ABSTRACT
A new steroid, 2a-oxa-2-oxo-5ß-hydroxy-3,4-dinor-24-methylcholesta-22E-ene (1), together with 10 known ones (2-11), was isolated from the marine sponge Cliona sp. The structures of these compounds were determined by the spectroscopic methods (UV, IR, MS, and NMR) and X-ray diffraction analysis. Compound 1 was the third example of 3,4-dinorsteroid with a hemiketal at C-5 that was isolated from the natural source. In addition, the antibacterial activities of these compounds were also evaluated. However, none of them exhibited significant inhibition effects.
Subject(s)
Anti-Bacterial Agents , Marine Biology , Porifera , Animals , Porifera/chemistry , Molecular Structure , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Microbial Sensitivity Tests , Nuclear Magnetic Resonance, Biomolecular , Steroids/chemistry , Steroids/pharmacology , Steroids/isolation & purification , Crystallography, X-RayABSTRACT
A chemical investigation on the marine sponge Dysidea sp. resulted in the isolation of a series of diketopiperazines, including two new compounds, dysidines A (1) and B (2) as well as six known ones (3-8). Their structures with absolute configurations were determined on the basis of UV, IR, HRMS, NMR and calculated ECD method. Additionally, the cytotoxic, anti-inflammatory, antibacterial and antiviral activities of 1-8 were also tested. However, none of them exhibited significant bioactivities.
ABSTRACT
Stroke is the most devastating disease, causing paralysis and eventually death. Many clinical and experimental trials have been done in search of a new safe and efficient medicine; nevertheless, scientists have yet to discover successful remedies that are also free of adverse effects. This is owing to the variability in intensity, localization, medication routes, and each patient's immune system reaction. HIF-1α represents the modern tool employed to treat stroke diseases due to its functions: downstream genes such as glucose metabolism, angiogenesis, erythropoiesis, and cell survival. Its role can be achieved via two downstream EPO and VEGF strongly related to apoptosis and antioxidant processes. Recently, scientists paid more attention to drugs dealing with the HIF-1 pathway. This review focuses on medicines used for ischemia treatment and their potential HIF-1α pathways. Furthermore, we discussed the interaction between HIF-1α and other biological pathways such as oxidative stress; however, a spotlight has been focused on certain potential signalling contributed to the HIF-1α pathway. HIF-1α is an essential regulator of oxygen balance within cells which affects and controls the expression of thousands of genes related to sustaining homeostasis as oxygen levels fluctuate. HIF-1α's role in ischemic stroke strongly depends on the duration and severity of brain damage after onset. HIF-1α remains difficult to investigate, particularly in ischemic stroke, due to alterations in the acute and chronic phases of the disease, as well as discrepancies between the penumbra and ischemic core. This review emphasizes these contrasts and analyzes the future of this intriguing and demanding field.
Subject(s)
Hypoxia-Inducible Factor 1, alpha Subunit , Ischemic Stroke , Humans , Ischemic Stroke/metabolism , Hypoxia-Inducible Factor 1, alpha Subunit/metabolism , Animals , Signal Transduction/physiology , Oxidative Stress/physiology , Brain Ischemia/metabolismABSTRACT
(+)- and (-)-Tedanine [(+)-1 and (-)-1], a pair of new enantiomeric indolone alkaloids, along with nine compounds (2-10) were isolated from the marine sponge Tedania sp. The structures of (+)-1 and (-)-1 including absolute configurations were determined by spectroscopic analysis and quantum chemical calculation. Compounds (+)-1 and (-)-1 were the first examples of indolone alkaloids isolated from this genus. In addition, the cytotoxic and antibacterial activities of these compounds were also evaluated.
Subject(s)
Alkaloids , Antineoplastic Agents , Porifera , Animals , Porifera/chemistry , Alkaloids/chemistry , Anti-Bacterial Agents/chemistry , Antineoplastic Agents/chemistry , Molecular StructureABSTRACT
Two new pairs of enantiomeric butenolides, (+)- and (-)-suberiteslide A, (+)- and (-)-subertieslide B had been obtained from the marine sponge Suberties sp. The structures with absolute configurations of these compounds were unequivocally determined by spectroscopic analyses and ECD (Electronic Circular Dichroism) method. It was the first separation of butenolides from the marine sponges of genus Suberites. Additionally, the anti-inflammatory, antibacterial and cytotoxic activities of these compounds were evaluated. The result indicated that only (-)-subertieslide B showed weak anti-inflammatory activity with the IC50 value of 40.8â µM.
