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1.
J Infect Dis ; 229(1): 117-121, 2024 Jan 12.
Article in English | MEDLINE | ID: mdl-37565805

ABSTRACT

Using a prospective, observational cohort study during the post-"dynamic COVID-zero" wave in China, we estimated short-term relative effectiveness against Omicron BA.5 infection of inhaled aerosolized adenovirus type 5-vectored ancestral strain coronavirus disease 2019 (COVID-19) vaccine as a second booster dose approximately 1 year after homologous boosted primary series of inactivated COVID-19 vaccine compared with no second booster. Participants reported nucleic acid or antigen test results weekly until they tested positive or completed predesignated follow-up. After excluding participants infected <14 days after study entry, relative effectiveness among the 6576 participants was 61% in 18- to 59-year-olds and 38% in ≥60-year-olds and was sustained for 12 weeks.


Subject(s)
COVID-19 Vaccines , COVID-19 , Humans , COVID-19/prevention & control , Prospective Studies , Vaccine Efficacy , China/epidemiology , Adenoviridae/genetics
2.
Biomater Sci ; 12(2): 425-439, 2024 Jan 16.
Article in English | MEDLINE | ID: mdl-38050470

ABSTRACT

In this work, we successfully constructed Mn-coordinated nitrogen-carbon nanoparticles (Mn-N-C NPs) exhibiting multienzyme-like activities. In a bacterial infectious microenvironment, the POD-like and OXD-like activities of Mn-N-C NPs could synergistically trigger the generation of ROS (˙OH and O2˙-), causing oxidative damage to the bacterial cell membrane for killing bacteria. Alternatively, in neutral or weak alkaline normal tissues, the excessive O2˙- could be converted into O2 and H2O2via the SOD-like ability of Mn-N-C NPs, and subsequently their CAT-like activity catalyzed excess H2O2 into H2O and O2 for protecting normal cells through the antioxidant defense. Mn-N-C NPs also possessed a good NIR-photothermal performance, which could enhance their POD-like and OXD-like activities. Furthermore, Mn-N-C NPs could facilitate the GSH oxidation process and disrupt the intrinsic balance in the bacterial protection microenvironment with the assistance of H2O2, which is beneficial for rapid bacterial death. Undoubtedly, the Mn-N-C NPs + H2O2 system showed the highest antibacterial activity when irradiated with an 808 nm laser, destroying the bacterial membrane and causing the efflux of proteins. Moreover, the Mn-N-C NPs + H2O2 system was immune to the development of bacterial resistance and could efficiently disrupt the formation of a bacterial biofilm with negligible cytotoxicity and low hemolysis ratio. Finally, Mn-N-C NPs exhibited an excellent antibacterial performance in vivo and could accelerate wound healing without cellular inflammation production. Therefore, due to their significant therapeutic effects, Mn-N-C NPs show great potential in fighting antibiotic-resistant bacteria.


Subject(s)
Bacterial Infections , Nanoparticles , Humans , Hydrogen Peroxide , Antioxidants , Bacterial Infections/drug therapy , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/therapeutic use
3.
J Nat Prod ; 86(11): 2468-2473, 2023 11 24.
Article in English | MEDLINE | ID: mdl-37939268

ABSTRACT

Three unusual sesterterpenoids featuring unprecedented rearranged colquhounane (C25) and tetranorcolquhounane (C21) frameworks, colquhounoids E (1) and F (3) and norcolquhounoid F (2), were isolated from a Lamiaceae medicinal plant Colquhounia coccinea var. mollis. Their structures were elucidated by spectroscopic analysis and quantum chemical calculations. A biomimetic inspired regioselective cyclopropane cleavage was achieved under acidic conditions. The immunosuppressive activities of these new sesterterpenoids were also evaluated.


