Lamellarin O,a Pyrrole Alkaloid from an Australian Marine Sponge,Ianthella sp., Reverses BCRP Mediated Drug Resistance in Cancer Cells     

Xiao-Cong Huang  Xue Xiao  Yun-Kai Zhang  Tanaji T. Talele  Angela A. Salim  Zhe-Sheng Chen  Robert J. Capon 《Marine drugs》2014,12(7):3818-3837

ATP binding cassette (ABC) transporters, such as P-gp, BCRP and MRP1, can increase efflux of clinical chemotherapeutic agents and lead to multi-drug resistance (MDR) in cancer cells. While the discovery and development of clinically useful inhibitors has proved elusive to date, this molecular target nevertheless remains a promising strategy for addressing and potentially overcoming MDR. In a search for new classes of inhibitor, we used fluorescent accumulation and efflux assays supported by cell flow cytometry and MDR reversal assays, against a panel of sensitive and MDR human cancer cell lines, to evaluate the marine sponge co-metabolites 1–12 as inhibitors of P-gp, BCRP or MRP1 initiated MDR. These studies identified and characterized lamellarin O (11) as a selective inhibitor of BCRP mediated drug efflux. A structure–activity relationship analysis inclusive of the natural products 1–12 and the synthetic analogues 13–19, supported by in silico docking studies, revealed key structural requirements for the lamellarin O (11) BCRP inhibitory pharmacophore.  相似文献   

Organic Solvent and Laundry Detergent Stable Crude Protease from Nile Tilapia (Oreochromis niloticus) Viscera     

Tanaji Kudre 《Journal Of Aquatic Food Product Technology》2013,22(1):87-100

The objective of this study was to explore the characteristic activity of crude protease extracted from Nile tilapia viscera. The optimal temperature and pH of the crude protease from Nile tilapia viscera were 60°C and 8.0, respectively. The enzyme was stable to heat treatment up to 45°C and over a pH range of 7–11 for 30–120 min. The protease was effectively inhibited by phenylmethylsulfonyl fluoride (PMSF) and soybean trypsin inhibitor (SBTI). It was activated by Ca²⁺ and Fe²⁺, while inhibited in order by Hg²⁺ > Fe³⁺ > Cu²⁺ > Mn²⁺. The protease showed great stability toward Tween 20, Tween 80, and Triton X-100 and moderate stability toward sodium dodecyl sulfate (SDS) and hydrogen peroxide (H₂O₂)_. Nevertheless, it showed excellent stability and compatibility with various solid and liquid laundry detergents at temperatures from 30 to 50°C. The protease showed not only an improved activity but also a satisfied stability in 25% (v/v) organic solvents for 7 days at 37°C. At higher concentrations (50–75%), the protease activity was decreased by hydrophilic solvents, except dimethyl sulfoxide (DMSO), whereas it was enhanced by hydrophobic solvents. Thus, the crude protease is an excellent candidate as a biocatalyst for detergents, foods, pharmaceuticals, and environmental applications.  相似文献   

Recovery of Proteins from Rohu Processing Waste Using pH Shift Method: Characterization of Isolates     

Vijay Kumar Reddy Surasani  Anuj Tyagi  Tanaji Kudre 《Journal Of Aquatic Food Product Technology》2017,26(3):356-365

Yield and physicochemical characteristics of protein isolates recovered from rohu processing waste by acid- and alkali-aided protein solubilization methods were studied. pH 2.0 from acidic side and pH 13.0 from alkaline side resulted in maximum protein solubility, whereas minimum solubility was observed at pH 5.5. Except for pH 13.0, theoretical protein recovery was more than the actual recovery after centrifugation. Maximum protein recovery after the first centrifugation cycle was observed for pH 2.0 and pH 13.0, and the maximum protein recovery during the second centrifugation cycle was observed at precipitation pH 5.5 in both acidic and alkaline methods. Acidic and alkaline methods resulted in a total process recovery of 31.81% ± 0.001% and 31.11% ± 0.01%, respectively. Isolates prepared by acidic method had more whiteness and high foaming capacity, whereas isolates prepared using alkaline methods had less whiteness, tough texture, and high foaming stability. No microbial counts were detected in any of the isolates. Acid and alkaline methods described in this study can be used for the recovery of proteins from rohu processing waste with good yields and functionality.  相似文献   

Sustained-release biopolymer based formulations for <Emphasis Type="Italic">Bacillus sphaericus</Emphasis> Neide ISPC-8     

Ashok?B.?Hadapad  Ramesh?S.?Hire  N.?Vijayalakshmi  Tanaji?K.?DongreEmail author 《Journal of pest science》2011,84(2):249-255

Sustained-release biopolymer based formulations for an indigenous Bacillus sphaericus Neide ISPC-8 strain were developed and evaluated under laboratory conditions. These formulations were assessed for residual activity, response to UV-B radiation and shelf-life. The mosquitocidal activity of tested formulations showed a varied residual activity pattern against Culex quinquefasciatus Say larvae. The residual activity of unformulated spore-crystal suspension drastically decreased after 4 days whereas the formulated preparations persisted until 28 days. All the formulations except sodium alginate-based formulation showed more than 95% mortality within 48 h. Although the sodium alginate-based formulation showed delayed initial mortality, it persisted for a longer period of time (42 days). Based on the persistence studies, promising formulations based on sodium alginate, gelatin and acacia gum were selected for further evaluation. The respective LC₅₀ values of these three formulations were 0.085, 0.117, and 0.196 mg/l against C. quinquefasciatus after 48 h. The biopolymers combined with Congo red protected the spore-crystal moiety from UV-B radiation. These formulations were found to be stable up to 18 months when stored at room temperature. Thus, these biopolymers could serve as suitable ingredients for development of biopesticide based on B. sphaericus ISPC-8.  相似文献