Background: Mechanistic insight into allosteric modulation of GPCRs can facilitate antagonist design. Results: Extracellular surface residues (ECS) of the ␣ 1B -adrenoceptor at the base of extracellular loop 3 interact with the allosteric antagonist TIA. Conclusion:The identified ECS pharmacophore provides the first structural constraints for allosteric antagonist design at ␣ 1 -adrenoceptors. Significance: Binding to the ECS of a GPCR can allosterically inhibit agonist signaling.

Despite the fact that fungi are important sources of both bioactive compounds and mycotoxins, and that they are very ubiquitous in our environment, their species identification is hampered by incomplete and often unclear literature. Fungi identification is primarily based on their phenotypic and physiological characteristics. Nowadays, many molecular methods to identify fungal species have been developed. One of the methods considered as a new concept to rapidly and accurately identify unknown fungal sample is DNA Barcoding. This literature review will outline the use of DNA barcoding approach to rapidly identify fungal species and the use of ITS region that recently has been designated as primary DNA barcode for fungal kingdom. "DNA barcode" is a short, highly variable and standardized DNA region with approximately 700 nucleotides in length, which is used as a unique pattern to identify living things. Internal Transcribed Spacer (ITS) region of nuclear DNA (rDNA) has become the most sequenced region to identify fungal taxonomy at species level, and even within species. ITS region is a highly polymorphic noncoding region with enough taxonomic units. Therefore, it is able to separate sequences into species level. Even though ribosomal ITS as a universal barcode marker for fungi is still hampered by few limitations, the ITS will remain as the key choice for fungal identification. The search for alternative regions as DNA marker to improve fungal identification, especially in specific heredities, has already started.

A new 3-alkylpiperidine compound (–)-acanthocyclamine A (1) has been obtained from the methanolic extract of Acanthostrongylophora ingens (order Haplosclerida, family Petrosiidae) collected from Wakatobi Marine National Park in South East Sulawesi, Indonesia. The structure of 1 was investigated by extensive 1D- and 2D-NMR experiments. The absolute configuration of 1 was established by X-ray crystallography from anomalous dispersion effects using Cu radiation as C2 (R), C3 (R), C7 (R), and C9 (R). A plausible biosynthetic scheme leading to 1 is presented, and compared with the biosynthetic pathway proposed for the manzamine alkaloids.

Marine fungi have become an important research subject of natural products with significant value due to its diversity in chemical structures and biological activities. Epipolythiodioxopiperazines (ETPs) which are characterized by the disulfide bridge or polysulfide dioxopiperazine six membered ring have been reported to have wide ranges of bioactivities. This research was aimed to isolate, identify and investigate anticancer properties of emestrin B produced by Emericella nidulans marine fungus. Emestrin B was isolated from mycelium of the E.nidulans fungus that cultivated on malt extract broth medium for 4 weeks by using repeated column chromatography. Elucidation of molecular structure using spectra data analysis of UPLC-ESI-ToF-MS, 1 H-NMR, and 13 C-NMR techniques concluded that the compound was emestrin B. The molecular formula of emestrin B was established as C 27 H 22 N 2 O 10 S 3 (m/z) 631.0525 [M+H] +. Emestrin B was cytotoxic against T47D, HeLa, and WiDr cells with IC 50 values of 0.16; 1.56; and 1.02 μg/ml, respectively. Based on flowcytometric analysis, emestrin B could induce apoptosis in T47D cells.

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ABSTRAKSebagai bagian dari penelitian penapisan lektin dari makroalga Indonesia, 17 esktrak protein makroalga yang dikoleksi dari Pantai Binuangeun, Banten telah diuji aktivitas hemagglutinasinya terhadap eritrosit kelinci dan eritrosit manusia golongan A, B, O, masing-masing dengan perlakuan enzim dan native. Ekstraksi dilakukan dengan menggunakan 2 jenis buffer, yaitu Phosphate Buffer Saline (PBS) dan Tris Buffer Saline (TBS) pH 7. Hasil penelitian menunjukkan bahwa pada beberapa sampel, ekstrak yang dihasilkan kedua buffer, menunjukkan aktivitas hemagglutinasi yang berbeda walaupun kadar total protein ekstrak makroalga yang diekstraksi dengan PBS dan TBS tidak berbeda. Sebagian besar ekstrak makroalga yang diuji mampu mengagglutinasi setidaknya satu jenis sel eritrosit yang digunakan. Secara umum, kelompok makroalga hijau memperlihatkan aktivitas hemagglutinasi yang lebih rendah dibandingkan kelompok makroalga merah dan coklat. Meskipun ekstrak Padina australis (makroalga coklat) memberikan hasil hemagglutinasi eritrosit kelinci negatif, namun ekstrak tersebut positif menghemagglutinasi eritrosit golongan darah B dan O. Di antara 8 makroalga hijau yang diuji, hanya dua sampel yang menunjukkan aktivitas hemagglutinasi, yaitu Chaetomorpha crassa dan Halimeda macroloba. Keempat ekstrak makroalga merah yang diuji menunjukkan aktivitas hemagglutinasi yang kuat terhadap eritrosit kelinci. Ekstrak makroalga merah Gracilaria lichenoides dan Gelidiella acerosa aktif terhadap semua jenis eritrosit uji. Sementara itu, hanya ekstrak Laurencia tronoi yang menunjukkan aktivitas hemagglutinasi terhadap eritrosit golongan darah A. KATA KUNCI:makroalga, lektin, hemagglutinasi ABSTRACT As part of lectins screening project from Indonesia's macroalgae, protein extracts from 17 macroalgae species collected from Binuangen Coast, Banten were examined for their hemagglutinating activity using native and enzyme-treated rabbit and human erythrocytes (A,B,O). Extraction of the macroalgae hemagglutinins was conducted using 2 buffers, e.g Phosphat buffer saline (PBS) and Tris buffer saline (TBS) pH

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Fish serum albumin (FSA) is an aquatic resource that has potential to be developed as nutraceutical. Therefore, research was undertaken to assess albumin levels in the aqueous extract of muscle tissue of several Perciformes commonly available at a local fish market in Indonesia. Three random replicates for each of 17 Perciformes species were collected and assessed for their FSA content by application of a reversed-phase (C4) HPLC analytical method. Results of these analyses showed that the albumin concentration of the extracts was in the range 3.49-12.61 g/L, and that they varied significantly (P < 0.05) between species and families. This finding may mean that FSA levels are species and family dependent, something that could be investigated in future studies. As fishes from the family Scrombidae showed the highest concentration (12.61 g/L) of FSA, they would likely have the most value as a source for production of albumin-based nutritional and/or clinical products.