Two new diketopiperazines from the marine sponge Dysidea sp.

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.

The Janus face of HIF-1α in ischemic stroke and the possible associated pathways.

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.

(+)- and (-)-Tedanine, a pair of new enantiomeric indolone alkaloids from the marine sponge Tedania sp.

(+)- 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.

Two New Pairs of Enantiomeric Butenolides from the Marine Sponge Suberties sp.

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 40.8 µM.

Spongimides A and B, two new alkaloids from the marine sponge Spongia sp.

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.

A new chlorobenzoate derivative from the red alga Solieria sp.

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.

A new amide from the marine sponge Haliclona baeri.

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.

Two new halogenated metabolites from the red alga Laurencia sp.

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.

Comparison of Administration of 0.02% Atropine and Orthokeratology for Myopia Control.

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.

(+)- and (-)-Spongiterpene, a pair of new valerenane sesquiterpene enantiomers from the marine sponge Spongia Sp.

(+)- 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.

Two new pyrrolidine alkaloids from the red alga Acanthophora spicifera.

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.

Solieritide A, a new polyketide from the red alga Solieria sp.

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.

Three New Butenolides from the Green Alga Caulerpa racemosa var. turbinata.

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.

A new thiodiketopiperzaine from the marine sponge Tedania sp.

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.

Acanthophoraine A, a new pyrrolidine alkaloid from the red alga Acanthophora spicifera.

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].

Effects of orthokeratology lens on axial length elongation in unilateral myopia and bilateral myopia with anisometropia children.

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.

Sinulaspirolactam A, a novel aza-spirocyclic valerenane sesquiterpenoid from soft coral Sinularia sp.

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.

Aspergchromones A and B, two new polyketides from the marine sponge-associated fungus Aspergillus sp. SCSIO XWS03F03.

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.

A new α-pyrone from the deep-sea actinomycete Nocardiopsis dassonvillei subsp. dassonvillei DSM 43111(T).

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.

Design and Synthesis of Dimeric Securinine Analogues with Neuritogenic Activities.

Neurite outgrowth is crucial during neuronal development and regeneration, and strategies that aim at promoting neuritogenesis are beneficial for reconstructing synaptic connections after neuronal degeneration and injury. Using a bivalent analogue strategy as a successful approach, the current study identifies a series of novel dimeric securinine analogues as potent neurite outgrowth enhancers. Compounds 13, 14, 17-19, and 21-23, with different lengths of carbon chain of N,N-dialkyl substituting diacid amide linker between two securinine molecules at C-15 position, exhibited notable positive effects on both neuronal differentiation and neurite extension of neuronal cells. Compound 14, one of the most active compounds, was used as a representative compound for mechanistic studies. Its action on neurite outgrowth was through phosphorylation/activation of multiple signaling molecules including Ca2+/calmodulin-dependent protein kinase II (CaMKII), extracellular signal-regulated kinase (ERK) and Akt. These findings collectively identify a new group of beneficial compounds for neuritogenesis, and may provide insights on drug discovery of neural repair and regeneration.