In this study, the extraction of anthocyanin colorant from karanda fruit (Carissa carandas L.) was carried out and optimized with multiple single factor assays. Selected conditions for yield maximization consisted of ripen fruits with black-purple color, material size of thin slices (1.0–1.5 mm), solvent of EtOH 50%, material/ solvent ratio of 1:3, temperature of 50 °C, extraction time of 45 min, and two extraction cycles. The anthocyanin content in the extract was 277.2 mg/L, which is equivalent to 9.33 mg anthocyanin per gram of dry material. Aqueous solutions of the extract and dried extracts from Carissa carandas fruit were evaluated for stability at two temperature conditions, namely room temperature (30 ± 2 °C) and 45 °C. The temperature exerted great impact on color change, anthocyanin content and the degree of polymerization of anthocyanin. Aqueous solutions of extract with citric acid (3.0–5.0 g/L) were generally more color stable and less anthocyanin degradable than those without citric acid. In the DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging assay, The half maximal inhibitory concentration (IC50) of the dried extract was 87.56 μg/mL, which was approximately 29 times higher than that of vitamin C. After 3-month storage at −18 °C, IC50 of the dried extract was 173.67 μg/mL.
To assess the antimalarial sensitivity of Plasmodium falciparum in vivo and in vitro in a highly endemic area of southern Viet Nam, a field study was conducted (in 1999) at a rubber plantation in Binh Phuoc Province north of Ho Chi Minh City. Fifty patients were treated with either artesunate (4 mg/kg on day 0, then 2 mg/kg on day 1 to 4) or mefloquine (10 mg/kg at 0 h, then 5 mg/kg at 6 h), and their progress was followed for 28 days under standard WHO protocols. Blood spots were taken at baseline from all patients, as well as from those who redeveloped parasitaemia during follow-up, for polymerase chain reaction (PCR) determination of parasite genotypes to assist differentiation of re-infection from recrudescence. Both treatments cleared parasites within 5 days. Of the 25 mefloquine-treated patients, 2 (8%) re-presented with probable re-infections. For artesunate, 4 patients (16%) had re-infections and 5 (20%) had recrudescences. Sensitivity tests in vitro of pre-treatment P. falciparum isolates showed geometric mean IC50 values of 29, 38, 209 and 15 nmol/L for chloroquine (n = 32), mefloquine (n = 33), quinine (n = 31) and artemisinin (n = 31), respectively. There were significant correlations between IC50s for artemisinin and mefloquine (r = 0.72, P = 0.004), and chloroquine and quinine (r = 0.44, P = 0.05). These data show that, although mefloquine has been used for 10 years in Binh Phuoc Province, it remains fully effective, perhaps because an artemisinin derivative is commonly given at the same time. The recrudescence rate for artesunate is similar to those reported in other epidemiological contexts. The present in-vitro data imply that quinine remains effective and that reduced drug pressure has been associated with increased sensitivity of local strains of P. falciparum to chloroquine. Although from one hyperendemic area, these results may have implications for antimalarial prophylaxis and treatment strategies for residents and travellers to southern Viet Nam.
