ABSTRACT
Structural characteristics-guided investigation of Ailanthus altissima (Mill.) Swingle resulted in the isolation and identification of seven undescribed potential Michael reaction acceptors (1-7). Ailanlactone A (1) possesses an unusual 1,7-epoxy-11,12-seco quassinoid core. Ailanterpene B (6) was a rare guaianolide-type sesquiterpene with a 5/6/6/6-fused skeleton. Their structures were determined through extensive analysis of physiochemical and spectroscopic data, quantum chemical calculations, and single crystal X-ray crystallographic technology using Cu Kα radiation. The cytotoxic activities of isolates on HepG2 and Hep3B cells were evaluated in vitro. Encouragingly, ailanaltiolide K (4) showed significant cytotoxicity against Hep3B cells with IC50 values of 1.41 ± 0.21 µM, whose covalent binding mode was uncovered in silico.
Subject(s)
Ailanthus , Quassins , Ailanthus/chemistry , Plant Extracts/chemistry , Plant Leaves , Quassins/chemistryABSTRACT
BACKGROUND: Patients with N2-3 nasopharyngeal carcinoma have a high risk of treatment being unsuccessful despite the current practice of using a concurrent adjuvant cisplatin-fluorouracil regimen. We aimed to compare the efficacy and safety of concurrent adjuvant cisplatin-gemcitabine with cisplatin-fluorouracil in N2-3 nasopharyngeal carcinoma. METHODS: We conducted an open-label, randomised, controlled, phase 3 trial at four cancer centres in China. Eligible patients were aged 18-65 years with untreated, non-keratinising, stage T1-4 N2-3 M0 nasopharyngeal carcinoma, an Eastern Cooperative Oncology Group performance status score of 0-1, and adequate bone marrow, liver, and renal function. Eligible patients were randomly assigned (1:1) to receive concurrent cisplatin (100 mg/m2 intravenously) on days 1, 22, and 43 of intensity-modulated radiotherapy followed by either gemcitabine (1 g/m2 intravenously on days 1 and 8) and cisplatin (80 mg/m2 intravenously for 4 h on day 1) once every 3 weeks or fluorouracil (4 g/m2 in continuous intravenous infusion for 96 h) and cisplatin (80 mg/m2 intravenously for 4 h on day 1) once every 4 weeks, for three cycles. Randomisation was done using a computer-generated random number code with a block size of six, stratified by treatment centre and nodal category. The primary endpoint was 3-year progression-free survival in the intention-to-treat population (ie, all patients randomly assigned to treatment). Safety was assessed in all participants who received at least one dose of chemoradiotherapy. This study was registered at ClinicalTrials.gov, NCT03321539, and patients are currently under follow-up. FINDINGS: From Oct 30, 2017, to July 9, 2020, 240 patients (median age 44 years [IQR 36-52]; 175 [73%] male and 65 [27%] female) were randomly assigned to the cisplatin-fluorouracil group (n=120) or cisplatin-gemcitabine group (n=120). As of data cutoff (Dec 25, 2022), median follow-up was 40 months (IQR 32-48). 3-year progression-free survival was 83·9% (95% CI 75·9-89·4; 19 disease progressions and 11 deaths) in the cisplatin-gemcitabine group and 71·5% (62·5-78·7; 34 disease progressions and seven deaths) in the cisplatin-fluorouracil group (stratified hazard ratio 0·54 [95% CI 0·32-0·93]; log rank p=0·023). The most common grade 3 or worse adverse events that occurred during treatment were leukopenia (61 [52%] of 117 in the cisplatin-gemcitabine group vs 34 [29%] of 116 in the cisplatin-fluorouracil group; p=0·00039), neutropenia (37 [32%] vs 19 [16%]; p=0·010), and mucositis (27 [23%] vs 32 [28%]; p=0·43). The most common grade 3 or worse late adverse event (occurring from 3 months after completion of radiotherapy) was auditory or hearing loss (six [5%] vs ten [9%]). One (1%) patient in the cisplatin-gemcitabine group died due to treatment-related complications (septic shock caused by neutropenic infection). No patients in the cisplatin-fluorouracil group had treatment-related deaths. INTERPRETATION: Our findings suggest that concurrent adjuvant cisplatin-gemcitabine could be used as an adjuvant therapy in the treatment of patients with N2-3 nasopharyngeal carcinoma, although long-term follow-up is required to confirm the optimal therapeutic ratio. FUNDING: National Key Research and Development Program of China, National Natural Science Foundation of China, Guangdong Major Project of Basic and Applied Basic Research, Sci-Tech Project Foundation of Guangzhou City, Sun Yat-sen University Clinical Research 5010 Program, Innovative Research Team of High-level Local Universities in Shanghai, Natural Science Foundation of Guangdong Province for Distinguished Young Scholar, Natural Science Foundation of Guangdong Province, Postdoctoral Innovative Talent Support Program, Pearl River S&T Nova Program of Guangzhou, Planned Science and Technology Project of Guangdong Province, Key Youth Teacher Cultivating Program of Sun Yat-sen University, the Rural Science and Technology Commissioner Program of Guangdong Province, and Fundamental Research Funds for the Central Universities.