Subject(s)
Porifera , Animals , Porifera/microbiology , 4-Butyrolactone/chemistry , Anti-Bacterial Agents/pharmacology , Circular Dichroism , Molecular StructureABSTRACT
Two new alkaloids, spongimides A (1) and B (2), along with five known ones (3-7), were isolated from the marine sponge Spongia sp. The structures of 1 and 2 were determined by the spectroscopic methods (UV, IR, MS, and NMR) and X-ray diffraction analysis. Compounds 1, 3, and 4 were the first examples of 2,4-imidazolidinediones isolated from this genus. In addition, the cytotoxic and antibacterial activities of compounds 1 and 2 were also evaluated.
Subject(s)
Alkaloids , Antineoplastic Agents , Porifera , Animals , Molecular Structure , Porifera/chemistry , Antineoplastic Agents/chemistry , Alkaloids/chemistry , Magnetic Resonance SpectroscopyABSTRACT
A new chlorobenzoate derivative, solieriate (1), together with six known compounds (2-7), were isolated from the red alga Solieria sp. The structures of 1-7 were determined by comprehensive spectroscopic methods and X-ray diffraction analysis. Compound 1 is the first example of halogenated derivative isolated from this genus. In addition, 1 exhibited moderate antibacterial activity on A. baumannii with MIC value of 64 µg/ml.
Subject(s)
Rhodophyta , Rhodophyta/chemistry , Crystallography, X-Ray , Anti-Bacterial Agents/chemistry , Chlorobenzoates , Molecular StructureABSTRACT
Two new halogenated metabolites, laurenhalogens A (1) and B (2), along with four known ones (3-6), were isolated from the red alga Laurencia sp. The structures of 1 and 2 were determined by the means of UV, IR, MS, NMR and X-ray diffraction analysis. In addition, the antibacterial activities of 1-6 were also evaluated.
Subject(s)
Laurencia , Sesquiterpenes , Laurencia/chemistry , Molecular Structure , Magnetic Resonance Spectroscopy , Anti-Bacterial Agents/chemistry , Crystallography, X-Ray , Sesquiterpenes/chemistryABSTRACT
A new amide, baeriamide (1), along with nine known diketopiperazines (2-10), was isolated from the marine sponge Haliclona baeri. Their structures were identified by the means of UV, IR, MS and NMR. The absolute configuration of 1 was established by Marfey's method and comparing the specific optical rotation with the known compound HCO-Val-Gly methyl ester. Compound 1 was derived from dehydration of formylated L-valine with γ-amino-butanoic acid methyl ester. Compounds 2-10 were isolated from the genus of Haliclona for the first time. The absolute confirmation of 7 was confirmed first by the means of single-crystal X-ray diffraction. The cytotoxic, antibacterial, antiviral and antifouling activities of these compounds were also tested. However, none of them exhibited significant bioactivities.
Subject(s)
Haliclona , Animals , Haliclona/chemistry , Amides/pharmacology , Magnetic Resonance Spectroscopy , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , DiketopiperazinesABSTRACT
(+)- and (-)-Spongiterpene [(+)-1 and (-)-1], a pair of new valerenane sesquiterpene enantiomers, along with four known compounds (2-5) were isolated from the marine sponge Spongia sp. The structures of (+)-1 and (-)-1 including absolute configurations were determined by spectroscopic analysis, quantum chemical calculation and X-ray diffraction. Compounds (+)-1 and (-)-1 were the first examples of valerenane sesquiterpenes isolated from the marine sponges. The cytotoxic activities of (+)-1 and (-)-1 were also evaluated.
Subject(s)
Aquatic Organisms/chemistry , Porifera/chemistry , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Death/drug effects , Cell Line, Tumor , Stereoisomerism , X-Ray DiffractionABSTRACT
Two new pyrrolidine alkaloids, acanthophoraines B (1) and C (2), together with five known ones (3-7) were isolated from the red alga Acanthophora spicifera. Their structures were elucidated by extensive spectroscopic methods and single-crystal X-ray diffraction analysis. The absolute configuration of 2 was established by ECD calculation. The antibacterial activities of 1-7 were also evaluated.
