1. The disposition of the new fluorinated, biocompatible, non-ionic telomeric carrier trisacryl conjugate (F-TAC) labelled with 13C and 14C on the amide function has been studied in the rat after p.o. and i.v. administration. 2. After i.v. administration, excretion measurements have shown that radioactivity was eliminated mainly in the urine (69% within 24 h), and that faecal excretion was low (8% within 72 h). After p.o. administration, faecal elimination was significantly increased (30% within 72 h). No radioactivity was eliminated as 14CO2, after either route of administration. 3. After i.v. administration, plasma radioactivity exhibited a biphasic decrease, with t1/2 = 20 min for the first phase and 29.5 h for the second phase. The maximal plasma concentration was obtained 40 min after oral dosing, followed by a monoexponential decrease with t1/2 = 38.1 h. The ratio AUC (p.o.)/AUC (i.v.) as an assessment of bioavailability was 0.22. 4. After both i.v. and p.o. administration, a relatively homogeneous concentration of radioactivity was found in most organs, close or below the plasma concentration, indicating that tissues do not exhibit a high affinity for this molecule. In addition, F-TAC did not cross the blood-brain barrier. 5. Analysis of urine and plasma on DOWEX AG1X2 anionic resin showed that < 20% of the radioactivity was bound to this support. 13C- and 19F-nmr analysis of the non-bound radioactivity identified it to unchanged F-TAC, with bound radioactivity being due to polyanionic telomers arising from the hydrolysis of the amide function.(ABSTRACT TRUNCATED AT 250 WORDS)
3-(3-Hydroxy-2-(hydroxymethyl)phenyl)propanoic acid, 2-hydroxymethyl-3-hydroxy-(E)-cinnamic acid, and colletofurans A−E were isolated from Colletotrichum boninense AM-12−2. Colletofurans A−E are the first natural compounds featuring a 1-octyl-1,3-dihydroisobenzofuran core. Their structures were initially established by 1D/2D-NMR and HRESITOFMS. Mosher's ester method was used to determine the absolute configurations of secondary alcohols in colletofurans A−C. The structures of colletofurans A and B−E were further confirmed by DFT GIAO calculations and the X-ray crystalline sponge method, respectively.
The learning process in the 21 st century must be contextual and require the Higher-Order Thinking Skill (HOTS) to prepare students in their life situations. The aim of this research is to analyze the students' critical thinking skill in improving HOTS of undergraduate pharmacy students. This student's essential thinking skill including HOTS, knowledge of theoretical concepts, and skill of students in the learning process. This research was conducted towards the first-year students of pharmacy undergraduate with three major subjects, including cell biology, basic chemistry, and basic pharmaceuticals. The qualitative descriptive method with assessment, observation, and interview in collecting data was used in this research. The population sample made up of thirty-eight students. The categories of students' critical thinking are divided into a low, moderate, and high percentages. The study shows that higher-order thinking skill of students was improved when a learning process pushed in activating the student's critical thinking.
The labelling of 2-chloroethylisocyanate with 14C and 1% on the carbonyl group from 3-chloropropionic acid 14C and 13C is described. This isocyanate was used to synthesize 4-tert butyl[3-(2-chloro ethyl) ureido] benzene). RESUMELe 2-chloroethyl isocyanate a 8te marque par 1% ou 1% sur le groupe carbonyl partir de I'acide 3-chloropropionique 1% ou 13C afin de realiser le marquage du 4-terbutyl [3-(2-chloroethyl ureido] benzene).
SUMMARYFgTACg a Perfluoroalkylated telomer, was labeled by l 4 C and l 3 C on the carbonyl group from acrylic acid 14C. The synthesis of this compound was performed via a five steps procedure. The labelling yield calculated from the precursor (Ba 14 or 13C02) is in the range of 25-30 %. RESUMELe telomere perfluore FgTACg a et6 marque par 14C et 13C sur le groupe carbonyle a partir de I'acide acrylique 1%. La synthese est realisbe en cinq etapes A partir de BaCOg comme precurseur. Le rendement de marquage calcule par rapport au precurseur (Bal4CO2 ou 13CO3) est de I'ordre de 25 a 30 %.
Endophytic fungi are potential microorganisms in lead compounds investigation as research objects for antibacterial and antifungal drug candidates. These microorganisms are able to produce various secondary metabolites, moreover they can even be regulated according to the needs of researchers. This is an advantage of endophytic fungi with good adaptability response. This study aims to explore the antibacterial, antifungal and antioxidant activity of endophytic fungi from the branch of the Melinjo tree (Gnetum gnemon L.) by qualitative analysis. This study resulted in 13 potential endophytic fungi extracts to be explored further for their compounds. Based on the results of the TLC test of the fungal extracts with 10% vanillin in H2SO4 as a reagent, it showed that the dominant compounds were alkaloids and polyphenols. The antibacterial activity test of extracts of the endophytic fungi was carried out by the disc diffusion agar method against Staphylococcus aureus and Pseudomonas aeruginosa bacteria, while antifungal agents were used for Candida albicans and Aspergillus clavatus.. Meanwhile, the qualitative test of antioxidants from fungal extracts using the DPPH spray reagent showed positive results of 8 fungal extracts. Screening of endophytic fungi from melinjo represented a source of endophytes potential as antibacterial, antifungal and antioxidant to be developed in exploration of secondary metabolites from natural products of microbial.Keywords: antioxidant, antimicrobial, methanol extracts, endophytes fungi
FgTACg a Perfluoroalkylated telomer, was labeled by 14C and 13C on the carbonyl group from acrylic acid 14C. The synthesis of this compound was performed via a five steps procedure. The labelling yield calculated from the precursor (Ba 14 or 13C02) is in the range of 25-30 Yo. RESUMELe telomdre perfluore FgTACg a et6 marque par 14C et 13C sur le groupe carbonyle a partir de I'acide actylique 14C. La synthese est rdalisee en cinq &apes a partir de BaCOg cornme precurseur. Le rendement de marquage calcule par rapport au precurseur (Ba14C02 ou l3C03) est de I'ordre de 25 a 30 Yo.
Antioksidan merupakan senyawa-senyawa yang dapat mencegah terbentuknya radikal bebas yang akan menyerang dinding sel. Penelitian ini dilakukan untuk mengetahui aktivitas antioksidan pada buah sawo manila (Manilkara zapota L). Senyawa antioksidan yang ditemukan pada buah sawo manila adalah senyawa alkaloid, flavonoid, tanin, dan saponin. Desain penelitian ini menggunakan desain eksperimental di laboratorium farmasi Universitas Hamzanwadi. Sampel diekstraksi dengan etanol 96%, dilanjutkan dengan proses fraksinasi menggunakan kolom kromatografi. Eluen yang digunakan pada proses fraksinasi yaitu etil asetat, etil asetat-metanol, dan metanol. Pengujian aktivitas antioksidan dilakukan secara kualitatif dan kuantitatif. Hasil pengujian secara kualitatif menunjukkan semua sampel mengandung antioksidan karena terlihat warna kuning ketika disemprotkan DPPH pada plat KLT. Sedangkan hasil pengujian secara kuantitatif menunjukkan bahwa nilai IC50 fraksi I 46 ppm dengan kategori sangat kuat, nilai IC50 fraksi II 97 ppm dengan kategori kuat, nilai IC50 fraksi III 149 ppm dengan kategori sedang, dan nilai IC50 vitamin C 29 ppm dengan kategori sangat kuat. Kesimpulannya yaitu fraksi buah sawo manila (Manilkara zapota L) memiliki aktivitas antioksidan dengan kategori sangat kuat, kuat dan sedang.
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