Subject(s)
Nasopharyngeal Neoplasms , Neutropenia , Adolescent , Male , Humans , Female , Adult , Cisplatin , Nasopharyngeal Carcinoma/drug therapy , Gemcitabine , China , Deoxycytidine , Chemoradiotherapy , Fluorouracil , Neutropenia/chemically induced , Nasopharyngeal Neoplasms/pathology , Antineoplastic Combined Chemotherapy Protocols/adverse effects , Chemotherapy, AdjuvantABSTRACT
As a medicinal plant, Artemisia annua is widely distributed in China. The purpose of this work was to analyze the chemical composition of essential oil from A. annua aerial portions, as well as to assess its repellent activity against Lasioderma serricorne and Tribolium castaneum adults. GC-FID and GC-MS analyses enabled the identification of 15 components representing 90.1% of the essential oil. The main components included artemisia ketone (70.6%), α-caryophyllene (5.1%) and germacrene D (3.8%). The essential oil was found to possess considerable ability to repel the two storage pests. This paper provided some evidence for the exploitation and utilization of A. annua resources as a natural repellent.
Subject(s)
Artemisia annua/chemistry , Coleoptera/drug effects , Insect Repellents/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Pest Control, Biological , Plant Components, Aerial/chemistry , Tribolium/drug effects , Animals , China , Gas Chromatography-Mass Spectrometry , Insect Repellents/chemistry , Insecticides/chemistry , Insecticides/pharmacology , Monoterpenes/pharmacologyABSTRACT
According to the classification of traditional Chinese medicine syndromes of coronavirus disease 2019 by the national competent authority, this study determined that human coronavirus 229 E(HCoV-229 E) was infected in a mouse model of cold and dampness syndrome, so as to build the human coronavirus pneumonia with pestilence attacking lung syndrome model. The model can simulate the traditional Chinese medicine treatment of common disease syndromes in Coronavirus Disease 2019 Diagnosis and Treatment Program(the sixth edition for trial). Specific steps were as follows. ABALB/c mouse model of cold and dampness syndrome was established, based on which, HCoV-229 E virus was infected; then the experiment was divided into normal control group, infection control group, cold-dampness control group, cold-dampness infection group(the model group), high-dose Chaiyin Particles group(8.8 g·kg~(-1)·d~(-1)), and low-dose Chaiyin Particles group(4.4 g·kg~(-1)·d~(-1)). On the day of infection, Chaiyin Particles was given for three consecutive days. Lung tissues were collected the day after the last dose, and the lung index and inhibition rate were calculated. The nucleic acid of lung tissue was extracted, and the HCoV-229 E virus load was detected by Real-time fluorescent quantitative RT-PCR. Blood leukocytes were separated, and the percentage of T and B lymphocytes was detected by flow cytometry. Lung tissue protein was extracted, and IL-6, IL-10, TNF-α and IFN-γ contents were detected by ELISA. High and low-dose Chaiyin Particles significantly reduced the lung index(P<0.01) of mice of human coronavirus pneumonia with pestilence attacking the lung syndrome, and the inhibition rates were 61.02% and 55.45%, respectively. Compared with the model control group, high and low-dose Chaiyin Particles significantly increased cross blood CD4~+ T lymphocytes, CD8~+T lymphocytes and total B lymphocyte percentage(P<0.05, P<0.01), and reduced IL-10, TNF-α and IFN-γ levels in lungs(P<0.01). In vitro results showed that TC_(50), TC_0, IC_(50) and TI of Chaiyin Particles were 4.46 mg·mL~(-1), 3.13 mg·mL~(-1), 1.12 mg·mL~(-1) and 4. The control group of in vitro culture cells had no HCoV-229 E virus nucleic acid expression. The expression of HCoV-229 E virus nucleic acid in the virus control group was 1.48×10~7 copies/mL, and Chaiyin Particles significantly reduced HCoV-229 E expression at doses of 3.13 and 1.56 mg·mL~(-1), and the expression of HCoV-229 E nucleic acid was 9.47×10~5 and 9.47×10~6 copies/mL, respectively. Chaiyin Particles has a better effect on the mouse model with human coronavirus pneumonia with pestilence attacking the lung syndrome, and could play a role by enhancing immunity, and reducing inflammatory factor expression.
