dependent expression of HO-1 | BV2 microglial cells and mouse hippocampal HT22 cells | *P < 0.05. | |||
0.24 μM/kg | Antihyperalgesic activity [66] | Inhibited carrageenan-induced hyperalgesia in mice | Female Swiss mice | 42 ± 6 % inhibition | |||
0.3 μM/kg | Antioedematogenic effect [65] | Inhibited edema produced in capsaicin-induced nociceptive | Male albino Swiss mice | 66 ± 10 % inhibition; ID50 value, 0.11 μM/kg | |||
26.93 μg/mL (for DPPH assay); 35.16 μg/mL (for ABTS assay) | Antioxidant [62] | Scavenged DPPH- and ABTS-free radicals | NA | 26.93 ± 0.0 % and 35.16 ± 0.26 % | |||
0.3 μM/kg | Antinociceptive [65] | Inhibited nociception in capsaicin-induced nociceptive mice model | Male albino Swiss mice | 58 ± 4 % inhibition | |||
0.3 mg/kg | Antinociceptive [66] | Inhibited reserpine-induced mechanical allodynia in mice | Male Swiss mice | 73 % inhibition | |||
0.001–10 mg/kg | Antinociceptive [67] | Inhibited acetic acid-induced abdominal constriction | Male Swiss mice | IC50, 99 ± 1 % and ID50 value, 0.07 (0.05–0.09 mg/kg) | |||
50 mg/kg | Anti-ulcer [66] | Reduced the percentage of ulcer | Female Swiss mice | 71 % | |||
5 mg/kg | Antitumour [69] | Reduced testosterone propionate-induced benign prostatic hyperplasia in rats | Wistar-Unilever rats | P < 0.05 | |||
15.0 μg/0.2 mL acetone | Antitumour [70] | Reduced the number and incidence of croton oil-induced mouse skin tumours | Swiss Webster albino mice | Reduced incidence of skin tumours by 55.6 % and tumour numbers by 65.0 %. | |||
10–80 nM/mL | Anti-proliferative [71] | Inhibited cell proliferation | Human colorectal adenocarcinoma CACO-2 cells | 60.0 ± 7.10 nM/mL | |||
12.5–100.0 μg/mL | Anti-proliferative [72] | Inhibited cell proliferation | HeLa and RAW 264.7 cells | IC50 values, 77.1 ± 2.1 μg/mL (HeLa cells); 69.2 ± 6 μg/mL (RAW 264.7 cells) | |||
5–100 μg/mL | Anti-diabetic [62] | Inhibited α-glucosidase enzyme activity | NA | IC50 value, 8.65 ± 1.71 μg/mL | |||
2 mg/kg | Anti-diabetic [73] | Reduced blood sugar level in hyperglycaemic rats | Male Wistar strain rats | 22.01 % reduction | |||
2.5–10 μM | Anti-diabetic [64] | Increased glucose uptake by mouse skeletal muscle cells | Mouse myoblast C2C12 cells | P < 0.01 | |||
Enhanced the secretion of insulin in pancreatic β-cells in response to high glucose | Rat insulinoma INS-1 cells | ||||||
4 | α-spinasterol-β-d-glucopyranoside tetraacetate | NA | NA | NA | NA | NA | |
5 | lariciresinol 9-O-β-d-glucopyranoside | NA | Anti-cancer [74] | Cytotoxic against human breast cancer cell lines | Human breast cancer cell lines (Bt549, MCF7, MDA-MB-231 and HCC70) | IC50 value, 24.81 μM | |
6 | alaschanioside A | NA | NA | NA | NA | ||
7 | alangilignoside D | NA | NA | NA | NA | NA | |
8 | syringaresinol | 25–100 μM | Anti-inflammatory [61] | Inhibited protein and mRNA expressions of LPS-stimulated iNOS, COX-2, NF-κB, NO, and PGE2, TNF, IL-1β, and IL-6 production | RAW264.7 cells | P < 0.01–0.05 | |
50 mg/kg | Anti-inflammatory [61] | Reduced carrageenin-induced paw edema volume (mL) | ICR mice | P < 0.01 | |||
50 mg/kg | Reduced carrageenin-induced paw edema volume (mL) | ICR mice | P < 0.01 | ||||
100 μM | Cytotoxicity [75] | Cytotoxic | Hepatoblastoma cells (HepG2) and human colorectal adenocarcinoma (HT29) cells | Non-significant | |||
NA | Anti-diabetic [63] | Inhibited α-glucosidase enzyme activity | NA | IC50 value, 19.5 ± 0.2 μg/mL | |||
20 μM | Antiphotoaging [76] | Inhibited UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling and enhanced collagen production | UVA-irradiated human HaCaT keratinocytes and dermal fibroblasts (HDFs) | Reduced the level of MMP-1 (induced by UVA) from 8.16 ng/mL to 2.56 ng/mL and from 2.28 ng/mL to 1.37 ng/mL in HaCaT keratinocytes and HDFs, respectively. | |||
9 | 2,6-dimethoxy-4-(2-propenyl)-phenyl-β-D-glucoside | NA | NA | NA | NA | NA | |
10 | (7′R, 8S)-9′-lariciresinol-(α-methyl)-butanoate | Roots [15] | NA | NA | NA | NA | NA |
11 | 5,9-dimethoxyl-7-(α-methyl)-butanoxyl-phenyl-2E-propenol-(α-methyl)-butanoate | NA | Anti-tumour [15] | Exhibited anti-cancer activity against human liver carcinoma cells | Human liver carcinoma, BEL 7402 cells | IC50 values, 106.67 ± 8.47 μM at 24 h, 50.51 ± 6.11 μM at 72 h |
In the “dose” column, “mg/kg, μM/kg” represents the oral/parenteral dose of the compound in mice/rats; concentration units (μg/mL, nM/mL) represent the concentration of the compound in the cell treatment. ABTS - 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid; COX – cyclooxygenase; DPPH – 2,2-diphenyl-1-picrylhydrazyl; ERK – extracellular signal-regulated kinase; HaCaT – cultured human keratinocyte (cells); HeLa – Lack's cervical cancer cells; HO-1 – heme oxygenase-1; IC50 – the half-maximal inhibitory concentration; ID50 – infectious dose 50; ICR – institute of cancer research; IL – interleukins; iNOS – inducible nitric oxide synthase; LPS – lipopolysaccharide; MMP-1 – matrix metalloproteinases; MAPK/AP-1 – mitogen-activated protein kinases (MAPK)/activator protein-1 (AP-1); mRNA – messenger ribonucleic acid; NA – not available/not tested; NF-κB – nuclear factor kappa B; NO – nitric oxide; PGE2 – prostaglandins E2; RAW 264.7 – macrophage-like, Abelson leukemia virus-transformed cell line derived from Balb/c mice; TNF – tumour necrosis factor.