Subject(s)
Lamiaceae , Plants, Medicinal , Spectrum Analysis , Lamiaceae/chemistry , Molecular Structure
4.
Nat Prod Res ; : 1-9, 2023 Aug 23.
Article in English | MEDLINE | ID: mdl-37610159

ABSTRACT

One new labdane diterpenoid, tricuspion A (1), as well as five known triterpenoids (2-6) were isolated from Salvia tricuspis Franch (family Labiatae). The structure of tricuspion A was identified by extensive spectroscopic analysis and by comparison with previously reported data. Compounds 1-6 were evaluated for their inhibitory effects on the NO production in LPS-stimulated BV-2 microglia cells, and 1 exhibited potent inhibitory activity with IC50 value of 14.92 ± 0.51 µM. Compound 1 might exert anti-neuroinflammatory activity through inhibiting the excessive production of NO and down-regulating the protein expression of iNOS and COX-2. As such, labdane diterpenoid (tricuspion A) could provide promising anti-neuroinflammatory lead compound for further structural modification.

5.
Inquiry ; 60: 469580231182040, 2023.
Article in English | MEDLINE | ID: mdl-37357725

ABSTRACT

The composition of influenza vaccines is updated annually. To ensure vaccine safety, the coverage and adverse events following immunization (AEFI) of 6 manufacturers of trivalent inactivated influenza vaccine (TIV3) need to be evaluated. In January 2022, we analyzed data from more than 1.59 million children in the Childhood Vaccination Information Management System and the AEFI Surveillance Information Management System and evaluated influenza vaccines for children aged 6 to 35 months in Guangzhou from 2016/17 to 2019/20 Vaccination rates and AEFI reporting rates. From 2016/17 to 2019/20, the 1-dose influenza vaccination rate was 25.0% (range: 20.7%-30.2%), and the 2-dose (full course) influenza vaccination rate was 21.6% (range: 17.7%-26.4%). The full vaccination coverage rate has trended down since 2017/2018 (2017/18: 26.0%; 2018/19: 8.3; 2019/20: 17.7%). Fifty-two cases (13.1/100 000) and 24 cases (6.9/100 000) received AEFI reports for 1 dose and 2 doses, respectively, mainly due to fever ≥38.6°C (39 cases for 1 dose, 9.8/100 000; 15 cases for 2 dose, 4.3/100 000) and allergic rash (9 cases with 1 dose, 2.3/100 000; 5 cases with 2 doses, 1.4/100 000). Patients who received A and F manufacturers were more likely to report side effects. The safety of influenza vaccines from 6 manufacturers is good, and it is necessary to improve the recommended information on influenza vaccines to dispel people's concerns and increase the vaccination rate.


Subject(s)
Exanthema , Influenza Vaccines , Influenza, Human , Vaccination Coverage , Vaccines, Inactivated , Child , Humans , Infant , Exanthema/chemically induced , Immunization , Influenza Vaccines/adverse effects , Influenza, Human/prevention & control , Influenza, Human/epidemiology , Vaccination , Vaccines, Inactivated/adverse effects
6.
J Ethnopharmacol ; 315: 116653, 2023 Oct 28.
Article in English | MEDLINE | ID: mdl-37236383