Subject(s)
Coronavirus 229E, Human , Coronavirus Infections/immunology , Coronavirus Infections/therapy , Drugs, Chinese Herbal/therapeutic use , Animals , Humans , Lung/immunology , Lung/virology , Medicine, Chinese Traditional , Mice , Mice, Inbred BALB CABSTRACT
The aim of this paper was to investigate the therapeutic effect of Compound Qinlan Oral Liquid recommended by Provincial Novel Coronary Virus Pneumonia Treatment Scheme on the treatment of BALB/c mice with combining disease with syndrome of human coronavirus pneumonia with pestilence attacking lung syndrome and to explore its clinical application in the treatment of novel coronavirus pneumonia, and to provide laboratory data support for clinical Chinese medicine. According to the classification of syndromes of novel coronavirus pneumonia by the national competent department of traditional Chinese medicine, this study determined that human coronavirus 229 E(HCoV-229 E)-infected mouse model of cold and dampness syndrome can be used to study human coronavirus pneumonia combined with pestilence attacking the lung syndrome model. This model is suitable for simulating traditional Chinese medicine treatment of common disease syndromes in Novel Coronavirus Pneumonia Diagnosis and Treatment program(trial implementation of the sixth edition). Specific steps are as follows. BALB/c mice of cold and dampness syndrome is infected with HCoV-229 E virus, and were divided into normal control group, infection control group, cold-dampness control group, cold-dampness infection group(the model group), and Compound Qilan Oral Liquid high dose group(22 mL·kg~(-1)·d~(-1)) and low dose group(11 mL·kg~(-1)·d~(-1)). On the day of infection, the Compound Qilan Oral Liquid was administered for three consecutive days. On the last dosing day, the lung tissue was dissected, and the lung index and inhibition rate were calculated. The nucleic acid of lung tissue was extracted and the HCoV-229 E virus load was detected by RT-PCR. Blood leukocytes were separated and the percentage of T and B lymphocytes was detected by flow cytometry. Lung tissue protein was extracted and the contents of IL-6, IL-10, TNF-α and IFN-γ were detected by ELISA. Serum was separated and the contents of gastrin(GAS) and motilin(MTL) were detected by ELISA. Histopathological analysis was performed with lung tissue. The high and low doses of Compound Qinlan Oral Liquid significantly reduced the lung index(P<0.01) of mice with combining disease with syndrome of human coronavirus pneumonia with pestilence attacking lung syndrome, and the inhibition rates were 59.01% and 47.72%, respectively. Compared with the model control group, the high and low doses of Compound Qinlan Oral Liquid significantly reduced lung tissue viral load(P<0.01), increased cross blood CD4~+ T lymphocytes, CD8~+ T lymphocytes and total B lymphocyte percentage(P<0.01), reduced serum motilin content(P<0.01), reduced IL-6, IL-10, TNF-α and IFN-γ levels in lungs(P<0.01) and reduced lung tissue inflammation. Compound Qinlan Oral Liquid has a better effect on the mouse model with combining disease with syndrome of human coronavirus pneumonia with pestilence attacking lung syndrome, which may attribute to its function of in virus replication inhibition, gastrointestinal function improvement, immunity enhancement, and inflammatory factor reduction.
Subject(s)
Betacoronavirus , Coronavirus Infections , Lung , Pandemics , Pneumonia, Viral , Animals , COVID-19 , Mice , Mice, Inbred BALB C , SARS-CoV-2ABSTRACT
This paper aimed to investigate the active components and molecular mechanism of Xiao'er Resuqing Oral Liquid on hand, foot and mouth disease(HFMD) based on network pharmacology and molecular docking methods. The potential active components of 8 herbs in Xiao'er Resuqing Oral Liquid were selected through Traditional Chinese Medicine Systems Pharmacology Database(TCMSP), Batman database and relevant literature consultation. Then related targets for the medicine were analyzed through PubChem and Swiss Target Prediction database, while related targets for HFMD were analyzed through GeneCards platform. The common targets for medicine and disease were put into STRING database to obtain the potential targets of Xiao'er Resuqing Oral Liquid for treatment of HFMD. The Cytoscape software was used to establish the "herbs-components-targets-disease" network. The protein-protein interaction(PPI) network was constructed based on STRING platform and Cytoscape software to screen the core targets. Based on Metascape platform, GO function enrichment analysis and KEGG signal pathway enrichment analysis were carried out. The main active components and potential key targets of Xiao'er Resuqing Oral Liquid were verified by molecular docking with Autodock vina 1.1.2 software. A total of 118 potential active components and 123 potential targets for treatment of HFMD were collected. PPI network indicated a total of 23 key targets, such as AKT1, MAPK1, IL6, VEGFA, EGFR, TNF, HRAS, CCND1, and CXCL8. GO function enrichment analysis results showed that there were 381 GO biological processes, 127 GO cellular components, and 117 GO molecular functions(P<0.01). KEGG enrichment analysis showed that 116 signal pathways were obtained(P<0.01), and the results showed that it was mainly associated with TNF signal pathway, IL-17 signal pathway, inflammatory mediator regulation of TRP channels, and cytokine-cytokine receptor interaction. Molecular docking results showed that the main active components all had a high binding ability with the main potential key targets. This study preliminarily investigated the multi-pathways, multi-targets and multi-components molecular mechanism of Xiao'er Resuqing Oral Liquid for treatment of HFMD, providing theoretical references for further researches on its active components and action mechanism.
