Antibacterial Compounds from Marine Bacteria, 2010–2015

Schinke, Cláudia; Martins, Thamires; Queiroz, S. C. do N. de; Melo, I. S. de; Reyes, Felix G. R.

doi:10.1021/acs.jnatprod.6b00235

Cited by 74 publications

(55 citation statements)

References 59 publications

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“…In another study conducted by Zhu et al, a library of marine natural products with diverse molecular scaffolds were studied and the results showed anti‐AD effects with two steroidal extracts isolated from the U . unicinctus . Using the FRET approach, the EC 50 values of these compounds when tested against BACE1, have identified hecogenin (compound 29 ) cholest‐4‐en‐3‐one to possess a value of 116.3 μM, while that of cholest‐4‐en‐3‐one (compound 30 ) was 390.6 μM.…”

Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

“…82 In another study conducted by Zhu et al, 85 a library of marine natural products with diverse molecular scaffolds were studied and the results showed anti-AD effects with two steroidal extracts isolated from the U. unicinctus. 86 Using the FRET approach, the EC 50 values of these compounds when tested against BACE1, have identified hecogenin (compound 29) cholest-4-en-3-one to possess a value of 116.3 μM, while that of cholest-4-en-3-one (compound 30) was 390.6 μM. In comparison with the more potent synthetic BACE1 inhibitors, the naturally derived hecogenin and cholest-4-en-3-one have lower molecular weights that would allow them to effectively penetrate the BBB.…”

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

See 1 more Smart Citation

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Moussa-Pacha

Abdin

Omar

et al. 2019

Medicinal Research Reviews

226

175

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Alzheimer's disease (AD) is an irreversible, progressive neurodegenerative brain disorder with no current cure. One of the important therapeutic approaches of AD is the inhibition of β‐site APP cleaving enzyme‐1 (BACE1), which is involved in the rate‐limiting step of the cleavage process of the amyloid precursor protein (APP) leading to the generation of the neurotoxic amyloid β (Aβ) protein after the γ‐secretase completes its function. The produced insoluble Aβ aggregates lead to plaques deposition and neurodegeneration. BACE1 is, therefore, one of the attractive targets for the treatment of AD. This approach led to the development of potent BACE1 inhibitors, many of which were advanced to late stages in clinical trials. Nonetheless, the high failure rate of lead drug candidates targeting BACE1 brought to the forefront the need for finding new targets to uncover the mystery behind AD. In this review, we aim to discuss the most promising classes of BACE1 inhibitors with a description and analysis of their pharmacodynamic and pharmacokinetic parameters, with more focus on the lead drug candidates that reached late stages of clinical trials, such as MK8931, AZD‐3293, JNJ‐54861911, E2609, and CNP520. In addition, the manuscript discusses the safety concerns and insignificant physiological effects, which were highlighted for the most successful BACE1 inhibitors. Furthermore, the review demonstrates with increasing evidence that despite tremendous efforts and promising results conceived with BACE1 inhibitors, the latest studies suggest that their clinical use for treating Alzheimer's disease should be reconsidered. Finally, the review sheds light on alternative therapeutic options for targeting AD.

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Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Moussa-Pacha

Abdin

Omar

et al. 2019

Medicinal Research Reviews

226

175

View full text Add to dashboard Cite

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“…In the same set of experiments, production of clorobiocin and its derivatives exceeded 100 mg/L in S. coelicolor M512, M1146 and M1154; an optimal production of caprazamycin aglycones reached 152 mg/L in the host M1154 when 0.6 % Q-5247 and 0.2 mg/L CoCl 2 were present (Flinspach et al, 2010). Similarly, kocurin, a new thiopeptide antibiotic isolated from Kocuria rosea (Schinke et al, 2017), was produced in M1146 by expressing the kocurin BGC (Linares-Otoya et al, 2017). …”

Section: Streptomyces Coelicolor As a Heterologous Hostmentioning

confidence: 99%

Streptomycetes: Surrogate hosts for the genetic manipulation of biosynthetic gene clusters and production of natural products

