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1.
Nat Prod Res ; : 1-11, 2021 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-34348550

RESUMO

2ß,3α,19-Triacetoxy-17-hydroxyspongia-13(16),14-diene (1), a novel acetoxy diterpenoid, and 18-nor-2,17-hydroxyspongia-1,4,13(16),14-quaien-3-one (2), belonging to the rare 18-nor-spongian carbon skeleton, together with six related known metabolites (3‒8), were isolated from the aquaculture Spongia officinalis Linnaeus, 1759. Their structures were elucidated by comprehensive spectroscopic analysis, quantum chemical calculation of NMR parameters, and electronic circular dichroism (ECD). Compounds 3, 4, and 5 exhibited moderate inhibition against STAT3/NF-κB, HIF-1, Wnt signalling pathways. Compounds 1, 3, and 5 showed cytotoxicity activities against K562 cell line with IC50 values of 7.3, 3.5, and 6.4 µM, respectively.

2.
Biomater Sci ; 9(16): 5612-5625, 2021 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-34254062

RESUMO

This study reports that the use of low-frequency sonophoresis (LFS) in combination with sponge Haliclona sp. spicules (SHS), referred to as cSoSp (combined Sonophoresis and Spicules), can enhance the transdermal drug delivery in a synergistic manner. The topical application of cSoSp in vitro significantly enhanced the skin absorption of Fluorescent-Dextrans (4000 Da, FD-4K), a model drug of low-molecular-weight heparin (LMWH). The utilization of cSoSp dramatically increased the transdermal flux of FD-4K (188.6 ± 93.7 ng cm-2 h-1) compared to LFS (5.8 ± 3.1 ng cm-2 h-1) and SHS (3.2 ± 1.2 ng cm-2 h-1) among others. The mechanism of action of cSoSp could be attributed to the synergism between plenty of long-lasting nano-channels created by SHS and the disorders of SC lipids made by shock waves of LFS, which improves the homogeneity of the cavitation effects. Furthermore, LMWH (3000 Da) was transdermally delivered by using cSoSp to treat both superficial venous thrombosis (SVT) and deep venous thrombosis (DVT) in the marginal ear vein of rabbits with a good therapeutic effect. Furthermore, skin irritation and toxicity studies using guinea pigs indicated that cSoSp was nonirritating without any morphological changes in the keratinocytes. cSoSp offers a promising strategy to enhance the transdermal delivery of hydrophilic macromolecules such as heparin.


Assuntos
Heparina , Trombose Venosa , Administração Cutânea , Animais , Cobaias , Heparina/metabolismo , Heparina de Baixo Peso Molecular , Coelhos , Pele/metabolismo , Absorção Cutânea , Trombose Venosa/tratamento farmacológico , Trombose Venosa/metabolismo
3.
Mar Drugs ; 19(4)2021 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-33921176

RESUMO

Uncontrolled bleeding is the main cause of mortality from trauma. Collagen has been developed as an important hemostatic material due to its platelet affinity function. A bath sponge skeleton is rich in collagen, also known as spongin. To understand the hemostatic effect of spongin, spongin materials, SX, SFM and SR were prepared from the bath sponge Spongia officinalis, and hemostatic experiments were performed. The SX, SFM and SR were significantly better than the positive control, type I collagen, in shortening the whole blood clotting time in vitro and hemostasis upon rat tail amputation. In a hemostatic experiment of rabbit common carotid artery injury, the hemostatic time and 3 h survival rate of the SFM group were 3.00 ± 1.53 min and 100%, respectively, which are significantly better than those of the commercial hemostat CELOX-A (10.33 ± 1.37 min and 67%, respectively). Additionally, the SFM showed good coagulation effects in platelet-deficient blood and defibrinated blood, while also showing good biocompatibility. Through a variety of tests, we speculated that the hemostatic activity of the SFM is mainly caused by its hyperabsorbency, high affinity to platelets and high effective concentration. Overall, the SFM and spongin derivates could be potential hemostatic agents for uncontrolled bleeding and hemorrhagic diseases caused by deficiency or dysfunction of coagulation factors.


