ABSTRACT
The chemical constituents from the fruits of Morinda citrifolia were systematically explored by chromatographic fractionation methods including silica gel, octadecylsilyl(ODS) gel, Sephadex LH-20 gel, and preparative high performance liquid chromatography(pre-HPLC). The chemical structures of all isolated compounds were identified on the basis of their physicochemical properties, spectroscopic analyses, as well as the comparisons of their physicochemical and spectroscopic data with the reported data in literature. As a result, 22 isolated compounds from the 90% ethanol extract of the fruits of M. citrifolia were identified, which were moricitritone(1), 2'-deoxythymidine(2), cyclo-(L-Pro-L-Tyr)(3), methyl-5-hydroxy-2-pyridinecarboxylate(4), methyl pyroglutamate(5), bisbenzopyran(6), epipinoresinol(7), 3, 3'-bisdemethyl pinoresinol(8), 3, 3'-bisdemethyltanegool(9), trimesic acid(10), crypticin B(11), kojic acid(12), vanillic acid(13), protocatechoic acid(14), 5-hydroxymethyl furfural(15), blumenol A(16), 1-O-(9Z, 12Z-octadecadienoyl) glycerol(17), mucic acid dimethylester(18), methyl 2-O-β-D-glucopyranosylbenzoate(19), 2-phenylethyl-O-β-D-glucoside(20), scopoletin(21), and quercetin(22). Among them, compound 1 was a new pyrone derivative, compounds 2, 4-7, 10-12, and 17 were isolated from the plants belonging to Morinda genus for the first time, and compound 18 was obtained from M. citrifolia for the first time. Moreover, on the basis of testing the activities of all isolated compounds on inhibiting the proliferation of synovial fibroblasts in vitro by MTS assay, the anti-rheumatoid arthritis activities of all isolated compounds were initially evaluated. The results showed that compounds 1-6, 9, 19, and 20 exhibited remarkable anti-rheumatoid arthritis activities, which displayed the inhibitory effects on the proliferation of MH7A synovial fibroblast cells with the IC_(50) values in the range of(3.69±0.08) to(168.96±0.98) μmol·L~(-1).
Subject(s)
Fruit/chemistry , Morinda/chemistry , Synoviocytes , Cell Proliferation , ArthritisABSTRACT
The chemical constituents from the stems and leaves of Cratoxylum cochinchinense were isolated and purified using silica gel, ODS gel, and Sephadex LH-20 gel column chromatography, as well as preparative HPLC. The chemical structures of all isolated compounds were identified on the basis of their physicochemical properties, spectroscopic analyses, and the comparison of their physicochemical and spectroscopic data with the reported data in literature. As a result, 21 compounds were isolated from the 90% ethanol extract of the stems and leaves of C. cochinchinense, which were identified as cratocochine(1), 1-hydroxy-3,7-dimethoxyxanthone(2), 1-hydroxy-5,6,7-trimethoxyxanthone(3), ferrxanthone(4), 3,6-dihydroxy-1,5-dimethoxyxanthone(5), 3,6-dihydroxy-1,7-dimethoxyxanthone(6), 1,2,5-trihydroxy-6,8-dimethoxyxanthone(7), securixanthone G(8), gentisein(9), 3,7-dihydroxy-1-methoxyxanthone(10), pancixanthone B(11), garcimangosxanthone A(12), pruniflorone L(13), 9-hydroxy alabaxanthone(14), cochinchinone A(15), luteolin(16), 3,5'-dimethoxy-4',7-epoxy-8,3'-neolignane-5,9,9'-triol(17), N-benzyl-9-oxo-10E,12E-octadecadienamide(18), 15-hydroxy-7,13E-labdadiene(19), stigmasta-4,22-dien-3-one(20), and stigmast-5-en-3β-ol(21). Among these isolates, compound 1 was a new xanthone, compounds 2-5, 7, 8, 12, and 16-21 were isolated from the Cratoxylum plant for the first time, and compounds 11 and 13 were obtained from C. cochinchinense for the first time. Furthermore, all isolated compounds 1-21 were appraised for their anti-rheumatoid arthritis activities by MTS method through measuring their anti-proliferative effect on synoviocytes in vitro. As a result, xanthones 1-15 displayed notable anti-rheumatoid arthritis activities, which showed inhibitory effects on the proliferation of MH7A synoviocytes with the IC_(50) values ranging from(8.98±0.12) to(228.68±0.32) μmol·L~(-1).