Nepal

Wang

2019

Biotechnology Advances

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Due to the worldwide prevalence of multidrug-resistant pathogens and high incidence of diseases such as cancer, there is an urgent need for the discovery and development of new drugs. Nearly half of the FDA-approved drugs are derived from natural products that are produced by living organisms, mainly bacteria, fungi, and plants. Commercial development is often limited by the low yield of the desired compounds expressed by the native producers. In addition, recent advances in whole genome sequencing and bioinformatics have revealed an abundance of cryptic biosynthetic gene clusters within microbial genomes. Genetic manipulation of clusters in the native host is commonly used to awaken poorly expressed or silent gene clusters, however, the lack of feasible genetic manipulation systems in many strains often hinders our ability to engineer the native producers. The transfer of gene clusters into heterologous hosts for expression of partial or entire biosynthetic pathways is an approach that can be used to overcome this limitation. Heterologous expression also facilitates the chimeric fusion of different biosynthetic pathways, leading to the generation of “unnatural” natural products. The genus Streptomyces is especially known to be a prolific source of drugs/antibiotics, its members are often used as heterologous expression hosts. In this review, we summarize recent applications of Streptomyces species, S. coelicolor, S. lividans, S. albus, S. venezuelae and S. avermitilis, as heterologous expression systems.

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“…Sampel teritip yang diambil di Pulau Panjang, Kabupaten Jepara, pada titik koordinat S 06o34'37.4" dan E 110o37'51.4" sebanyak satu koloni. Berdasarkan hasil identifikasi menggunakan buku "Zoologische Verhandelingen" (Henry dan Patsy, 1975 (Schinke et al, 2017). Namun, eksplorasi bahan bioktif pada teritip masih sangat sedikit dilakukan.…”

Section: Hasil Dan Pembahasanunclassified

Aktivitas Antagonis Bakteri yang Berasosiasi dengan Teritip (Balanus sp.) terhadap Bakteri Escherichia coli dan Bacillus cereus

2019

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Marine invertebrates are the most productive source of bioactive compounds. However, most of the compounds originally produced by the microorganisms living associated with the invertebrates. Barnacle is an invertebrate that has a unique interaction with bacteria. Escherichia coli and Bacillus cereus are the cause of the foodborne disease that causes of remarkedly losses in the food industry. The barnacle was collected from Panjang Island, Jepara. The bacterial isolates were obtained by serial dilution followed by isolation based on morphological characteristics. The antagonistic assay to E. coli dan B. cereus was utilized for screened the isolates. Then, the active isolates were cultured for the further test with the disc diffusion agar method of the supernatant followed by the extracts. The most active isolates were identified based on molecular method. A total of 14 isolates were obtained from the Balanus sp., which six of them have activity against the E. coli and B. cereus. The isolates TJ 5.4 and TJ 5.5 have the strongest activity the bacteria. Base on the analyses of the BLAST and phylogenetic tree the isolates showed 99% homology the Bacillus wiedmannii (TJ 5.4) and Lysinibacillus macroides (TJ 5.5). Invertebrata laut merupakan salah satu sumber bahan bioaktif yang paling produktif. Sebagian senyawa yang terdapat dalam biota laut, sejatinya diproduksi oleh mikroorganisme yang hidup berasosiasi dengan biota laut tersebut. Teritip merupakan salah satu hewan invertebrata yang memiliki berbagai interaksi unik dengan bakteri. Bakteri Escherichia coli dan Bacillus cereus merupakan dua dari beberapa bakteri patogen yang sering menjadi agen penyebab foodborne disease. Teritip dikoleksi dari Pulau Panjang, Jepara. Isolat bakteri diperoleh dengan metoda pengenceran bertingkat dan dilanjutkan isolasi berdasarkan karakteristik morfologis. Uji antagonis terhadap E. coli dan B. cereus digunakan untuk menskrining bioaktivitas isolat. Isolat yang aktif dikultur untuk uji lanjut yaitu supernatant dan dilanjutkan ekstraknya dengan metoda disc diffusion agar. Bakteri yang paling aktif diidentifikasi secara molekuler untuk mengetahui spesiesnya. Sebanyak 14 isolat bakteri diperoleh dari Balanus sp. dimana enam diantaranya memiliki aktivitas terhadap bakteri uji. Isolat TJ 5.4 dan TJ 5.5 memiliki aktivitas paling kuat terhadap E. coli dan B. cereus. Berdasarkan pengolahan sekuen dan analisis pohon filogenetik, dua isolat bakteri tersebut memiliki homologi 99% terhadap bakteri Bacillus wiedmannii (TJ 5.4) dan Lysinibacillus macroides (TJ 5.5).

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Antibacterial Compounds from Marine Bacteria, 2010–2015

Cited by 74 publications

References 59 publications

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Streptomycetes: Surrogate hosts for the genetic manipulation of biosynthetic gene clusters and production of natural products

Aktivitas Antagonis Bakteri yang Berasosiasi dengan Teritip (Balanus sp.) terhadap Bakteri Escherichia coli dan Bacillus cereus

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