Subject(s)
Drugs, Chinese Herbal , Hand, Foot and Mouth Disease , Humans , Medicine, Chinese Traditional , Molecular Docking Simulation , Signal TransductionABSTRACT
BACKGROUND AND PURPOSE: Nasopharyngeal carcinoma (NPC) patients can be separated into two risk subgroups according to tumor responses to induction chemotherapy (IC). We aimed to elucidate the optimal cumulative cisplatin dose (CCD) of concurrent chemoradiotherapy (CCRT) for different NPC patient subgroups. PARTICIPANTS AND METHODS: A total of 990 patients with incident NPC diagnosed between 2008 and 2017 treated with IC plus CCRT were included in our observational study. The clinicopathological features of patients with different tumor responses were compared using the Chi-square test or Fisher's exact test. Prognosis was assessed using a multivariate Cox proportional hazards model. In addition, acute and late toxicities were compared between different CCD groups. RESULTS: After IC, 761/990 (76.9%) patients had a complete tumor response (CR)/partial response (PR) and 229 (23.1%) had stable disease (SD)/disease progression (PD). An unsatisfactory tumor response (SD/PD) after IC correlated with poor clinical outcome (3-year PFS 61.4% vs. 83.2%, Pâ¯<â¯0.001 and 3-year LRFS 80.9% vs. 94.5%, Pâ¯<â¯0.001). Patients who achieved CR/PR after IC received a CCD >200â¯mg/m2 and showed higher 3-year PFS and DMFS rates than those receiving a CCD <100â¯mg/m2 (PFS: 85.4% vs. 77.9%, Pâ¯=â¯0.045; DMFS: 89.4% vs. 77.9%, Pâ¯=â¯0.015). Multivariate analysis also showed that CCD was an independent prognostic factor for PFS and DMFS in CR/PR subgroup. Moreover, the medium dose group showed similar efficacy as high dose group but was associated with fewer grade 1-4 acute toxicities. However, application of different CCD didn't result in significantly different survival outcomes in SD/PD subgroup. CONCLUSIONS: Tumor response to IC was an independent prognostic factor for patients with NPC. For the patients who achieved CR/PR after IC, patients receiving high CCD showed significantly improved 3-year PFS and DMFS compared with patients receiving low CCD. Balancing toxicity and efficacy, 200â¯mg/m2 seemed to be the optimal dose in the CR/PR groups. However, enhancement of CCD did not provide survival benefit for patients who achieved SD/PD after IC, and treatment options for these patients require further consideration.
Subject(s)
Antineoplastic Combined Chemotherapy Protocols/administration & dosage , Cisplatin/administration & dosage , Nasopharyngeal Carcinoma/drug therapy , Nasopharyngeal Neoplasms/drug therapy , Adolescent , Adult , Aged , Chemoradiotherapy , Child , Disease Progression , Docetaxel/administration & dosage , Dose-Response Relationship, Drug , Female , Fluorouracil/administration & dosage , Humans , Male , Middle Aged , Multivariate Analysis , Nasopharyngeal Carcinoma/pathology , Nasopharyngeal Carcinoma/radiotherapy , Nasopharyngeal Neoplasms/pathology , Nasopharyngeal Neoplasms/radiotherapy , Neoplasm Staging , Paclitaxel/administration & dosage , Prognosis , Proportional Hazards Models , Remission Induction , Retrospective Studies , Young AdultABSTRACT
The essential oil was extracted from the roots of Valeriana officinalis L. by hydrodistillation. The qualitative and quantitative analysis of its chemical constituents was conducted on GC-MS and GC-FID in this study. Seventeen compounds were detected and the major constituents included bornyl acetate (48.2%) and camphene (13.8%). The toxic and repellent effects of the essential oil and its two major constituents were evaluated on Liposcelis bostrychophila and Tribolium castaneum. The results of bioassays indicated that the essential oil showed the promising fumigant and contact toxicity against L. bostrychophila (LC50 = 2.8 mg/L air and LD50 = 50.9 µg/cm2, respectively) and the notable contact effect on T. castaneum (LD50 = 10.0 µg/adult). Meanwhile, the essential oil showed comparable repellent effect on T. castaneum at all testing concentrations. Bornyl acetate and camphene also exhibited strong fumigant and contact toxicity against both species of pests (LC50 = 1.1, 10.1 mg/L air and LD50 = 32.9, 701.3 µg/cm2 for L. bostrychophila; > 126.3, 4.1 mg/L air, and 66.0, 21.6 µg/adult for T. castaneum). Bornyl acetate and camphene showed moderate repellent effect on T. castaneum and conversely showed attractant effect on L. bostrychophila. This work highlights the insecticidal potential of V. officinalis, which has been noted as a traditional medicinal plant.