Subject(s)
Alkaloids , Anti-Infective Agents , Rhodophyta , Alkaloids/pharmacology , Anti-Bacterial Agents/pharmacology , Crystallography, X-Ray , Molecular Structure , Pyrrolidines/pharmacologyABSTRACT
A new polyketide, solieritide A (1), along with six known ones (2-7), had been isolated from the red alga Solieria sp. The structures of these compounds were elucidated by spectroscopic analysis. The absolute configuration of 1 was determined by the method of X-ray diffraction. Compound 1 was a rare polyketide bearing benzopyrone ring fused with γ-butyrolactone. Compounds 2-7 were isolated from the red algae of genus Solieria for the first time. The antibacterial activities of 1-7 were also discussed.
Subject(s)
Anti-Infective Agents , Polyketides , Rhodophyta , 4-Butyrolactone , Anti-Bacterial Agents/pharmacology , Molecular Structure , Polyketides/pharmacologyABSTRACT
OBJECTIVE: To compare the efficacies of 0.02% atropine eye drops and orthokeratology to control axial length (AL) elongation in children with myopia. METHODS: In this historical control study, 247 children with myopia whose administration of 0.02% atropine (n=142) or underwent orthokeratology from an earlier study (n=105, control group) were enrolled. Data on AL and other baseline parameters were recorded at baseline and after 1 and 2 years of treatment. RESULTS: The mean changes in AL in the first and second years of treatment were 0.30±0.21 and 0.28±0.20 mm, respectively, in the 0.02% atropine group and 0.16±0.20 and 0.20±0.16 mm, respectively, in the orthokeratology group. Axial length elongations after 2 years of treatment were 0.58±0.35 and 0.36±0.30 mm (P=0.007) in the 0.02% atropine and orthokeratology groups, respectively. Multivariate regression analyses showed that the AL elongation was significantly faster in the 0.02% atropine group than in the orthokeratology group (ß=0.18, P=0.009). In multivariate regression analyses, younger age and shorter baseline AL were associated with a rapid AL elongation in the 0.02% atropine group (ßage=-0.04, P=0.01; ßAL=-0.17, P=0.03), while younger age, lower baseline spherical equivalent refractive error (SER), and shorter baseline AL were associated with a greater increase in AL in the orthokeratology group (ßage=-0.03, P=0.04; ßSER=0.06, P=0.03; ßAL=-0.11, P=0.009). Faster AL elongation was found in the 0.02% atropine group compared with the orthokeratology group at higher baseline SER (P=0.04, interaction test). CONCLUSION: Within the limits of this study design, orthokeratology seems to be a better method for controlling AL elongation compared with administration of 0.02% atropine in children with higher myopia over a treatment period of 2 years.
Subject(s)
Myopia , Orthokeratologic Procedures , Atropine , Axial Length, Eye , Child , Humans , Infant, Newborn , Myopia/therapy , Refraction, OcularABSTRACT
Three new butenolides, caulerpalide A and a pair of enantiomers, (+)-caulerpalide B and (-)-caulerpalide B, together with seven known compounds, have been isolated from the green alga Caulerpa racemosa var. turbinata. All these structures were determined by spectroscopic techniques. The absolute configurations of caulerpalide A, (+)-caulerpalide B and (-)-caulerpalide B were elucidated by the method of ECD calculation. This is the first separation of butenolides from the algae of genus Caulerpa. Additionally, the antibacterial activities of the nine isolated compounds were also evaluated.
Subject(s)
4-Butyrolactone/analogs & derivatives , Anti-Bacterial Agents/pharmacology , Caulerpa/chemistry , 4-Butyrolactone/chemistry , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Acinetobacter baumannii/drug effects , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Dose-Response Relationship, Drug , Enterococcus faecalis/drug effects , Escherichia coli/drug effects , Methicillin-Resistant Staphylococcus aureus/drug effects , Microbial Sensitivity Tests , Molecular Conformation , Pseudomonas aeruginosa/drug effects , Structure-Activity RelationshipABSTRACT
PURPOSE: To investigate the effect of orthokeratology (OK) lens on axial length (AL) elongation in unilateral myopia and bilateral myopia with anisometropia children. METHODS: Twenty-seven unilateral myopia (group 1) and 25 bilateral myopia with anisometropia children (group 2) were involved in this 1-year retrospective study. The eyes with higher spherical equivalent refractive error (SER) were assigned to the H eyes subgroup and the fellow eyes with lower SER to the L eyes subgroup in the two groups. RESULTS: The mean change in AL of H eyes and L eyes were 0.11 ± 0.19 mm, 0.30 ± 0.28 mm in group 1 (P = 0.04) and 0.09± 0.14mm, 0.13± 0.16mm in group 2 (P = 0.36), respectively. Multivariate regression analyses showed that significant difference of change in AL was found between H eyes and L eyes in group1 (ß=0.25, P = 0.03), but no difference in group 2 (ß=0.09, P = 0.12). The AL of H eyes in group 1 and group 2, H eyes in group 1 and L eyes in group 2 had the same increased rate (ß= -0.04, P = 0.43; ß = 0.02, P = 0.56). CONCLUSIONS: Monocular OK lens is effective on suppression AL elongation of the myopic eyes and reduce anisometropia value in unilateral myopic children. The OK lens can control the AL elongation in both eyes at the same rate, but it cannot reduce anisometropia value in bilateral myopia with anisometropia children after 1-year follow-up.
