Alyssin and Iberin in Cruciferous Vegetables Exert Anticancer Activity in HepG2 by Increasing Intracellular Reactive Oxygen Species and Tubulin Depolymerization

To determine the chemopreventive potential of alyssin and iberin, the in vitro anticancer activities and molecular targets of isothiocyanates (ITCs) were measured and compared to sulforaphane in hepatocellular carcinoma cell HepG2. The SR-FTIR spectra observed a similar pattern vis-à-vis the biomolecular alteration amongst the ITCs-treated cells suggesting a similar mode of action. All of the ITCs in this study cause cancer cell death through both apoptosis and necrosis in concentration dependent manner (20–80 μM). We found no interactions of any of the ITCs studied with DNA. Notwithstanding, all of the ITCs studied increased intracellular reactive oxygen species (ROS) and suppressed tubulin polymerization, which led to cell-cycle arrest in the S and G₂/M phase. Alyssin possessed the most potent anticancer ability; possibly due to its ability to increase intracellular ROS rather than tubulin depolymerization. Nevertheless, the structural influence of alkyl chain length on anticancer capabilities of ITCs remains inconclusive. The results of this study indicate an optional, potent ITC (viz., alyssin) because of its underlying mechanisms against hepatic cancer. As a consequence, further selection and development of effective chemotherapeutic ITCs is recommended.

Antibacterial activity and bioactive compounds of 50% hydroethanolic extract of Alpinia zerumbet (Pers.) B.L. Burtt and amp; R.M. Sm

To evaluate antibacterial activity and the bioactive compounds of 50% hydroethanolic extract of Alpinia zerumbet (A. zerumbet) rhizomes. Methods: Eight reference microbial strains including two Gram-positive bacteria [Staphylococcus aureus (ATCC 29213) and Enterococcus faecalis (ATCC 29212)] and six Gram-negative bacteria [Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATTC 700603), Proteus mirabilis (DMST 8212), Salmonella enterica subsp. enterica serovar Vellore. (ATCC 15611), Shigella flexneri (ATCC 12022) and Pseudomonas aeruginosa (ATCC 27853)], were used to test antimicrobial susceptibility by the broth microdilution method. Bioactive compounds were analyzed by using HPLC. Results: The minimum inhibitory concentration values of A. zerumbet extract were 8 mg/mL for Staphylococcus aureus, Escherichia coli and Shigella flexneri and 16 mg/mL for Enterococcus faecalis and the other four Gram-negative bacilli. HPLC chromatograms revealed that the A. zerumbet extract contained hydroxybenzoic acids, hydroxycinnamic acids and flavonoids. Conclusions: The constituents of A. zerumbet rhizomes could be a potential source of antibacterial compounds, warranting further study of A. zerumbet extract.

Biomolecular changes and DNA targeting effect of sesamol in human lung adenocarcinoma (SK-LU-1) cells by FTIR microscopy

Objective: To investigate biomolecular alteration of sesamol on human lung adenocarcinoma (SK-LU-1) cells compared with cisplatin using Fourier transform infrared microscopy (FTIR). Methods: Cytotoxicity of sesamol was investigated against SK-LU-1 cells by using neutral red. DNA fragmentation and the cell cycle analysis were determined by agarose gel electrophoresis and flow cytometry, respectively. The FTIR microscopy technique was applied to explore the changes in cellular biochemical compositions in cells treated with sesamol that the biochemical and biological assays cannot cover. The alkylating property was determined by 4-(4-nitrobenzyl)pyridine assay. Results: Sesamol and cisplatin exerted an antiproliferative effect at 48 h with respective IC

Inhibition of two stages of melanin synthesis by sesamol, sesamin and sesamolin

Objective To investigate the antimelanogenesis properties of three sesame compounds-sesamol, sesamin and sesamolin via two stages of melanin synthesis vis-à-vis sunscreen function and enzyme inhibition in melanoma cell line in order to search for alternative depigmenting agents. Methods Antimelanogenic effects of sesame lignans were assessed in SK-MEL2 compared with the reference depigmenting agents, kojic acid and β-arbutin, in order to evaluate: (a) the sunscreen function of sesamol, sesamin and sesamolin by measurement of UV absorbtion property; (b) the inhibition of tyrosinase activity through mushroom and cellular tyrosinase; and (c) the effect on melanin content and melanogenic protein expression (tyrosinase, TRP-1 and TRP-2) by Western blot analysis; and (d) the toxicity of sesamol, sesamin and sesamolin to cells using cell cytotoxicity assay. Results The results showed that sesamin, sesamolin and sesamol exerted satisfiable sunscreen function by absorbed UVB at 290 nm. Sesamol exhibited the highest inhibition of mushroom tyrosinase activity, but lipophilic sesamolin exhibited the highest cellular tyrosinase inhibition (IC

Sulforaphene in Raphanus sativus L. var. caudatus Alef increased in late-bolting stage as well as anticancer activity

Objectives To evaluate the concentration differences of sulforaphene and sulforaphane at various ages and in different parts of Raphanus sativus L. var. caudatus with respect to their potential cancer preventive effect on HCT116 colon cancer cells. Methods FTIR–ATR and GC–MS were used to characterize the isothiocyanates in the plant extracts followed by HPLC for quantification. Antiproliferation and apoptosis induction were determined by using MTT assay and flow cytometry, respectively. Results The respective rank of anticancer activity of Raphanus sativus were as follows: vegetative (3 week) < older rosette (4 week) < early-bolting (5 week) < senescence (7 week) < late-bolting (6 week). The low to high concentration of sulforaphene and sulforaphane occurred in the same stage order. Conclusions The reproductive parts (flower, pod, and dry seed) of Raphanus sativus have the greatest isothiocyanate concentration, evidenced by a sulforaphene concentration higher than the sulforaphane. This result should inform the selection of the most appropriate harvesting stage and plant part for use as a potential chemopreventive agent.