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Caesalpinia minax Hance, whose seeds are known as "Ku-shi-lian" in China, have been used in Chinese folk medicine for treatment of rheumatism, dysentery, and skin itching. However, the anti-neuroinflammatory constituents of its leaves and their mechanism are rarely reported. AIM OF THE STUDY: To search for new anti-neuro-inflammatory compounds from the leaves of C. minax and elucidate their mechanism on anti-neuroinflammatory effect. MATERIALS AND METHODS: The main metabolites of the ethyl acetate fraction from C. minax were analyzed and purified via HPLC and various column chromatography techniques. Their structures were elucidated on the basis of 1D and 2D NMR, HR-ESI-MS, and single crystal X-ray diffraction analysis. Anti-neuroinflammatory activity was evaluated in BV-2 microglia cells induced by LPS. The expression levels of molecules in NF-κB and MAPK signaling pathways were analyzed through western blotting. Meanwhile, the time- and dose-dependent expression of associated proteins such as iNOS and COX-2 were detected by western blotting. Furthermore, Compounds 1 and 3 were performed on the NF-κB p65 active site using molecular docking simulation to elucidate the molecular level inhibition mechanism. RESULTS: 20 cassane diterpenoids, including two novel ones (caeminaxins A and B) were isolated from the leaves of C. minax Hance. Caeminaxins A and B possessed a rare unsaturated carbonyl moiety in their structures. Most of the metabolites exhibited potent inhibition effects with IC50 values ranging from 10.86 ± 0.82 to 32.55 ± 0.47 µM. Among them, caeminaxin A inhibited seriously the expression of iNOS and COX-2 proteins and restrained the phosphorylation of MAPK and the activation of NF-κB signaling pathways in BV-2 cells. The anti-neuro-inflammatory mechanism of caeminaxin A has been studied systematically for the first time. Furthermore, biosynthesis pathways for compounds 1-20 were discussed. CONCLUSIONS: The new cassane diterpenoid, caeminaxin A, alleviated the expression of iNOS and COX-2 protein and down-regulated of intracellular MAPK and NF-κB signaling pathways. The results implied that cassane diterpenoids had potential to be developed into therapeutic agents for neurodegenerative disorders such as Alzheimer's disease.


Subject(s)
Caesalpinia , Diterpenes , NF-kappa B/metabolism , Caesalpinia/chemistry , Microglia/metabolism , Cyclooxygenase 2 , Molecular Docking Simulation , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Plant Leaves/metabolism , Diterpenes/pharmacology , Diterpenes/therapeutic use , Diterpenes/chemistry , Lipopolysaccharides/pharmacology
7.
Phytochemistry ; 212: 113710, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37178942

ABSTRACT

Six undescribed C27-phytoecdysteroid derivatives, named superecdysones A-F, and ten known analogs were extracted from the whole plant of Dianthus superbus L. Their structures were identified by extensive spectroscopy, mass spectrometric methods, chemical transformations, chiral HPLC analysis, and the single-crystal X-ray diffraction analysis. Superecdysones A and B possess a tetrahydrofuran ring in the side chain and superecdysones C-E are rare phytoecdysones containing a (R)-lactic acid moiety, whereas superecdysone F is an uncommon B-ring-modified ecdysone. Notably, based on the variable temperature (from 333 K to 253 K) NMR experiments of superecdysone C, the missing carbon signals were visible at 253 K and assigned. The neuroinflammatory bioassay of all compounds were evaluated, and 22-acetyl-2-deoxyecdysone, 2-deoxy-20-hydroxyecdysone, 20-hydroxyecdysone, ecdysterone-22-O-benzoate, 20-hydroxyecdysone-20,22-O-R-ethylidene, and acetonide derivative 20-hydroxyecdysterone-20, 22-acetonide significantly suppressed the LPS-induced nitric oxide generation in microglia cells (BV-2), with IC50 values ranging from 6.9 to 23.0 µM. Structure-activity relationships were also discussed. Molecular docking simulations of the active compounds confirmed the possible mechanism of action against neuroinflammations. Furthermore, none compounds showed cytotoxicity against HepG2 and MCF-7. It is the first report about the occurrence and anti-neuroinflammatory activity of the phytoecdysteroids in the genus Dianthus. Our findings demonstrated that ecdysteroids may be used as potential anti-inflammatory drugs.