Subject(s)
Camphanes/pharmacology , Insect Repellents/pharmacology , Oils, Volatile/pharmacology , Terpenes/pharmacology , Valerian/chemistry , Animals , Bicyclic Monoterpenes , Food Storage , Gas Chromatography-Mass Spectrometry , Oils, Volatile/analysis , Oils, Volatile/chemistry , Phthiraptera/drug effects , Tribolium/drug effectsABSTRACT
In this work, the essential oils (EO) were extracted from seven typical Chinese herbs, and their repellent and contact toxicities against Tribolium castaneum adults (red flour beetles) were evaluated. The experimental results showed that the above EOs presented the various levels of repellent and contact toxicities. The EOs extracted from A. lancea and A argyi of the Compositae (Asteraceae) family presented obvious repellent effects (Repellency Percentageâ¯>â¯90% at 3.15â¯nL/cm2 after 4â¯h exposure) and strong contact toxicity with LD50 values of 5.78 and 3.09⯵g/adult respectively. Based on literature researches and screening results, the EO from A. lancea was analyzed by GC-MS and chosen for further identification of bioactive components. Altogether 59 chemical components were identified and 17 of them were recognized as sesquiterpene compounds, accounting for 57.8% of the total weight of the EO. From the identified sesquiterpenes, three individual compounds (ß-eudesmol, hinesol, valencene) were selected for the laboratory bioassays of the toxicity against red flour beetles. It was found that all the three compounds expressed some repellent effects. Although ß-eudesmol (31.2%) and hinesol (5.1%) were identified as main constituents and had been considered to be symbolic characteristics of high medicinal value, valencene (0.3%) showed strong repellent property which could be comparable to that of DEET (N, Ndiethyl3methylbenzamide), a powerful commercial pesticides, and it had best toxicity with LD50 values of 3.25 (µg/adult) in the contact test. This work may provide toxicity evidence of seven common herbs against red flour beetles, add the information for the development and comprehensive utilization of A. lancea, and will contribute to the application of grain preservation.
Subject(s)
Atractylodes/chemistry , Drugs, Chinese Herbal/chemistry , Insecticides , Tribolium , Animals , Gas Chromatography-Mass Spectrometry , Insect Repellents/chemistry , Insect Repellents/isolation & purification , Insecticides/chemistry , Insecticides/isolation & purification , Oils, Volatile , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purificationABSTRACT
The extract from Cinnamomum cassia Presl bark was obtained with supercritical CO2 fluid extraction (SFE). Chemical components of the SFE extract were characterized by GC-MS spectrometry. The repellency and contact toxicity of the SFE extract were evaluated against the adults of Tribolium castaneum and Lasioderma serricorne along with those of its two main compounds. The results of GC-MS analysis indicated that 33 volatile constituents were identified from the extract. The main components included trans-cinnamaldehyde (32.1%), 3,3-dimethylhexane (10.6%) and 2,4-di-tert-butylphenol (7.9%). Testing results showed that the SFE extract had potent contact toxicity against T. castaneum and L. serricorne with LD50 values of 3.96 and 23.89 µg/adult, respectively. LD50 values of trans-cinnamaldehyde against T. castaneum and L. serricorne were 5.78 and 3.24 µg/adult, respectively. Additionally, percentage repellency values of the SFE extract and trans-cinnamaldehyde against T. castaneum and L. serricorne were rather high (PR = 100% and PR > 90%, respectively) at 78.63 and 15.73 nL/cm2 at 2 h post-exposure. 2,4-Di-tert-butylphenol showed some repellency against both beetle species. Considering its insecticidal and repellent effects, the SFE extract from C. cassia bark might be used in integrated pest management programs for T. castaneum and L. serricorne.
Subject(s)
Cinnamomum aromaticum/chemistry , Insect Repellents/analysis , Insecticides/analysis , Tribolium , Animals , Carbon Dioxide , Chromatography, Supercritical Fluid , Gas Chromatography-Mass Spectrometry , Plant Bark/chemistry , Plant Extracts/chemistryABSTRACT
The major chemical constituents of the essential oil extracted from Artemisia dubia wall. ex Bess. (Family: Asteraceae) were found as terpinolene (19.02%), limonene (17.40%), 2,5-etheno[4.2.2]propella-3,7,9-triene (11.29%), isoelemicin (11.05%) and p-cymene-8-ol (5.93%). Terpinolene and limonene were separated as main components from the essential oil. The essential oil showed fumigant toxicity against Tribolium castaneum and Liposcelis bostrychophila with LC50 values of 49.54 and 0.74 mg/L, respectively. The essential oil and isolated compounds of A. dubia showed repellency activities against both insects. Terpinolene and limonene showed the fumigant toxicity against T. castaneum. Terpinolene showed obvious fumigant toxicity against L. bostrychophila. The results indicated that the essential oil of A. dubia had potential to be developed into natural insecticides for controlling stored product pests.
