The rapid appraisal method was used to identity the botanicals used ethnomedicinally from a total of 300 randomly selected respondents drawn from the existing three geo-political zones of Ekiti State, Nigeria. The res...The rapid appraisal method was used to identity the botanicals used ethnomedicinally from a total of 300 randomly selected respondents drawn from the existing three geo-political zones of Ekiti State, Nigeria. The results obtained revealed that about 40% of the 71 botanicals identified presently rare. Most of the presently abundant botanicals are species primarily cultivated for other purpose other than medicine. Most of the identified species are valued for their curative effects on malaria and fever, the predominant diseases in the study area. The need for the conservation of the rare species cannot be over emphasised as most rural dwellers in the study area depend mostly on herbs from these species. Strategies towards the attainment of this goal are proposed.展开更多
Aim: To study the pharmacokinetic (PK) properties in rabbits treated with N-Ile^1-Thr^2-63-desulfato-r-hirudin (rH) newly developed in China by means of bioassay in order to provide preclinical experiment basis f...Aim: To study the pharmacokinetic (PK) properties in rabbits treated with N-Ile^1-Thr^2-63-desulfato-r-hirudin (rH) newly developed in China by means of bioassay in order to provide preclinical experiment basis for its development as a novel anticoagulant agent. Methods: rH plasma concentration was determined using bioassay based on ex vivo antithrombin activity of rH. Normal rabbits received iv rH 4.0, 2.0 and 1.0 mg/kg or sc rH 2.0 mg/kg, respectively. The rabbits with acute severe renal failure were given iv rH 2.0 mg/kg. Results: The bioassay described in this paper met requirements for study of PK in rabbits. The major PK parameters after iv dosing were as follows: t1/2p 58.4-59 min. Vd 0.09-0.12 L/kg, CL 0.0035-0.0040 L/(kg·min); AUC were proportional to the doses, ti/2 and CL did not change significantly with the doses. The sc bioavailability reached 94%. The rabbits suffering from acute severe renal failure presented 11-fold longer t1/2p and 13-fold greater.4 UC than normal healthy rabbits. Conclusion: rH exhibited rapid elimination, distribution was only limited to extracellular space and good absorption from sc site. The excretion ofrH by kidneys played a very important role in the elimination of rH. The PK ofrH could be described by the two- and one-compartment model after iv and sc dosing, respectively, and folio,wed linear kinetics.展开更多
Until recently, little was known about the fungi found in shark gills and their biomedicinal potential. In this article, we described the isolation, bioactivity, diversity, and secondary metabolites of bioactive fungi...Until recently, little was known about the fungi found in shark gills and their biomedicinal potential. In this article, we described the isolation, bioactivity, diversity, and secondary metabolites of bioactive fungi from the gill of a shark (Carcharodon carcharias). A total of 115 isolates were obtained and grown in 12 culture media. Fifty-eight of these isolates demonstrated significant activity in four antimicrobial, pesticidal, and cytotoxic bioassay models. Four randomly selected bioactive isolates inhibited human cancer cell proliferation during re-screening. These active isolates were segregated into 6 genera using the internal transcribed spacer-large subunit (ITS-LSU) rDNA-sequence BLAST comparison. Four genera, Penicillium, Aspergillus, Mucor, and Chaetomium were the dominant taxa. A phylogenic tree illustrated their intergenera and intragenera genetic diversity. HPLC-DAD-HRMS analysis and subsequent database searching revealed that nine representative strains produced diverse bioactive compound profiles. These results detail the broad range of bioactive fimgi found in a shark's gills, revealing their biopharmaceutical potential. To the best of our knowledge, this is the first study characterizing shark gill fungi and their bioactivity.展开更多
文摘The rapid appraisal method was used to identity the botanicals used ethnomedicinally from a total of 300 randomly selected respondents drawn from the existing three geo-political zones of Ekiti State, Nigeria. The results obtained revealed that about 40% of the 71 botanicals identified presently rare. Most of the presently abundant botanicals are species primarily cultivated for other purpose other than medicine. Most of the identified species are valued for their curative effects on malaria and fever, the predominant diseases in the study area. The need for the conservation of the rare species cannot be over emphasised as most rural dwellers in the study area depend mostly on herbs from these species. Strategies towards the attainment of this goal are proposed.
基金Project (No. 96-C02-01-05A) supported by the National NaturalScience Foundation of China
文摘Aim: To study the pharmacokinetic (PK) properties in rabbits treated with N-Ile^1-Thr^2-63-desulfato-r-hirudin (rH) newly developed in China by means of bioassay in order to provide preclinical experiment basis for its development as a novel anticoagulant agent. Methods: rH plasma concentration was determined using bioassay based on ex vivo antithrombin activity of rH. Normal rabbits received iv rH 4.0, 2.0 and 1.0 mg/kg or sc rH 2.0 mg/kg, respectively. The rabbits with acute severe renal failure were given iv rH 2.0 mg/kg. Results: The bioassay described in this paper met requirements for study of PK in rabbits. The major PK parameters after iv dosing were as follows: t1/2p 58.4-59 min. Vd 0.09-0.12 L/kg, CL 0.0035-0.0040 L/(kg·min); AUC were proportional to the doses, ti/2 and CL did not change significantly with the doses. The sc bioavailability reached 94%. The rabbits suffering from acute severe renal failure presented 11-fold longer t1/2p and 13-fold greater.4 UC than normal healthy rabbits. Conclusion: rH exhibited rapid elimination, distribution was only limited to extracellular space and good absorption from sc site. The excretion ofrH by kidneys played a very important role in the elimination of rH. The PK ofrH could be described by the two- and one-compartment model after iv and sc dosing, respectively, and folio,wed linear kinetics.
基金Supported by the National Natural Science Foundation of China(No.20902009)the National Science Foundation for Post-Doctoral Scientists of China(Nos.2011M500051,2012T50258)+2 种基金the Yang Fan Scarce Top Talent Project of Guangdong Province(to ZHANG Yi)the Program for Scientific Research Start-up Funds of Guangdong Ocean University(GDOU)(to ZHANG Yi)the Natural Science Research Project of GDOU(No.C14519)
文摘Until recently, little was known about the fungi found in shark gills and their biomedicinal potential. In this article, we described the isolation, bioactivity, diversity, and secondary metabolites of bioactive fungi from the gill of a shark (Carcharodon carcharias). A total of 115 isolates were obtained and grown in 12 culture media. Fifty-eight of these isolates demonstrated significant activity in four antimicrobial, pesticidal, and cytotoxic bioassay models. Four randomly selected bioactive isolates inhibited human cancer cell proliferation during re-screening. These active isolates were segregated into 6 genera using the internal transcribed spacer-large subunit (ITS-LSU) rDNA-sequence BLAST comparison. Four genera, Penicillium, Aspergillus, Mucor, and Chaetomium were the dominant taxa. A phylogenic tree illustrated their intergenera and intragenera genetic diversity. HPLC-DAD-HRMS analysis and subsequent database searching revealed that nine representative strains produced diverse bioactive compound profiles. These results detail the broad range of bioactive fimgi found in a shark's gills, revealing their biopharmaceutical potential. To the best of our knowledge, this is the first study characterizing shark gill fungi and their bioactivity.