Assuntos
Lesões das Artérias Carótidas/tratamento farmacológico , Colágeno/farmacologia , Hemorragia/prevenção & controle , Hemostasia/efeitos dos fármacos , Hemostáticos/farmacologia , Poríferos/metabolismo , Animais , Coagulação Sanguínea/efeitos dos fármacos , Testes de Coagulação Sanguínea , Colágeno/isolamento & purificação , Colágeno/toxicidade , Modelos Animais de Doenças , Hemostáticos/isolamento & purificação , Hemostáticos/toxicidade , Estrutura Molecular , Ativação Plaquetária/efeitos dos fármacos , Testes de Função Plaquetária , Coelhos , Ratos , Relação Estrutura-Atividade
4.
Pharm Res ; 37(6): 100, 2020 May 20.
Artigo em Inglês | MEDLINE | ID: mdl-32436083

RESUMO

PURPOSE: We investigated the potential correlations between skin barrier integrity and hydrophilic drugs distribution in skin in the presence of different types of penetration enhancers (PEs) and their combinations. METHODS: We measured skin conductivity to evaluate skin barrier integrity before and after the topical application of different chemical PEs, physical PE, peptide PE and their combinations in vitro. We also investigated their effect on the skin distribution profiles of two hydrophilic model drugs, Fluorescein sodium (376 Da) and Fluorescein isothiocyanate-dextrans 10 (10 KDa). RESULTS: The physical PE significantly increased the skin conductivity compared to all other PEs, while the peptide PE had no effect on it. The drug deposition in different skin layers was not only dependent on PE applied but also its own molecular weight. We further found two excellent correlations: one (R2 = 0.9388) between skin barrier integrity and total skin absorption of FNa and another one(R2 = 0.9212) between skin barrier integrity and the deposition of FNa in dermis and receptor in presence of chemical or physical PEs and their combinations. CONCLUSIONS: The total skin absorption or the deposition in dermis and receptor of small hydrophilic drug in the presence of chemical and physical PEs and their combinations show a good correlation with skin barrier integrity. However, such correlations hold true neither for large hydrophilic drug nor for peptide PE. All good relationships found in this work will allow screening suitable PEs or combinations by measuring the skin conductivity induced by corresponding PEs. Graphical Abstract The total skin absorption of small hydrophilic drug shows a good correlation with skin barrier integrity in the presence of chemical and physical penetration enhancers and their combinations. However, such a correlation hold true neither for large hydrophilic drug nor for peptide penetration enhancer.


Assuntos
Melhoramento Biomédico/métodos , Portadores de Fármacos/química , Peptídeos/química , Preparações Farmacêuticas/química , Absorção Cutânea/efeitos dos fármacos , Pele/metabolismo , Administração Cutânea , Animais , Dextranos/administração & dosagem , Dextranos/química , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Excipientes/química , Fluoresceína/administração & dosagem , Fluoresceína/química , Fluoresceína-5-Isotiocianato/administração & dosagem , Fluoresceína-5-Isotiocianato/análogos & derivados , Fluoresceína-5-Isotiocianato/química , Cobaias , Humanos , Interações Hidrofóbicas e Hidrofílicas , Técnicas In Vitro , Conformação Molecular , Estrutura Molecular , Peso Molecular , Permeabilidade , Preparações Farmacêuticas/administração & dosagem , Solubilidade , Relação Estrutura-Atividade , Distribuição Tecidual
5.
Mol Ther Nucleic Acids ; 20: 639-648, 2020 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-32380414

RESUMO

We report the topical administration of sponge Haliclona sp. Spicules (SHS) combined with cationic flexible liposomes (CFL) to increase the delivery of small interfering RNA (siRNA) into viable skin cells in vitro and in vivo. SHS can be applied topically as novel microneedles to overcome skin barrier by creating plenty of new microchannels in stratum corneum. Subsequently, well-designed CFL can be also utilized topically as nanocarriers to overcome skin cells membrane by delivering siRNA to skin deep layers through these microchannels and thereby facilitating their cell internalization. The topical application of SHS in combination with CFL (0.05% of lipids, w/v), referred to as CFL(0.05%), enhanced siRNA skin penetration in vitro by 72.95 ± 2.97-fold compared to control group (p < 0.001). Further, the topical application of SHS in combination with CFL(0.05%) on female BALB/c mice skin resulted in 29.21% ± 1.41% of glyceraldehyde-3-phosphate dehydrogenase (GAPDH) knockdown at all application area in vivo, which was not significantly different from the GAPDH protein knockdown rate in the subcutaneous injection center. However, the high knockdown rate only appears in the vicinity (<0.5 cm) of the injection center. In sum, this study provides a promising strategy of topical delivery of siRNA by the combined used of SHS and well-designed CFL.