Subject(s)
Artemisia/chemistry , Insect Repellents/pharmacology , Oils, Volatile/chemistry , Phthiraptera/drug effects , Tribolium/drug effects , Animals , Cyclohexane Monoterpenes , Cyclohexenes/pharmacology , Food Storage , Insect Control/methods , Insect Repellents/chemistry , Limonene , Terpenes/pharmacologyABSTRACT
Sixteen compounds were isolated from the leaves and stems of Murrayatetramera Huang. Based on the NMR and MS spectral results, the structures were determined. It was confirmed that the isolated compounds included three new compounds (9, 10 and 13) and one new natural product (8), which were identified asmurratetra A (9), murratetra B (10), murratetra C (13) and [2-(7-methoxy-2-oxochromen-8-yl)-3-methylbut-2-enyl]3-methylbut-2-enoate (8), respectively. Meanwhile, the repellent activity against Tribolium castaneum was investigated for 13 of these isolated compounds. The results showed that the tested compounds had various levels of repellent activity against T. castaneum. Among them, compounds 1 (4(15)-eudesmene-1ß,6α-diol), 11 (isoferulic acid) and 16 (2,3-dihydroxypropyl hexadecanoate) showed fair repellent activity against T. castaneum. They might be considered as potential leading compounds for the development of natural repellents.
Subject(s)
Insect Repellents/chemistry , Insect Repellents/pharmacology , Murraya/chemistry , Plant Extracts/chemistry , Tribolium/drug effects , Animals , Magnetic Resonance Spectroscopy , Molecular StructureABSTRACT
The contact toxicity and repellent activities of the essential oil extracted from the rhizomes of Zingiber zerumbet (L.) Smith (Zingiberaceae) was evaluated against cigarette beetles (Lasioderma serricorne). The essential oil obtained by hydrodistillation was investigated by GC-FID and GC-MS. The main constituents of the essential oil were zerumbone (40.2%), α-caryophyllene (8.6%), humulene epoxide II (7.3%), camphene (5.9%) and fenchene (4.7%). Zerumbone and its analogues totally are accounting for 60.3% of the essential oil. It was found that the essential oil possessed contact toxicity against L. serricorne adults with a LD50 value of 48.3 µg/adult. α-Caryophyllene (LD50 = 13.1 µg/adult) exhibited stronger contact toxicity against L. serricorne than humulene oxide (LD50 = 31.2 µg/adult), ß-caryophyllene (LD50 = 35.5 µg/adult) and zerumbone (LD50 = 42.4 µg/adult). Moreover, α-caryophyllene possessed strong repellent activity (Class IV and V, respectively) against the beetles at 78.63 nL/cm2, after 2 and 4 h treatment. The results indicate that zerumbone and its analogues might be developed into natural insecticides or repellents for control of cigarette beetles, but their bioactivities are affected by their structures.
Subject(s)
Coleoptera , Insect Repellents , Insecticides , Plant Oils , Sesquiterpenes , Animals , Monoterpenes/isolation & purification , Plant Oils/isolation & purification , Sesquiterpenes/isolation & purification , ZingiberaceaeABSTRACT
Purpose To evaluate the prognostic value of the restaging system after neoadjuvant chemotherapy (NACT) in patients with advanced-stage nasopharyngeal carcinoma (NPC). Materials and Methods This study was approved by the clinical research committee and a written informed consent was required before enrolling in the study. Prospectively enrolled were 412 consecutive patients with stage III-IVb NPC treated with NACT followed by concurrent chemotherapy and radiation therapy. Patients were staged before NACT and restaged after NACT. The progression-free survival (PFS) and distant metastasis-free survival (DMFS) were calculated with the Kaplan-Meier method, and differences were compared by using the log-rank test. Results Post-NACT T classification (PFS, P = .001) and N classification (PFS, P < .001; DMFS, P = .001) resulted in better survival curve separations than pre-NACT T classification and N classification. Patients downstaged from N2-N3 to N0-N1 disease had a better prognosis than did patients who continued to have N2-N3 diseases (3-year PFS, 83.8% vs 66.6%, P = .001; 3-year DMFS, 88.0% vs 78.4%, P = .026). Multivariate analysis revealed that post-NACT T classification (hazard ratio [HR] = 1.67; 95% confidence interval [CI]: 1.18, 2.36; P = .003) and post-NACT N classification (HR = 1.54; 95% CI: 1.17, 2.03; P = .002) were independent prognostic factors for PFS; also, post-NACT N classification (HR = 1.48; 95% CI: 1.05, 2.07; P = .025) was an independent prognostic factor for DMFS. Multivariate analysis in patients with N2-N3 disease demonstrated that the N downstaging effects of NACT was the only independent prognostic factor for PFS (HR = 0.48; 95% CI: 0.29, 0.81; P = .006) and DMFS (HR = 0.52; 95% CI: 0.28, 0.97; P = .039). Conclusion The post-NACT stage is more representative of prognosis than the pre-NACT stage in advanced-stage NPC patients, which suggests that major clinical decisions should be based on the post-NACT stage. © RSNA, 2016 Online supplemental material is available for this article.