BackgroundArtemisinin derivatives have been used for malaria treatment in Vietnam since 1989. Reported malaria cases have decreased from 1,672,000 with 4,650 deaths in 1991, to 91,635 with 43 deaths in 2006. Current national guidelines recommend artemisinin-based combination therapy (ACT), although artesunate is still available as monotherapy through the private sector. Recent reports suggest that effectiveness of ACT and artesunate monotherapy has declined in western Cambodia. This study examined Plasmodium falciparum resistance patterns over 10 years in southwest Vietnam in infected patients treated with artemisinin compounds.MethodsThe study was conducted in two communes in Phuoc Long district, Binh Phuoc province, 100 km west of the Cambodian border. This was chosen as a likely site for emerging artemisinin resistance because of the high prevalence of P. falciparum malaria, and the length of time that artemisinin had been in use. In vivo and in vitro monitoring of P. falciparum susceptibility to anti-malarial drugs was conducted in 1998, 2001, 2004/5, and 2008/9. Patients with confirmed P. falciparum malaria received therapy with 5 or 7 days of artemisinin (1998 and 2001 respectively) or 7 days of artesunateResultsIn the four surveys, 270 patients were recruited and treated. The mean parasite clearance times differed between 1998, 2001 and 2004/5 (1.8, 2.3 and 2.1 days, P < 0.01) but not between 1998 and 2008/2009. The mean parasite clearance times were correlated with parasite density at day 0 (r = 0.4; P < 0.001). Treatment failure rates after PCR adjustment were 13.8%, 2.9%, 1.2%, and 0% respectively. Susceptibility of P. falciparum to artemisinin in in vitro tests was stable during the period, except for a rise in EC90 and EC99 in 2001.ConclusionsThis study showed stable levels of P. falciparum sensitivity to artemisinin compounds in the two sites over a ten-year period. The introduction of ACT in this area in 2003 may have protected against the development of artemisinin resistance. Adherence to the latest WHO and Vietnamese guidelines, which recommend ACT as first-line therapy in all malarious areas, and continued monitoring along the Vietnam-Cambodia border will be essential to prevent the spread of artemisinin resistance in Vietnam.
The addition of chalcone and amine components into indirubin-3′-oxime resulted in 15 new derivatives with high yields. Structures of new derivatives were also elucidated through 1D, 2D-NMR and HR-MS(eSi) spectra and X-ray crystallography. All designed compounds were screened for cytotoxic activity against four human cancer cell lines (HepG2, LU-1, SW480 and HL-60) and one human normal kidney cell line (HEK-293). Compound 6f exhibited the most marked cytotoxicity meanwhile cytotoxicity of compounds 6e, 6h and 6l was more profound toward cancer cell lines than toward normal cell. These new derivatives were further analyzed via molecular docking studies on GSK-3β enzyme. Docking analysis shows that most of the derivatives exhibited potential inhibition activity against GSK-3β with characteristic interacting residues in the binding site. The fast pulling of ligand scheme was then employed to refine the binding affinity and mechanism between ligands and GSK-3β enzyme. the computational results are expected to contribute to predicting enzyme target of the trial inhibitors and their possible interaction, from which the design of new cytotoxic agents could be created in the future. Cancer is ranked second globally as cause of death. The disease originated due to the inability of cells to control growth, often leading to the formation of cancerous tumors or liquid cancer. (i.e. leukemia and lymphoma cancer). Routines for cancer treatment consist of chemotherapy and radiotherapy where the former utilizes molecule-size drugs aiming at eradication and inhibition of cancer tumors. However, this treatment technique has been shown to suffer from several inherent shortcomings including the development of drug resistance, off-target toxicity and limited targeting capabilities 1,2. Glycogen synthase kinase-3 (GSK-3) is defined as a multifunctional serine/threonine protein kinase that regulates the phosphorylation of various cellular targets 3. The function of GSK-3 is essential for the development
This research aimed to optimize the total polyphenol content (TPC) extracted from soybean sprout powder under different experimental parameters, including ethanol concentration (60–100% v/v), extraction temperature (40–80 °C), extraction time (15–150 min), material:solvent ratio (1:4–1:10 g/mL), the number extraction cycles (1, 2 and 3 times), the age of sprout (0–7 days), and the used part of the sprout (cotyledon, hypocotyl, or radicle). The obtained results were used in response surface methodology, in combination with a central composite design, to model the total polyphenol content (TPC) with respect to three variables, including ethanol concentration, extraction temperature, and material:solvent ratio. The experimental conditions for optimal recovery of TPC consisted of ethanol concentration of 88% (v/v), extraction temperature of 59 °C, material:solvent ratio of 1:6.5 g/mL, extraction time of 60 min, and 2 cycles of maceration. In addition, for maximal TPC, the sprout should undergo the germination of 5 days and the radicle fraction should be used. Based on the suggested optimum conditions, the obtained and verified TPC was 19.801 mg genistein (GE)/g dry weight (d.w.). The obtained dried extract also exhibited low antioxidant activity.
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