Subject(s)
Dianthus , Dianthus/chemistry , Ecdysterone/pharmacology , Molecular Docking Simulation , Neuroinflammatory Diseases , Ecdysteroids/pharmacology
8.
Pest Manag Sci ; 79(7): 2539-2555, 2023 Jul.
Article in English | MEDLINE | ID: mdl-36864521

ABSTRACT

BACKGROUND: Natural products play a significant role in the development of novel bactericide candidates. Caesalpinia pulcherrima, a traditional medicine, had anti-inflammatory, antimicrobial, and antifeedant activities, therefore the previous bioassay results of C. pulcherrima implied that its main active ingredients may have potential to be used as botanical bactericides. RESULTS: Bio-guided isolation of C. pulcherrima was conducted to obtain 11 novel cassane diterpenoids (capulchemins A-K) and 10 known sesquiterpenes. Their structures were established by extensive spectroscopic methods and single-crystal X-ray diffraction analyses. Capulchemins A-F possess a rare aromatic C ring, while capulchemin K with a 15,16-degradative carbon skeleton represents a rare group of cassane diterpenes. Capulchemin A exhibited remarkable antibacterial activity against four phytopathogenic bacteria, particularly against Pseudomonas syringae pv. actinidae and Bacillus cereus, with minimal inhibitory concentration values of 3.13 µM. Meanwhile, capulchemin A showed significant control effect on kiwifruit canker in vivo. Further investigation of its mechanism of antibacterial activity revealed that compound 1 was closely related to destroy cell membrane to cause cell death. Additionally, some of those cassane diterpenoids showed potential antifeedant against Mythimna separate walker and Plutella xylostella. Consequently, capulchemin A could have the potential to be used as a template for the development for new eco-friendly NP-based bactericides. CONCLUSION: These data contribute to a better understanding of the antibacterial activity of cassane diterpenes. Cassane diterpenes have been discovered to be leading to broad application prospects in the development as novel botanical bactericides. © 2023 Society of Chemical Industry.


Subject(s)
Anti-Bacterial Agents , Caesalpinia , Diterpenes , Plant Extracts , Animals , Anti-Bacterial Agents/pharmacology , Caesalpinia/chemistry , Diterpenes/pharmacology , Diterpenes/chemistry , Microbial Sensitivity Tests , Molecular Structure , Moths , Seeds/chemistry , Plant Extracts/pharmacology
9.
Phytochemistry ; 206: 113531, 2023 Feb.
Article in English | MEDLINE | ID: mdl-36464100

ABSTRACT

Eleven undescribed diterpenoids possessing labdane, 3,18-cyclo-labdane, 19 (4 â†’ 3)-labdane and 12-nor-labdane skeletons, named leucolactones A-K, were isolated from the heartwood of a large woody Lamiaceae plant, Leucosceptrum canum. Their structures were determined by NMR, MS, and in the case of leucolactones A by single crystal X-ray diffraction analysis. Plausible biosynthetic pathway of leucolactones were proposed. Leucolactones showed significant inhibitory effects against seed germination and root elongation of Arabidopsis thaliana in the Petri dish bioassay. Among them, the diastereomeric leucolactones G and H were the most potent, with EC50 values for root elongation of 6.53 ± 1.35 and 9.75 ± 1.25 µM, respectively. The preliminary structure-activity relationship of leucolactones was discussed. The increase of auxin reporter activity in A. thaliana DR5::GUS roots by leucolactone H was observed, indicating that leucolactones altered auxin accumulation and distribution. These findings suggested that leucolactones might be involved in regulation of plant growth and development through altering auxin accumulation and distribution, presumably contributing to the heartwood formation in L. canum.


Subject(s)
Arabidopsis Proteins , Arabidopsis , Diterpenes , Lamiaceae , Arabidopsis/metabolism , Germination , Seeds/metabolism , Diterpenes/pharmacology , Diterpenes/metabolism , Lamiaceae/chemistry , Indoleacetic Acids/metabolism , Plant Roots/metabolism , Arabidopsis Proteins/metabolism
10.
Int J Mol Sci ; 23(21)2022 Oct 28.
Article in English | MEDLINE | ID: mdl-36361922