Subject(s)
Synoviocytes , Clusiaceae/chemistry , Xanthones/analysis , Plant Leaves/chemistry , Cell Proliferation , ArthritisABSTRACT
Objective: To develop the photosensitizer rose-bengal (RB)/upconverting nanoparticles (UCNPs)/dihydroartemisinin (DHA) co-encapsulated liposomes (LIP-RUD) and preliminarily study the in vitro inhibition effects on human colon cancer. Methods: The hydrophilic UCNPs were synthesized by solvothermal and ligand conversion and RB/UCNPs/DHA were encapsulated by thin-film dispersion method to obtain LIP-RUD. HPLC was performed to determine the loading ratio (LR) of RB and DHA. Zetasizer was used to evaluate the physiochemical properties of liposomes. The production of ROS was investigated by SOSG probe. In vitro cellular uptake of LIP-RUD was observed by confocal laser scanning microscopy (CLSM) and the cytotoxicity on HCT-116 cells was estimated by MTT assay. Results: LIP-RUD showed an average particle diameter of 150 nm with zeta potential of -12 mV. The LR of RB and DHA were 54.5% and 86.5%, respectively. The energy conversion efficiency of UCNPs and RB reached 49.8%. After irradiation, the singlet oxygen (1O2) was generated and 74.9% of encapsulated DHA was released from LIP-RUD at 12 h, which showed an improvement of up to 25.6% compared to the absence of laser irradiation group. In cellular experiments, LIP-RUD exerted improved cytotoxicity on HCT-116 cells. IC50 was 15.33 μmol/L under laser irradiation. Conclusion: LIP-RUD provides a new thought in the treatment of human colon cancer by the combination of photodynamic therapy (PDT) and chemotherapy, which is expected to enhance the penetration depth of PDT and the therapeutic effect of combination therapy.
ABSTRACT
Evaluation of the relative efficacy of powdered leaf extracts of Aloe vera(Linn) and Aloe schweinfurthii(Baker) in the control of some plant pathogens was undertaken in this work. Antimicrobial activities ofthe extracts obtained using cold water, hot water and ethanol were tested against four fungal spp., namely, Alternaria solani,Colletotrichum lindemuthianum, Sclerotium rolfsiiand Trichophyton rubrum. The phytochemical screening of the leaf extracts of the two aloe species revealed the presence of bioactive compounds such as alkaloids, tannins, saponins, flavonoids, cardiac glycosides, phytates and oxalates. The extracts were observed to exhibit varying inhibitory effects on the selected fungi. Ethanolic extract of A. veraat 50mg/ml and 100mg/ml had the greatest impact on A. solaniand C. lindemuthianum respectively.Similarly, cold water extract of A. schweinfurthiiat 100mg/ml was the most effective against S. rolfsiiandT. rubrum.However, hot water extract of A. vera wasleast effective against C. lindemuthianum. Also, the efficacy of cold water extract of A. schweinfurthii at 50mg/mlwas very low against T. rubrumand A. solani. The hot water extract of A. schweinfurthii at 20mg/ml also showed the least effect against S. rolfsii. Consequently, extracts from both Aloe species can be recommended in the management of the four fungal pathogens evaluated in this study. It is hoped that in no distant future, botanical fungicides would be developed from the two Aloe species
ABSTRACT