Subject(s)
Anisometropia/therapy , Axial Length, Eye/pathology , Contact Lenses , Myopia/therapy , Orthokeratologic Procedures , Adolescent , Anisometropia/physiopathology , Child , Corneal Topography , Female , Humans , Male , Myopia/physiopathology , Refraction, Ocular , Retrospective StudiesABSTRACT
A new pyrrolidine alkaloid, acanthophoraine A (1), along with six known alkaloids (2-7), had been isolated from the red alga Acanthophora spicifera. The structures of these compounds were identified by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 represents the first example of N-isobutyl pyrrolidone with an urea arm. The antimicrobial activity of 1 was also evaluated.[Figure: see text].
Subject(s)
Alkaloids/isolation & purification , Pyrrolidines/isolation & purification , Rhodophyta/chemistry , Alkaloids/chemistry , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/pharmacology , Molecular Conformation , Molecular Structure , Pyrrolidines/chemistry , Spectrum AnalysisABSTRACT
A new thiodiketopiperzaine, tedanizaine A (1), together with six known ones, were isolated from the marine sponge Tedania sp. Their structures were determined by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 was the second example of thiodiketopiperazine bearing a thiazolidine unit. Cytotoxic activities of 1 were also evaluated.
Subject(s)
Cytotoxins/isolation & purification , Diketopiperazines/isolation & purification , Porifera/chemistry , Thiazoles/isolation & purification , Animals , Cell Line , Cytotoxins/chemistry , Cytotoxins/pharmacology , Diketopiperazines/chemistry , Diketopiperazines/pharmacology , Humans , Molecular Conformation , Molecular Structure , Spectrum Analysis , Thiazoles/chemistry , Thiazoles/pharmacologyABSTRACT
A novel valerenane sesquiterpenoid sinulaspirolactam A (1), together with five known compounds, was isolated from the soft coral Sinularia sp. Their structures were determined by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 was the first example of valerenane sesquiterpenoid bearing an aza-spiro[4.5] ring moiety, the plausible biogenetic pathway of which was proposed. Cytotoxic activities of these compounds were also evaluated.
Subject(s)
Anthozoa/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , Animals , Cell Line, Tumor , Cell Survival/drug effects , Models, Molecular , Molecular StructureABSTRACT
Two new polyketides, aspergchromones A (1) and B (2), together with five known compounds, secalonic acid D (3), noreugenin (4), (3S)-5-hydroxymellein (5), (4S)-6-hydroxyisosclerone (6), and (-)-regiolone (7), were isolated from the ethyl acetate extract of marine sponge-derived fungus Aspergillus sp. SCSIO XWS03F03. Their structures were elucidated by means of spectroscopic techniques (1D and 2D NMR, MS, UV, and IR). The absolute configurations of the new compounds were established by ECD calculations. Compound 3 showed moderate antimicrobial activity.
Subject(s)
Aspergillus/chemistry , Polyketides/isolation & purification , Porifera/microbiology , Xanthones/isolation & purification , Animals , Marine Biology , Microbial Sensitivity Tests , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Polyketides/chemistry , Xanthones/chemistryABSTRACT
A new α-pyrone, nocapyrone S (1), together with five known compounds (2-6), were isolated from the deep-sea actinomycete Nocardiopsis dassonvillei subsp. dassonvillei DSM 43111(T). Their structures were determined by spectroscopic analyses. The absolute configuration of 1 was established by quantum approaches. Cytotoxic activity of 1 was evaluated against K562, MCF-7, SGC7901, A375, Hela, and HepG2 cell lines.