Sulforaphene and sulforaphane in commonly consumed cruciferous plants contributed to antiproliferation in HCT116 colon cancer cells

Objective: To analyze two isothiocyanates (sulforaphene and sulforaphane) and their antiproliferative effect of 11 indigenous cruciferous vegetables. Methods: Phytoconstituents identification was conducted by high performance liquid chromatography and gas chromatography-mass spectrometer techniques. The antiproliferation was evaluated in colon cancer cell line HCT116 by MTT assay. Results: Isothiocyanate identification by high performance liquid chromatography showed that broccoli, cabbage, "Khi-Hood" (Raphanus sativus L. var. caudatus Alef) and Chinese radish contained isothiocyanates sulforaphane. Sulforaphene and sulforaphane in broccoli, cabbage and "Khi-Hood" were characterized by the gas chromatography-mass spectrometer analysis. Antiproliferation screening by MTT assay found that the potent plants which possessed IC

Synergistic anticancer effect of the extracts from Polyalthia evecta caused apoptosis in human hepatoma (HepG2) cells

Objective: To evaluate the anticancer activity of the extract fraction of Polyalthia evecta (P. evecta) (Pierre) Finet & Gagnep and the synergistic anticancer effect of the extracts from P. evecta by using the ATR/FT-IR spectroscopy. Methods: The 50% ethanol-water crude leaf extract of P. evecta (EW-L) was prepared and was further fractionated to isolate various fractions. The anticancer activity was investigated from cytotoxicity against HepG2 using a neutral red assay and apoptosis induction by evaluation of nuclei morphological changes after DAPI staining. Synergistic anticancer effects of the extracts from P. evecta were performed using the ATR/FT-IR spectroscopy. Results: The result showed that the EW-L showed higher cytotoxicity and apoptosis induction in HepG2 cells than its fractionated extracts. The hexane extract exhibited higher cytotoxicity and apoptosis induction than the water extracts, but less than the EW-L. The combined water and hexane extracts apparently increased cytotoxicity and apoptosis induction. The %apoptotic cells induced by the extract mixture were increased about 2-fold compared to the single hexane extract. Conclusions: The polar extract fraction is necessary for the anticancer activity of the non-polar extract fraction. The ATR/FT-IR spectra illustrates the physical interaction among the constituents in the extract mixture and reveals the presence of polyphenolic constituents in the EW-L, which might play a role for the synergistic anticancer effect.

Anticancer effect of the extracts from Polyalthia evecta against human hepatoma cell line (HepG2)

Objective: To investigate the anticancer activity of Polyalthia evecta (P. evecta) (Pierre) Finet& Gagnep against human hepatoma cell line (HepG2). Methods: The anticancer activity was based on (a) the cytotoxicity against human hepatoma cells (HepG2) assessed using a neutral red assay and (b) apoptosis induction determined by evaluation of nuclei morphological changes after DAPI staining. Preliminary phytochemical analysis of the crude extract was assessed by HPLC analysis. Results: The 50% ethanol-water crude leaf extract of P. evecta (EW-L) showed greater potential anticancer activity with high cytotoxicity [IC50 = (62.8 ± 7.3)μg/mL] and higher selectivity in HepG2 cells than normal Vero cells [selective index (SI) = 7.9]. The SI of EW-L was higher than the positive control, melphalan (SI = 1.6) and the apoptotic cells (46.4 ± 2.6) % induced by EW-L was higher than the melphalan (41.6 ± 2.1)% (P<0.05). The HPLC chromatogram of the EW-L revealed the presence of various kinds of polyphenolics and flavonoids in it. Conclusions:P. evecta is a potential plant with anticancer activity. The isolation of pure compounds and determination of the bioactivity of individual compounds will be further performed.

Antioxidant Activity and Cytotoxicity in Breast Cancer Cells Line of Mushrooms Extracts; Lentinus polychrous Lev. Compared to Ganoderma lucidum (Fr.) Karst

This study examined the antioxidative activity, and cytotoxic effect in breast cancer cell line (MCF-7) of medicinal mushrooms extracts; Lentinus polychrous Lev. and Ganoderma lucidum (Fr.) Karst. Antioxidative activity and cytotoxic effect were determined using the 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH) assay and the Neutral red assay, respectively. Results show that G. lucidum extracts from mycelia have antioxidative activity with the DPPH scavenging capacity in the range 1.34\±0.12 and 13.77\±0.98 \µmol/g and the total phenolic compounds in the range 9.91\±2.32 to 119.70\±1.74 mg/100g. L. polychrous Lev. extracts from mycelia had antioxidative activity with the DPPH scavenging capacity in the range 1.33\±1.58 to 11.84\±1.77 \µmol/g and the total phenolic compounds was approximately 10.42\±0.69 to 116.57\±5.27 mg/100g. This study shows that an extract from edible L. polychrous Lev. mushroom extracts exhibited similar antioxidative activity and the total phenolic compounds to the G. lucidum extracts. Moreover, the extract from G. lucidum caused a 50% decrease in breast cancer cell viability with concentration (IC₅₀) of 415.6 \µg/mL. The extract from L. polychrous Lev. mycelia demonstrated IC₅₀ values greater than 500 \µg/mL. It was found that the L. polychrous Lev. Mycelia extract; an edible mushroom in Thailand, possessed radical scavenging activity and the total phenolic content were not different from the G. lucidum extract. Future work on the separation of bioactive compounds contributing to the antioxidant activity and cytotoxicity of the L. polychrous Lev. Mycelia extract should be performed in comparison to the G. lucidum extract.