Subject(s)
Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Magnetic Resonance Imaging/methods , Nasopharyngeal Neoplasms/drug therapy , Nasopharyngeal Neoplasms/pathology , Adult , Aged , Biomarkers, Tumor/analysis , Carcinoma , Chemotherapy, Adjuvant , Cisplatin/administration & dosage , Docetaxel , Female , Fluorouracil/administration & dosage , Humans , Male , Middle Aged , Nasopharyngeal Carcinoma , Nasopharyngeal Neoplasms/radiotherapy , Neoadjuvant Therapy , Neoplasm Staging , Prognosis , Prospective Studies , Radiotherapy, Intensity-Modulated , Survival Rate , Taxoids , Treatment OutcomeABSTRACT
A screening of Chinese medicinal herbs and wild plants for agrochemicals was carried out; the essential oil of Glycosmis lucida leaves was found to possess significant repellent activity against Tribolium castaneum and Liposcelis bostrychophila. It was found that the main components included elixene (19.81%), spathulenol (10.68%), anethole (12.05%), verbenone (10.32%) followed by ß-caryophyllene (6.87%). The essential oil, anethole and verbenone were strongly repellent against T. castaneum (96, 86 and 94%, respectively, at 15.73 nL cm-2) and L. bostrychophila (100, 68 and 72%, respectively, at 31.58 nL cm-2) after a 2h treatment. The results indicate that anethole and verbenone had the potential to be developed as natural repellents for control of stored product insects.
Subject(s)
Insect Repellents/pharmacology , Oils, Volatile/pharmacology , Rutaceae/chemistry , Allylbenzene Derivatives , Animals , Anisoles/pharmacology , Oils, Volatile/analysis , TriboliumABSTRACT
The chemical constituents of the essential oil extracted from Artemisia anethoides and the bioactivities of essential oil against Tribolium castaneum and Lasioderma serricorne were investigated. The main components of the essential oil were 1,8-cineole (36.54%), 2-isopropyl-5-methyl-3-cyclohexen-1-one (10.40%), terpinen-4-ol (8.58%), 2-isopropyltoluene (6.20) and pinocarveol (5.08%). The essential oil of A. anethoides possessed contact and fumigant toxicities against T. castaneum adults (LD50 = 28.80 µg/adult and LC50 = 13.05 mg/L air, respectively) and against L. serricorne (LD50 = 24.03 µg/adult and LD50 = 8.04 mg/L air, respectively). The crude oil showed repellent activity against T. castaneum and L. serricorne. Especially, the percentage repellency of essential oil was same level with DEET (positive control) against T. castaneum. The results indicated that the essential oil of A. anethoides had the potential to be developed as insecticide and repellent for control of T. castaneum and L. serricorne.
Subject(s)
Artemisia/chemistry , Coleoptera/drug effects , Insecticides/isolation & purification , Insecticides/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/pharmacology , Tribolium/drug effects , Animals , Dose-Response Relationship, Drug , Insecticides/chemistry , Oils, Volatile/isolation & purificationABSTRACT
Two essential oil samples were obtained from the pericarp of Zanthoxylum bungeanum with the methods of hydrodistillation (HD) and supercritical fluid CO2 extraction (SFE), their chemical components were identified, and their bioactivities against Lasioderma serricorne adults were evaluated. In the process of testing, the two samples showed significant bioactivities against Lasioderma serricorne adults. For an example, the SFE-sample expressed relatively stronger fumigant toxicity on Lasioderma serricorne adults (LC50 = 3.99 µg/mL air) than that of the HD-sample (LC50 = 12.54 µg/mL air). According to GC-MS analysis, the chemical components between two samples were different. The major chemical components for HD included linalool (25.99%), limonene (19.34%), linalyl anthranilate (12.22%), 4-terpinenol (10.49%), eucalyptol (6.53%) and α-terpineol (5.02%), while for SFE included nonanoic acid (21.43%), γ-terpinene (14.51%), eucalyptol (13.45%), α-terpineol (5.83%) and caryophyllene oxide (5.48%). The results showed that different chemical components result in different bioactivities. This work provides theoretical basis for traditional Chinese concept of antagonistic storage, and it also provides important information for the development and comprehensive utilization of Zanthoxylum bungeanum.