6.
Biomater Sci ; 7(4): 1299-1310, 2019 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-30821312

RESUMO

We demonstrated that the topical combined use of sponge Haliclona sp. spicules (SHS) and flexible liposomes (FL), referred to as SFLS (SHS-Flexible Liposomes combined System), can result in synergy to improve the skin absorption and deposition of hyaluronic acid (HA), especially in deep skin layers, both in vitro and in vivo. SHS treatment can result in skin micro-channels which are continuous, deep enough (48.6 ± 13.5 µm) and available in large quantities (850 ± 125 micro-channels per mm2). These micro-channels gradually closed up in 120 h and also allowed the intact vesicles of flexible liposomes and vesicle-bound or vesicle-encapsulated HA to penetrate into the skin-deep layers under the driving force of transdermal osmotic gradients. Specifically, SFLS topical application enhanced the penetration of FITC-HA (MW: 250 kDa) into porcine skin in vitro up to 23.2 ± 3.7%, which is 19.4 ± 3.1-fold (p < 0.001) that of a Phosphate Buffered Saline (PBS) group, 3.4 ± 0.5-fold (p < 0.01) that of an SHS group and 3.6 ± 0.6-fold (p < 0.01) that from the combined use of a Dermaroller and flexible liposomes. Moreover, SFLS can lead to significantly enhanced skin deposition of HA in all skin layers, especially in deep skin layers: up to 86.8 ± 4.1% of HA absorbed by skin was accumulated in deep skin layers. The effectiveness of SFLS topical application was also confirmed in vivo by using BALB/c mice. In addition, a skin irritation and toxicity study showed that the SFLS treatment may cause very minimal redness and the skin can recover in a short time. In sum, the combined use of SHS and FL (SFLS) offers a promising strategy to safely and effectively improve the skin delivery of hydrophilic biomacromolecules such as HA.


Assuntos
Ácido Hialurônico/química , Poríferos/química , Pele/química , Animais , Feminino , Cabelo/química , Cabelo/citologia , Ácido Hialurônico/administração & dosagem , Lipossomos/química , Camundongos , Camundongos Endogâmicos BALB C , Pele/citologia , Absorção Cutânea , Suínos
7.
Microorganisms ; 8(1)2019 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-31905988

RESUMO

Some sponges have been shown to accumulate abundant phosphorus in the form of polyphosphate (polyP) granules even in waters where phosphorus is present at low concentrations. But the polyP accumulation occurring in sponges and their symbiotic bacteria have been little studied. The amounts of polyP exhibited significant differences in twelve sponges from marine environments with high or low dissolved inorganic phosphorus (DIP) concentrations which were quantified by spectral analysis, even though in the same sponge genus, e.g., Mycale sp. or Callyspongia sp. PolyP enrichment rates of sponges in oligotrophic environments were far higher than those in eutrophic environments. Massive polyP granules were observed under confocal microscopy in samples from very low DIP environments. The composition of sponge symbiotic microbes was analyzed by high-throughput sequencing and the corresponding polyphosphate kinase (ppk) genes were detected. Sequence analysis revealed that in the low DIP environment, those sponges with higher polyP content and enrichment rates had relatively higher abundances of cyanobacteria. Mantel tests and canonical correspondence analysis (CCA) examined that the polyP enrichment rate was most strongly correlated with the structure of microbial communities, including genera Synechococcus, Rhodopirellula, Blastopirellula, and Rubripirellula. About 50% of ppk genes obtained from the total DNA of sponge holobionts, had above 80% amino acid sequence similarities to those sequences from Synechococcus. In general, it suggested that sponges employed differentiated strategies towards the use of phosphorus in different nutrient environments and the symbiotic Synechococcus could play a key role in accumulating polyP.