ABSTRACT

AtDjC5 belongs to the J-protein family in Arabidopsis thaliana. Its biological functions remain unclear. In this study, we examined the roles of AtDjC5 in resisting heat stress using reverse genetic analysis. After the seedlings were exposed directly to 44 °C for 90 min, AtDjC5 knockout seedlings displayed decreases in the survival rate, membrane system stability, and cell vitality compared to WT seedlings, indicating that AtDjC5 is involved in plant basal thermotolerance. The AtDjC5 knockout seedlings pre-exposed to 37 °C for 30 min exhibited decreases in the survival rate and total chlorophyll contents and increased cell death when they were subsequently exposed to 45 °C compared to the WT seedlings, indicating that AtDjC5 plays an important role in plant acquired thermotolerance. AtDjC5 was found to localize to the endoplasmic reticulum. The expression of the AtDjC5 gene was induced by heat and TM (an ER stress inducer) treatment. Furthermore, we found that the knockout of AtDjC5 inhibited ER stress-induced autophagy and the expression of ER stress-related genes. Taken together, these results suggest that AtDjC5 facilitates thermotolerance, likely by aiding in the ER stress response.


Subject(s)
Arabidopsis Proteins , Arabidopsis , Thermotolerance , Arabidopsis/metabolism , Thermotolerance/genetics , Arabidopsis Proteins/genetics , Arabidopsis Proteins/metabolism , Seedlings/metabolism , Heat-Shock Response/genetics , Gene Expression Regulation, Plant
12.
Phytochemistry ; 196: 113082, 2022 Apr.
Article in English | MEDLINE | ID: mdl-35051786

ABSTRACT

Sixteen cassane diterpenoids (CAs), including four undescribed lactam-type, four unreported lactone-type, along with eight known ones, were isolated from the aerial parts of Caesalpinia pulcherrima (L.) Sw. Their structures were characterized by comprehensive spectroscopic analyses (including NMR and HRESIMS). The absolute configuration of pulcherritam A was finally established by single-crystal X-ray diffraction with Cu Kα radiation. Notably, pulcherritam s A-D were elucidated as a group of rare CAs bearing an α, ß-unsaturated γ-lactam ring rather than a typical lactone moiety. Almost all compounds were examined for their antibacterial. The results reveal that pulcherritam H exhibited significant antibacterial activities against Bacillus cereus, Staphylococcus aureus, as well as Pseudomonas syringae pv. actinidae (Psa) with the MIC from 6.25 to 12.5 µM, while pulcherritams A and C displayed potent antibacterial activities against methicillin-resistant Staphylococcus aureus (MRSA). Then, all isolates were evaluated for their anti-glioblastoma activities. Pulcherritam A and Pulcherrimin G illustrated moderate inhibitory activity against glioblastoma multiforme (GBM) U87MG cell, and the other compounds did not show obvious inhibitory activity against GBM U87MG cell. Furthermore, the preliminary structure-activity relationship and their biosynthetic pathway were also discussed.


Subject(s)
Caesalpinia , Diterpenes , Glioblastoma , Methicillin-Resistant Staphylococcus aureus , Anti-Bacterial Agents/pharmacology , Caesalpinia/chemistry , Diterpenes/chemistry , Molecular Structure , Plant Components, Aerial
13.
Neoplasma ; 69(1): 49-58, 2022 Jan.
Article in English | MEDLINE | ID: mdl-34881626