Objective To investigate the effect of Semaphorin3A (Sema3A) on axon growth of primary retinal ganglion cells (RGCs) in mice.Methods C57/BL6 mice within 24 hours after birth were sacrificed and the eyeballs were removed,RGCs was isolated from retina and cultured in vitro.The primary cultured RGCs was identified by Brn3a immunofluorescence staining.Seven days after culture,the RGCs was divided into control group,0.05 μg/ml Sema3A group,0.10 μg/ml Sema3A group and 0.50 μg/ml Sema3A group,and the processing time was 2 hours.Immunofluorescence staining was used to detect the expression of neuron-specific marker β3-tubulin and dendritic marker MAP2,β3-tubulin+/MAP2-was identified as axons.The length of axons was measured by Image J software.The axon lengths of 0.10 μg/ml Sema3A group and control group at 0.5,1 and 2 hours after treatment were calculated.The primary cultured cells were divided into control group,Sema3A treatment group,Y27632 treatment group and combined treatment group according to different drugs.The average axon lengths were compared among the groups.The use and care of the animals complied with the Statement of the Association for Research in Vision and Ophthalmology (ARVO).Results Brn3a was positively expressed in primary cultured RGCs as a specific cell marker.Seven days after culture,RGCs tended to mature,with complete elongated neuronal processes and branches.The axon lengths of 0.05,0.10 and 0.50 μg/ml Sema3A groups were (69.35±1.49),(60.45±1.42) and (93.65±1.86) μm,which were significantly shorter than (109.80±2.29) μm of the control group (all at P＜0.01).The axon length of 0.10 μg/ml Sema3A group was (165.00 ±4.39)μm and (97.63 ±2.79)μm at 1 hour and 2 hours after treatment,respectively,which was significantly lower than (210.40 ±4.44) μm and (199.00 ± 4.36) μm of control group at corresponding time points (both at P＜0.01).There was a significant difference in the axon length of control group,Sema3A treatment group,mixed treatment group and Y27632 treatment group (F =142.50,P＜0.01).The RGC axon length of Sema3A treatment group was significantly lower than that of control group and combined treatment group (both at P＜0.01).Conclusions Sema3A can inhibit axon growth of primary retinal RGCs in mice,and ROCK signaling pathway inhibitors can alleviate such restrain effect.
ABSTRACT
UDP-glucuronosyltransferase 1A1 (UGT1A1) plays a key role in detoxification of many potentially harmful compounds and drugs. UGT1A1 inhibition may bring risks of drug-drug interactions (DDIs), hyperbilirubinemia and drug-induced liver injury. This study aimed to investigate and compare the inhibitory effects of icotinib and erlotinib against UGT1A1, as well as to evaluate their potential DDI risksUGT1A1 inhibition. The results demonstrated that both icotinib and erlotinib are UGT1A1 inhibitors, but the inhibitory effect of icotinib on UGT1A1 is weaker than that of erlotinib. The ICvalues of icotinib and erlotinib against UGT1A1-mediated NCHN--glucuronidation in human liver microsomes (HLMs) were 5.15 and 0.68 μmol/L, respectively. Inhibition kinetic analyses demonstrated that both icotinib and erlotinib were non-competitive inhibitors against UGT1A1-mediated glucuronidation of NCHN in HLMs, with thevalues of 8.55 and 1.23 μmol/L, respectively. Furthermore, their potential DDI risksUGT1A1 inhibition were quantitatively predicted by the ratio of the areas under the concentration-time curve (AUC) of NCHN. These findings are helpful for the medicinal chemists to design and develop next generation tyrosine kinase inhibitors with improved safety, as well as to guide reasonable applications of icotinib and erlotinib in clinic, especially for avoiding their potential DDI risksUGT1A1 inhibition.