Subject(s)
Coleoptera/drug effects , Insect Repellents , Insecticides , Plant Oils , Zanthoxylum/chemistry , Animals , Chromatography, Supercritical Fluid , Distillation , Fatty Acids/analysis , Fatty Acids/isolation & purification , Gas Chromatography-Mass Spectrometry , Insect Repellents/analysis , Insect Repellents/isolation & purification , Insecticides/analysis , Insecticides/isolation & purification , Monoterpenes/analysis , Monoterpenes/isolation & purification , Plant Oils/analysis , Plant Oils/isolation & purification , Sesquiterpenes/analysis , Sesquiterpenes/isolation & purificationABSTRACT
Maca has been used as a foodstuff and a traditional medicine in the Andean region for over 2,000 years. Recently the neuroprotective effects of maca also arouse interest of researchers. Decrease in mitochondrial function and decline in autophagy signaling may participate in the process of age-related cognitive decline. This study aimed to investigate if maca could improve cognitive function of middle-aged mice and if this effect was associated with improvement of mitochondrial activity and modulation of autophagy signaling in mouse cortex. Fourteen-month-old male ICR mice received maca powder administered by gavage for five weeks. Maca improved cognitive function, motor coordination, and endurance capacity in middle-aged mice, accompanied by increased mitochondrial respiratory function and upregulation of autophagy-related proteins in cortex. Our findings suggest that maca is a newly defined nutritional plant which can improve mitochondrial function and upregulate autophagy-related proteins and may be an effective functional food for slowing down age-related cognitive decline.
ABSTRACT
This study was designed to investigate the effect of Huangqin Tang (HQT) on TLR4/Myd88 pathway and the downstream cytokines in rats with ulcerative colitis (UC) to explore its underlying mechanisms of action. The model of UC rats with cell immunoreactivity was made using a compound method (trinitrobenzene sulfonic acid plus ethanol). Rats were randomly divided into the control group, the model group, the salazosulfapyridine (SASP) group, high, medium and low dose(20, 10, 5 g·kg-1) of HQT groups. After a three-day treatment, production of NO in serum was detected by Griess assay, the levels of interleukin (IL)-4, IL-10, IL-17 and prostaglandin E2ï¼PGE2ï¼ in serum were detected by ELISA. After a five-day treatment, the positive protein expressions of COX-2 and iNOS in the colon tissue were determined by ICH method, the protein expressions of TLR4 and MyD88 in colon tissue were determined by Western blot. Compared with the control group, the levels of NO, IL-17, PGE2, the protein expressions of TLR4, MyD88 and the protein positive expressions of COX-2, iNOS were apparently higher in the model group. Compared with model group, the above indexes were significantly improved in the SASP and high-dose HQT groups (P < 0.05). These results show that HQT has a definite effect on UC in rats. Its mechanisms of action may be achieved by inhibiting the activity of TLR4/MyD88/NF-κB signal pathway and down-regulation of NO, IL-17 and PGE2 production.
Subject(s)
Colitis, Ulcerative/drug therapy , Drugs, Chinese Herbal/pharmacology , Myeloid Differentiation Factor 88/metabolism , Signal Transduction , Toll-Like Receptor 4/metabolism , Animals , Colitis, Ulcerative/chemically induced , Cyclooxygenase 2/metabolism , Cytokines/blood , Dinoprostone/blood , Down-Regulation , NF-kappa B/metabolism , Nitric Oxide Synthase Type II/metabolism , Rats , Rats, Sprague-Dawley , Scutellaria baicalensisABSTRACT
Amomum maximum Roxb. is a perennial herb distributed in South China and Southeast Asia. The objective of this work was to analyze the chemical constituents and assess insecticidal and repellent activities of the essential oil from Amomum maximum fruits against Tribolium castaneum (Herbst) and Liposcelis bostrychophila (Badonnel). The essential oil was obtained by hydrodistillation and analyzed by gas chromatography-flame ionization detector and gas chromatography-mass spectrometry. The main components of the essential oil were identified to be ß-pinene (23.39%), ß-caryophyllene (16.43%), α-pinene (7.55%), sylvestrene (6.61%) and ç-cadinene (4.19%). It was found that the essential oil of A. maximum fruits possessed contact and fumigant toxicities against T. castaneum adults (LD50 = 29.57 µg/adult and LC(50) = 23.09 mg/L air, respectively) and showed contact toxicity against L. bostrychophila (LD(50) = 67.46 µg/cm(2)). Repellency of the crude oil was also evaluated. After 2 h treatment, the essential oil possessed 100% repellency at 78.63 nL/cm(2) against T. castaneum and 84% repellency at 63.17 nL/cm(2) against L. bostrychophila. The results indicated that the essential oil of A. maximum fruits had the potential to be developed as a natural insecticide and repellent for control of T. castaneum and L. bostrychophila.