ABSTRACT

The small nucleolar RNA host gene 16 (SNHG16) has recently been shown to be a putative oncogene in gastric cancer (GC) and other cancer types, but how its four lncRNA variants are expressed in any physiological and pathological situation remains unknown. To investigate the expression and function of the four lncRNA variants of SNHG16, mainly the variant 1, in GC, we performed quantitative PCR to determine the RNA levels of the four variants in 60 GC tissue samples and several cell lines. We also studied how knocking down of SNHG16 with siRNA affected proliferation, apoptosis, cell cycle progression, as well as migration and invasion of GC cells. Our results showed that variants 1 and 4 were overexpressed in GC tissues compared with adjacent uninvolved tissues. Knockdown of the four variants, mainly the variant 1, enhanced apoptosis and inhibited cell cycle progression of a GC cell line by arresting the cells at the G1 phase. These cellular effects were associated not only with decreased protein levels of c-Myc, PCNA, cyclins D1, E1, A2 and B, as well as CDKs 2 and 6, but also with increased protein levels of the p21, p27 and p53. Knockdown of total SNHG16 lncRNAs also inhibited invasion and migration of the GC cells in vitro. These results collectively suggest that SNHG16 may be oncogenic in GC by regulating cell cycle progression and may serve as a GC biomarker.


Subject(s)
MicroRNAs , RNA, Long Noncoding , Stomach Neoplasms , Cell Cycle/genetics , Cell Line, Tumor , Cell Movement/genetics , Cell Proliferation/genetics , Gene Expression Regulation, Neoplastic , Humans , Oncogenes/genetics , RNA, Long Noncoding/genetics , Stomach Neoplasms/genetics
14.
Nat Prod Res ; 36(18): 4636-4644, 2022 Sep.
Article in English | MEDLINE | ID: mdl-34842014

ABSTRACT

Three undescribed cassane-type diterpenoids (CAs), caesalpulcherrins K-M (1-3), together with three known ones (4-6) were isolated from the aerial parts of Caesalpinia pulcherrima (L.) Sw (Fabaceae). Their structures were elucidated via analysis of NMR (1 D and 2 D) and HRESIMS data. The character for caesalpulcherrin K possessing the olefin bond at C-11 and C-12 in its cassane skeleton was observed, which belonged to a small group among more than 450 CAs. That is, only fifteen derivatives have been reported up to now, to our knowledge. Biological evaluation revealed that compounds 1-6 exhibited moderate anti-inflammatory activity, with an IC50 value from 6.04 ± 0.34 to 8.92 ± 0.65 µM. Furthermore, compounds 5 and 6 exhibited significant α-glucosidase inhibitory activity at 10 µM.


Subject(s)
Caesalpinia , Diterpenes , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/pharmacology , Caesalpinia/chemistry , Diterpenes/chemistry , Glycoside Hydrolases , Molecular Structure , Seeds/chemistry
15.
Emerg Microbes Infect ; 10(1): 1751-1759, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34396940

ABSTRACT

The effectiveness of inactivated SARS-CoV-2 vaccines against the Delta variant, which has been associated with greater transmissibility and virulence, remains unclear. We conducted a test-negative case-control study to explore the vaccine effectiveness (VE) in real-world settings. We recruited participants aged 18-59 years who consisted of SARS-CoV-2 test-positive cases (n = 74) and test-negative controls (n = 292) during the outbreak of the Delta variant in May 2021 in Guangzhou city, China. Vaccination status was compared to estimate The VE of SARS-CoV-2 inactivated vaccines. A single dose of inactivated SARS-CoV-2 vaccine yielded the VE of only 13.8%. After adjusting for age and sex, the overall VE for two-dose vaccination was 59.0% (95% confidence interval: 16.0% to 81.6%) against coronavirus disease 2019 (COVID-19) and 70.2% (95% confidence interval: 29.6-89.3%) against moderate COVID-19 and 100% against severe COVID-19 which might be overestimated due to the small sample size. The VE of two-dose vaccination against COVID-19 reached 72.5% among participants aged 40-59 years, and was higher in females than in males against COVID-19 and moderate diseases. While single dose vaccination was not sufficiently protective, the two-dose dosing scheme of the inactivated vaccines was effective against the Delta variant infection in real-world settings, with the estimated efficacy exceeding the World Health Organization minimal threshold of 50%.