8.
FEMS Microbiol Ecol ; 94(5)2018 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-29617990

RESUMO

Tedania sp. is a dominant sponge that is ubiquitous along the southeast coast of China. High-throughput sequencing and transmission electron microscopy were used to describe a detailed profile of sponge-associated microbiomes at seven life stages: adult, embryo-containing spawning adult, embryo, pre-competent larva at 2 h and 4 h, competent larva at 8 h and post-larva within 1-2h after settlement, as well as the surrounding seawater. Among a total of 15098 operational taxonomic units (OTUs), 13 were present exclusively in all stages of the sponge life cycle and could thus be identified as sponge-specific bacteria. Many OTUs were shared between the sponge and seawater, though abundance differed. The relative abundance of ß-Proteobacteria associated with sponges was much higher than found in seawater. The microbiomes from each life stage also exhibited a characteristic distribution. Synechococcales dominated in adults, and Enterobacteriaceae was prominent in larvae. The competent larva was notable, with sharp increases in the total OTUs, diversity indices, richness estimates and unique OTUs. Some bacterial groups that were rare in other sponge stages and seawater, such as Clostridia (5.6%), were markedly more abundant in competent larvae. In conclusion, this work greatly advances our understanding of the dynamics and persistence of the sponge-microbe association.


Assuntos
Bactérias/isolamento & purificação , Estágios do Ciclo de Vida , Microbiota , Poríferos/microbiologia , Animais , Bactérias/classificação , Bactérias/genética , Biodiversidade , China , DNA Bacteriano/genética , Sequenciamento de Nucleotídeos em Larga Escala , Filogenia , Poríferos/crescimento & desenvolvimento , RNA Ribossômico 16S/genética , Água do Mar/microbiologia , Análise de Sequência de DNA
9.
Mol Pharm ; 14(9): 3188-3200, 2017 09 05.
Artigo em Inglês | MEDLINE | ID: mdl-28763230

RESUMO

We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 µm in length and ∼7 µm in diameter). SHS can physically disrupt skin in a dose-dependent manner and retain within the skin over at least 72 h, which allows sustained skin penetration of hydrophilic biomacromolecules. The magnitude of enhancement of FD delivery into skin induced by SHS treatment was dependent on its molecular weight. Specifically, SHS topical application enhanced FD-10 (MW: 10 kDa) penetration into porcine skin in vitro by 33.09 ± 7.16-fold compared to control group (p < 0.01). SHS dramatically increased the accumulation of FD-10 into and across the dermis by 62.32 ± 13.48-fold compared to the control group (p < 0.01). In vivo experiments performed using BALB/c mice also confirmed the effectiveness of SHS topical application; the skin absorption of FD-10 with SHS topical application was 72.14 ± 48.75-fold (p < 0.05) and 15.39 ± 9.91-fold (p < 0.05) higher than those from the PBS and Dermaroller microneedling, respectively. Further, skin irritation study and transepidermal water loss (TEWL) measurement using guinea pig skin in vivo indicated that skin disruption induced by SHS treatment is self-limited and can be recovered with time and efficiently. SHS can offer a safe, effective, and sustained skin delivery of hydrophilic biomacromolecules and presents a promising platform technology for a wide range of cosmetic and medical applications.


Assuntos
Haliclona/metabolismo , Pele/metabolismo , Animais , Epiderme/metabolismo , Feminino , Cobaias , Interações Hidrofóbicas e Hidrofílicas , Camundongos Endogâmicos BALB C , Microscopia Confocal , Microscopia Eletrônica de Varredura , Peso Molecular , Absorção Cutânea , Água/metabolismo
10.
Genes (Basel) ; 6(4): 1023-52, 2015 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-26492274

RESUMO

Sponges are an ancient metazoan group with broad ecological, evolutionary, and biotechnological importance. As in other marine invertebrates with a biphasic life cycle, the developing sponge undergoes a significant morphological, physiological, and ecological transformation during settlement and metamorphosis. In this study, we compare new transcriptome datasets for three life cycle stages of the red sponge (Mycale phyllophila) to test whether gene expression (as in the model poriferan, Amphimedon queenslandica) also varies more after settlement and metamorphosis. In contrast to A. queenslandica, we find that the transcriptome of M. phyllophila changes more during the earlier pre-competent larva/post-larva transition that spans these defining events. We also find that this transition is marked by a greater frequency of significantly up-regulated Gene Ontology terms including those for morphogenesis, differentiation, and development and that the transcriptomes of its pre-competent larvae and adult are distinct. The life cycle transcriptome variation between M. phyllophila and A. queenslandica may be due to their long separate evolutionary histories and corresponding differences in developmental rates and timing. This study now calls for new transcriptome datasets of M. phyllophila and other sponges, which will allow for tests of the generality of our life cycle expression differences and for the greater exploitation of poriferans in both basic and applied research.

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