Volume 75, Issue 5-6

Potentilla anserina L. is not only a medicinal plant, but also a traditional cuisine. Hence, an acute toxicity study was performed to confirm its safety profile. Forty Kunming mice were randomly divided into two groups: control group and P. anserina L. extract group. Using the maximum dosage method, the P. anserina L. extract group was given the maximum dose within 12 h, equivalent to 345.6 g/kg crude drug. The control group was given distilled water. After administration, toxicity symptoms of mice were observed, body weight and food intake were recorded. After 14 days, blood was collected to measure biochemical parameters, autopsy was carried out to observe the changes of organs, and the vital organs were separated, weighed, and preserved for histopathological examination. The results showed that P. anserina L. extract group had no toxic symptoms. The activity, weight, and diet of mice were normal, and no abnormality was found in organ index, renal function, liver function, anatomical observation, and histopathological examination. Therefore, the maximum oral dosage (345.6 g/kg) of P. anserina L. was good safety. This study indicated that P. anserina L. had a large safety range and the clinical application was safe.

This study aimed to evaluate the selective cytotoxicity of six natural compounds on four cancerous cells (MCF-7, HeLa, Caco-2 and A549) and two normal intestinal and lung cells (Hs1.Int and Wl-38) cells. We also attempted to analyze basically the structure–activity relationships and to understand the mechanism of action of active compounds using the Caspase-Glo ® 3/7 kit. Globimetulin B ( 2 ) isolated from Globimetula dinklagei was significantly cytotoxic on cancerous cells with 50% inhibitory concentrations (IC 50 ) ranging from 12.75 to 37.65 μM and the selectivity index (SI) values varying between 1.13 and 3.48 against both normal cells. The compound 3-O-β- d -glucopyranosyl-28-hydroxy-α-amyrin ( 5 ) isolated from Phragmanthera capitata exhibited the highest cytotoxic activity on HeLa cells with the IC 50 of 6.88 μM and the SI of 5.20 and 8.71 against Hs1.Int and Wl-38 cells, respectively. A hydroxyl group at C-3 of compounds was suggested as playing an important role in the cytotoxic activity. The induction of caspase-3 and -7 activity represents some proof that apoptosis has occurred in treated cells. Globimetulin B ( 2 ) selectively killed cancer cells with less toxicity to non-cancerous cells as compared to conventional doxorubicin therapy.

The compound α-mangostin (AMG) extracted from Garcinia mangostana L. has potent anticancer properties but its clinical application is limited because of its poor solubility. In this study, AMG-loaded nanoparticles (NMG) were synthesized using a new formula and their apoptosis activity against human cervical carcinoma (HeLa) cells was investigated in comparison with organic solvent-soluble AMG in free form. The NMG was successfully synthesized with a particle size of <50 nm, polydispersity index <0.3, and zeta potential of −35.2 mV. At a concentration of 10 μg/mL, AMG reduced cell survival by 60%, whereas NMG treatment resulted in >90% cell death (p < 0.05). The AMG- or NMG-treated cells also showed changes in the size and shape and exhibited enhanced intensity of blue-stained nuclei, as well as decreased cell density, especially in NMG-treated cells. After 24 h of incubation with AMG or NMG, the cells went through late apoptosis at a rate of approximately 34% in 20 μg/mL AMG treatment and 27% in 10 μg/mL NMG treatment (p < 0.05). Thus, HeLa cells underwent more pronounced cell death through apoptosis induction caused by the NMG treatment compared to that caused by AMG. Clearly, the new NMG improved AMG bioavailability while maintaining the desired activity.

Helichrysum plicatum species are used in Turkish folk medicine as lithagogue, diuretic, and nephritic. Research on the methanol (MeOH) extract of flowers of H. plicatum DC. subsp. plicatum resulted in the isolation of eight known compounds ( 1–8 ). The chemical structures of the compounds were determined as β-sitosterol ( 1 ), apigenin ( 2 ), nonacosanoic acid ( 3 ), astragalin ( 4 ), β-sitosterol-3- O -β-D-glucopyranoside ( 5 ), helichrysin A ( 6 ), helichrysin B ( 7 ), and isosalipurposide ( 8 ) by spectroscopic and chromatographic/spectrometric methods, including 1D and 2D nuclear magnetic resonance and liquid chromatography-tandem mass spectrometry. Nonacosanoic acid ( 3 ) was isolated for the first time from H. plicatum DC. subsp. plicatum . The MeOH extract and isolated compounds were evaluated for their in vitro human carbonic anhydrase I (hCAI) and II (hCAII), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase inhibitory activities. The IC 50 values of H. plicatum DC. subsp. plicatum MeOH extract for hCAI, hCAII, AChE, BChE, and α-glycosidase were found to be 77.87, 52.90, 115.50, 117.46, and 81.53 mg/mL, respectively. The compounds showed IC 50 values of 1.43–4.47, 1.40–4.32, 1.69–2.90, 1.09–3.89, and 1.61–3.80 μM against hCAI, hCAII, AChE, BChE, and α-glycosidase, respectively. In summary, H. plicatum DC. subsp. plicatum secondary metabolites demonstrated strong inhibitory effects especially against hCAI and hCAII, whereas the MeOH extract showed a weak inhibitory effect on all enzymes.

The objective of this study is to determine essential oil, diterpenoid and phenolic contents of Sideritis hololeuca along with their biological activities. Phytol was found to be the main component of the essential oil. Seven known kaurane diterpenoids, siderol (140 mg, 0.16%, w/w), 7-acetoxy sideroxol (15 mg, 0.02%, w/w), eubol (6 mg, 0.01%, w/w), eubotriol (5 mg, 0.03%, w/w), 7-epicandicandiol (3 mg, 0.02%, w/w), ent -7α-acetoxy-18-hydroxykaur-16-ene (5 mg, 0.01%, w/w) and linearol [by liquid chromatography-tandem mass spectrometry (LC-MS/MS)] were determined from the species. Moreover, vanillin (21 mg, 0.10%, w/w), which was not isolated from any Sideritis species earlier, was isolated from an acetone extract of S. hololeuca . Quantitative amounts of some phenolic compounds in n -hexane, dichloromethane, acetone, methanol extracts and infusion and decoction of the plants were also investigated by LC-MS/MS. Antioxidant capacity and acetylcholinesterase, butyrylcholinesterase inhibition effects of the species were evaluated. The extracts of methanol and infusion and decoction of species showed moderate butyrylcholinesterase inhibition activity. The highest inhibition was observed from the decoction of species. The Cu 2+ reducing power of infusion was determined as 1.435 mmol TR g −1 .

The design of this study was developed to examine the chemical composition, anticholinesterase and anti-inflammatory inhibitory activities of the essential oil of Dipterocarpus cornutus Dyer from Malaysia. Gas chromatography (GC) and gas chromatography/mass spectrometry (GC-MS) analysis of the essential oil revealed 20 components, representing 94.6% of the oil. The major components identified were α-gurjunene (50.6%), α-selinene (8.3%), spathulenol (5.7%), and bicyclogermacrene (5.4%). Anticholinesterase and anti-inflammatory activity were also evaluated using the Ellman method and lipoxygenase (LOX) enzyme, respectively, in which the essential oil revealed weak inhibitory activity against the acetylcholinesterase (AChE) (I%: 30.2%) and butyrylcholinesterase (BChE) (I%: 32.5%), while moderate inhibitory activity was reported in the LOX (I%: 70.2%). The approach adopted in this study and results are reported for the first time which could be useful for the characterization, pharmaceutical and therapeutic applications of the essential oil from Dipterocarpus genus.