Subject(s)
COVID-19 Vaccines/standards , COVID-19/prevention & control , SARS-CoV-2/genetics , Adolescent , Adult , Age Distribution , COVID-19/classification , COVID-19 Vaccines/administration & dosage , Case-Control Studies , China , Disease Outbreaks , Female , Genetic Variation , Humans , Male , Middle Aged , Vaccines, Inactivated/administration & dosage , Vaccines, Inactivated/standards , Young Adult
16.
Expert Rev Vaccines ; 20(7): 907-918, 2021 07.
Article in English | MEDLINE | ID: mdl-34036862

ABSTRACT

Background: Since 2016, China has approved the use of inactivated enterovirus 71 (EV71) vaccines produced by three manufacturers. The coverage and safety of different EV71 vaccines need to be evaluated.Research design and methods: The EV71 vaccination and AEFI data were collected from the Guangzhou Children's Vaccination Information Report Management System and the China AEFI Monitoring Information Management System, and the EV71 vaccine coverage rate and the AEFI incidence rate were analyzed.Results: From 2016 to 2019, the number of people who should have been vaccinated in Guangzhou was 2,781,618, and the coverage rates for doses 1 and 2 were 24.71% and 19.44%, respectively. The inoculation rates of vaccines from manufacturers A and B were between 3.03 and 10.46%. The reported incidence of AEFIs was 11.97 per 100,000 (147 cases), with fever (106 cases, 8.63 per 100,000) and allergic rash (59 cases, 4.80 per 100,000) being the most common reactions. There were no differences in the AEFI responses to the EV71 vaccines from the three manufacturers.Conclusion: The EV71 vaccines from the three manufacturers have good safety, but the EV71 vaccine coverage rate is low. It is recommended that vaccine publicity be strengthened and that the vaccine coverage rate in children be increased.


Subject(s)
Enterovirus A, Human , Enterovirus , Child , Humans , Immunization , Vaccination , Vaccines, Inactivated/adverse effects
17.
J Org Chem ; 86(16): 11169-11176, 2021 08 20.
Article in English | MEDLINE | ID: mdl-33826334

ABSTRACT

A pair of new C-14 epimeric sesterterpenoids, colquhounoid D (1) and 14-epi-colquhounoid D (2), and five degradation products featuring new C20 and C21 frameworks, norcolquhounoids A-E (3-7), were isolated from Colquhounia coccinea var. mollis. Their structures were elucidated by comprehensive spectroscopic analysis and single-crystal X-ray diffraction. Degradation of the C25 skeleton to the C21 skeleton was also achieved using aqueous NaIO4 and RuCl3. Compounds 1 and 2 showed significant immunosuppressive activity on the cytokine IFN-γ secretion of mouse splenocytes induced by anti-CD3/CD4 monoclonal antibodies, with IC50 of 8.38 and 5.79 µM, respectively, and compounds 5 and 6 were moderately active.


Subject(s)
Molecular Structure , Animals , Crystallography, X-Ray , Mice , Spectrum Analysis
18.
J Agric Food Chem ; 68(14): 4227-4236, 2020 Apr 08.
Article in English | MEDLINE | ID: mdl-32191454

ABSTRACT

Ten new cassane diterpenoids, caesalpulcherrins A-J (1-10), together with 11 known analogues (11-21) were isolated from the aerial parts of Caesalpinia pulcherrima. Their structures and relative stereochemistry were elucidated by spectrometric and spectroscopic methods, including one-dimensional (1D) and two-dimensional (2D) NMR, high-resolution electrospray ionization mass spectrometry (HRESIMS), and single-crystal X-ray diffraction analysis. Compounds 1-4 represent the first examples of 2,5-dimethoxyfuranocassane diterpenoids. Results of the antifeedant activity indicated that isovouacapenol C (12) and pulcherrin N (14) exhibited remarkable antifeedant activity against Mythimna separate with EC50 values of 3.43 and 4.20 µg/cm2, respectively. Meanwhile, pulcherrimin C (13) and 12-demethyl neocaesalpin F (18) exerted significant antifeedant activity against Plutella xylostella with an EC50 data of 4.00 and 3.05 µg/cm2, respectively. Some of the compounds showed obvious toxic activity against the plant-feeding generalist insect herbivores, M. separate and P. xylostella, at 0.8 mg/mL (800 ppm). Furthermore, the structure-activity relationships of antifeedant and insecticidal activities are also discussed in the article.