ABSTRACT
Objective: To investigate the antibacterial activities of green vegetables (pennywort, mint, garlic, parsley and celery) against four common enteric bacteria [Salmonella enterica (ATCC 25957) (S. enterica), Shigella flexneri (ATCC 12022) (S. flexneri), Escherichia coli (ATCC 43889) (E. coli) and Enterobacter cloacae (ATCC 13047) (E. cloacae)] as an alternative medicine for controlling food borne diarrhea disease and the synergistic effect of green vegetables against those bacteria. Methods: Five common vegetables (pennywort, mint, garlic, parsley and celery) were purchased and extracted. The antimicrobial activities of these extracts were tested against four common enteric bacteria (S. enterica, S. flexneri, E. coli and E. cloacae). Ten different concentrations of the extracts (from 640 to 1.25 mg/mL) were prepared and used for the study. The minimal inhibitory concentration (MIC) was determined by the broth dilution method. The antimicrobial activities were assessed by using both well diffusion and disc diffusion methods. Results: Garlic extract showed excellent inhibitory effects on all enteric bacteria. Other plants (parsley, celery, mint and pennywort) were not effective against enteric bacteria. The MIC of garlic against S. flexneri and E. cloacae was 40 mg/mL. The MIC of S. enterica and E. coli were 20 and 10 mg/mL, respectively. The performance of the well diffusion method was better than that of the disc diffusion method with clear and sharp inhibition zones of tested bacteria against plant extracts. Conclusions: Garlic had excellent antimicrobial effects against enteric bacteria and was recommended to be given to patients with gastroenteritis. The other vegetables (pennywort, mint, parsley and celery) showed no inhibitory effects on enteric bacteria but still can be used for its richness in vitamins and fibers. The performance of the well diffusion method was better than that of the disc diffusion method in detecting the antibacterial effects of green vegetables.
ABSTRACT
The study aimed to evaluate the possible inhibitory effects of different concentrations of crabgrass (Digitaria horizontalis Willd.) dry mass incorporated to the soil over the germination and early growth of soybean (Glycine max (L.) Merril.), dry bean (Phaseolus vulgaris L.), and turnip (Raphanus raphanistrum L.). The experimental design adopted was completely random, with four replications where, each one was consisted of a 2.5 L capacity pot. Dry mass of crabgrass at equivalent amounts of 0, 2.5, 5.0 and 10 t ha-1 were incorporated into the soil. Crops seedling emergence was checked daily, and germination, speed germination index, mean germination time, relative frequency and synchronization index of germination were computed at the final of 10 days .The height and dry mass of plants were evaluated at 35 days after sowing. The incorporation to the soil of D. horizontalis dry mass caused significant reduction of the height and dry weight of soybean, dry bean and turnip, but were not observed consistent influence over the germination of these species.
Subject(s)
Digitaria , Phaseolus , Plant Weeds , Raphanus , Glycine maxABSTRACT
Xanthine oxidase inhibitory activity has been reported from different plants such as Cinnamomum cassia, Chrysanthemum indicum, Lycopus europaeus, Polygonum cuspidatum, Acacia confuse, Coccinia grandis, Datura metel, Strychnos nux-vomica, Vitex negundo, Coccinia grandis, Vitex negundo, Fraxinus angustifolia, Pistacia lentiscus, Hyptis obtusiflora, H. lantanaefolia, Artemisia vulgaris, Caesalpinia sappan, Blumea balsamifera, Chrysanthemum sinense, Tetracera scandens, C. sinense, Allium Cepa, Pistacia integerrima, Caesalpinia sappan and Caesalpinia sappan. This review very clearly specify that plants could be utilized for the inhibition of xathine oxidase and out of them Clerodendrum floribundum, Eremophila maculata, Stemodia grossa Benth, Eucalyptus deglupta, Syzygium malaccense and Larix laricina exhibited 84%, 61%, 57%, 51%, 64%, 86 % xanthine pxidase inhibition at concentration of 50 μg/ml, 50 μg/ml, 50 μg/ml, 44.5 μg/ml, 51 μg/ml, 6.26mg/dl respectively.
ABSTRACT
The recombinant human fusion protein GM-CSF/LIF was used to study the effects of different doses rhGM-LIF, rhGM-CSF,rhLIF,and rhGM-CSF plus rhLIF on tumor cells in our paper. The results showed that rhGM-LIF induced myeloid leukemia cells differentiation and inhibited the growth of the cells significantly. Its effect was dose-related, more significantly than rhGM-CSF,rhLIF,and rhGM-CSF plus rhLIF in some dose range. It is important that rhGM-LIF can inhibit the growth of human liver cancer cell. The rhGM-LIF might be a useful recombinant protein for tumor thera-py.