Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active c...Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active components from Chinese medicinal plants ' ,we have examined the aerial parts of this herb, leading to the isolation of a clerodane-typediterpene, 18, 19-dihydroxy-5α, 10β-neo-cleroda-3, 13 (l4)-dien-16, 15-butenolide (1). In thispaper we report the structural elucidation, and the antitumor and antibacterial activities of thiscompound. It was found that 1 possesses moderate cytotoxicity against human leukemia cells (HL-60)and activity against microorganisms.展开更多
The research on discovery and development of new treatments for cutaneous leishmaniasis has been declared as priority. Using bioinformatics approaches, this study aimed to identify antileishmanial activity in drugs th...The research on discovery and development of new treatments for cutaneous leishmaniasis has been declared as priority. Using bioinformatics approaches, this study aimed to identify antileishmanial activity in drugs that are currently used as anti-inflammatory and wound healing by such anti-Leishmania activity was validated by in vitro and in vivo assays. In silico analysis identified 153 compounds from which 87 were selected by data mining of DrugBank database, 22 and 44 were detected by PASS (http://pass.cribi.unipd.it) and BLAST (http://blast.ncbi.nlm.nih. gov/) alignment, respectively. The majority of identified drugs are used as skin protector, anti-acne, anti-ulcerative (wound healer) or anti-inflammatory and few of them had specific antileishmanial activity. The efficacy as antileishmanial was validated in vitro in 12/23 tested compounds and in all seven compounds that were evaluated in in vivo assays. Notably, this is the first report of antileishmanial activity for adapalene. In conclusion, bioinformatics tools not only can help to reduce time and cost of the drug discovery process but also may increase the chance that candidates identified in silico which have a validated antileishmanial activity by combining different biological properties.展开更多
Objective:To investigate the effect of Shenqi Compound Formula (SCF) on peroxisome proliferators-activated receptor γ (PPARγ) in white adipose tissue of rats with macrovascular lesion in early stage of diabetes. Met...Objective:To investigate the effect of Shenqi Compound Formula (SCF) on peroxisome proliferators-activated receptor γ (PPARγ) in white adipose tissue of rats with macrovascular lesion in early stage of diabetes. Methods: Corresponding treatment was given to rats in model group, Ramipril group, normal control group, low dosage SCF group and high dosage SCF group respectively for 32 days. The expressions of PPARγ and adiponectin Messenger RNA (mRNA) were detected by real-time reverse transcriptase poly-merase chain reaction. Results: The expressions of PPARγ and adiponectin mRNA increased significantly in both low and high dosage SCF groups as compared with the model group, and a positive linear correlation was found between the expressions of PPARγ and adiponectin mRNA. Conclusions: SCF can prevent macrovascular lesion in early stage of diabetes, which is possibly related with up-regulating expressions of PPARγ and activating PPARγ.展开更多
Aqueous extracts from the native Chilean Quillaja saponaria tree are used orally and topically to treat lung inflammatory problems and toothache. This study aimed to corroborate their presumed anti-inflammatory activi...Aqueous extracts from the native Chilean Quillaja saponaria tree are used orally and topically to treat lung inflammatory problems and toothache. This study aimed to corroborate their presumed anti-inflammatory activity, identify their active ingredients and validate their use. The topical anti-inflammatory activity of a commercial partially purified Quillaja saponin aqueous extract (Ultra Dry 100Q, UD), the crude acid hydrolysate (H-100Q) of this material, its two most abundant sapogenins QA (quillaic acid) and PA (phytolaccagenic acid), and two formulations containing QA were subjected to topical assays for the inhibition ofmurine ear inflammation elicited by AA (arachidonic acid) or TPA (phorbol ester). The dose-dependent anti-inflammatory activity of QA was confirmed in both AA (maximal effect 92.1%) and TPA (maximal effect 62.2%) assays, and PA showed significant anti-inflammatory activity against AA (46.5%). Two dermo pharmaceutical formulations containing 8% w/v QA as the active ingredient--a cream and a gel--also exhibited significant anti-inflammatory effects in the TPA (50.8%) and AA (39.5%) assays.展开更多
文摘Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active components from Chinese medicinal plants ' ,we have examined the aerial parts of this herb, leading to the isolation of a clerodane-typediterpene, 18, 19-dihydroxy-5α, 10β-neo-cleroda-3, 13 (l4)-dien-16, 15-butenolide (1). In thispaper we report the structural elucidation, and the antitumor and antibacterial activities of thiscompound. It was found that 1 possesses moderate cytotoxicity against human leukemia cells (HL-60)and activity against microorganisms.
文摘The research on discovery and development of new treatments for cutaneous leishmaniasis has been declared as priority. Using bioinformatics approaches, this study aimed to identify antileishmanial activity in drugs that are currently used as anti-inflammatory and wound healing by such anti-Leishmania activity was validated by in vitro and in vivo assays. In silico analysis identified 153 compounds from which 87 were selected by data mining of DrugBank database, 22 and 44 were detected by PASS (http://pass.cribi.unipd.it) and BLAST (http://blast.ncbi.nlm.nih. gov/) alignment, respectively. The majority of identified drugs are used as skin protector, anti-acne, anti-ulcerative (wound healer) or anti-inflammatory and few of them had specific antileishmanial activity. The efficacy as antileishmanial was validated in vitro in 12/23 tested compounds and in all seven compounds that were evaluated in in vivo assays. Notably, this is the first report of antileishmanial activity for adapalene. In conclusion, bioinformatics tools not only can help to reduce time and cost of the drug discovery process but also may increase the chance that candidates identified in silico which have a validated antileishmanial activity by combining different biological properties.
文摘Objective:To investigate the effect of Shenqi Compound Formula (SCF) on peroxisome proliferators-activated receptor γ (PPARγ) in white adipose tissue of rats with macrovascular lesion in early stage of diabetes. Methods: Corresponding treatment was given to rats in model group, Ramipril group, normal control group, low dosage SCF group and high dosage SCF group respectively for 32 days. The expressions of PPARγ and adiponectin Messenger RNA (mRNA) were detected by real-time reverse transcriptase poly-merase chain reaction. Results: The expressions of PPARγ and adiponectin mRNA increased significantly in both low and high dosage SCF groups as compared with the model group, and a positive linear correlation was found between the expressions of PPARγ and adiponectin mRNA. Conclusions: SCF can prevent macrovascular lesion in early stage of diabetes, which is possibly related with up-regulating expressions of PPARγ and activating PPARγ.
文摘Aqueous extracts from the native Chilean Quillaja saponaria tree are used orally and topically to treat lung inflammatory problems and toothache. This study aimed to corroborate their presumed anti-inflammatory activity, identify their active ingredients and validate their use. The topical anti-inflammatory activity of a commercial partially purified Quillaja saponin aqueous extract (Ultra Dry 100Q, UD), the crude acid hydrolysate (H-100Q) of this material, its two most abundant sapogenins QA (quillaic acid) and PA (phytolaccagenic acid), and two formulations containing QA were subjected to topical assays for the inhibition ofmurine ear inflammation elicited by AA (arachidonic acid) or TPA (phorbol ester). The dose-dependent anti-inflammatory activity of QA was confirmed in both AA (maximal effect 92.1%) and TPA (maximal effect 62.2%) assays, and PA showed significant anti-inflammatory activity against AA (46.5%). Two dermo pharmaceutical formulations containing 8% w/v QA as the active ingredient--a cream and a gel--also exhibited significant anti-inflammatory effects in the TPA (50.8%) and AA (39.5%) assays.