Subject(s)
Caesalpinia/chemistry , Diterpenes/chemistry , Insecticides/chemistry , Plant Components, Aerial/chemistry , Plant Extracts/chemistry , Amino Acids, Sulfur/chemistry , Amino Acids, Sulfur/pharmacology , Animals , Crystallography, X-Ray , Diterpenes/pharmacology , Drug Evaluation, Preclinical , Insecticides/pharmacology , Magnetic Resonance Spectroscopy , Molecular Structure , Moths , Piperidines/chemistry , Piperidines/pharmacology , Plant Extracts/pharmacology , Spectrometry, Mass, Electrospray Ionization , Structure-Activity Relationship
19.
Int J Surg Case Rep ; 68: 151-153, 2020.
Article in English | MEDLINE | ID: mdl-32146428

ABSTRACT

INTRODUCTION: Bladder stone is a rare and ancient disease. Nowadays new technologies have been developed in the effort to make less invasive stone treatment. Bladder calculi account for 5% of urinary calculi. PRESENTATION OF CASE: A 52-year-old male patient with symptoms of lower abdominal pain, dysuria and pollakiuria was admitted. Urinalysis showed that pH5.0 and presence of calcium oxalate crystals and leukocyturia but erthrocyturia and nitrite were absent. Abdominal ultrasonogry revealed hydronephrosis, thickened bladder wall and large single stone. Plain radiography showed a large bladder stone measuring 12 × 10 cm. DISCUSSION: In our case 1 extremely large bladder calculus occupied most of the bladder and pressing on the orifices of the ureters, leading to the presence of hydronephrosis. For large-sized bladder stones, all the reports have recommended open cystolithotomy. CONCLUSION: The combination of improved nutrition and modern antibiotic treatment has to be led to the frequency of bladder lithiasis. Calcium intake shouldn't be restricted, whereas oxalate, sodium, and protein intakes have to be limited.

20.
Phytochemistry ; 172: 112285, 2020 Apr.
Article in English | MEDLINE | ID: mdl-32035325

ABSTRACT

Plant glandular trichomes (GTs) are adaptive epidermal structures that synthesize and accumulate diverse specialized metabolites well-known as defense chemicals against biotic attacks, but their roles against abiotic challenges including UV radiation and cold climates remain largely unexplored. Colquhounia vestita Wall is a Chinese-Himalayan Lamiaceae plant with dense peltate and capitate GTs on its leaf and stem surfaces under a scanning electron microscope. Three diterpenoid acids, including a clerodane 5-epi-hardwickiic acid and two labdanes polyalthic acid and E-communic acid, were identified from the peltate GTs of C. vestita through laser microdissection coupled with UPLC-MS/MS. Under UV radiation and cold stresses, the major GT component polyalthic acid increased the biomass of Arabidopsis thaliana seedlings and decreased their malondialdehyde content. Furthermore, polyalthic acid promoted photosynthetic efficiency and the expression of genes encoding peroxidative enzymes under UV radiation, and stimulated Ca2+ elevation and the expression of calmodulin binding transcription activator gene CAMTA3 and two downstream cold-responsive genes CBF3 and RD29A under cold stress. Therefore, polyalthic acid in GTs is likely to endow the plant with enhanced tolerance to UV radiation and cold stresses, which extends the current understanding of the function of GT compounds in plant adaptation to abiotic environments.


Subject(s)
Lamiaceae , Trichomes , Chromatography, Liquid , Cold-Shock Response , Gene Expression Regulation, Plant , Tandem Mass Spectrometry , Ultraviolet Rays
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