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Chemical compositions and biological activities of essential oils obtained from some Apiaceous and Lamiaceous plants collected in Thailand

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Asian Pacific Journal of Tropical Medicine 2018年第8期11卷 486-494页

作者： Nawanit Thanaseelungkoon Jakaphun Julsrigival Kulwadee Phannachet Sunee Chansakaow Department of pharmaceutical sciences Faculty of Pharmacy Chiang Mai University Department of Microbiology Faculty of Medicine Chiang Mai University

Objective: To determine the chemical composition, as well as the antioxidant, antityrosinase and antibacterial activities of essential oils obtained from some Apiaceous and Lamiaceous plants collected in Thailand. Methods: The essential oils of the specified spices and aromatic herbs were obtained by hydro-distillation, and their chemical constituents were analyzed by gas chromatography/mass spectrometry. Antioxidant assays were based on the scavenging effects of 2,2-Diphenyl-1-picrylhydrazyl(DPPH) and 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)(ABTS) free radicals as well as the lipid oxidation inhibition of β-carotene bleaching by linoleic acid. Tyrosinase enzyme inhibition was evaluated by the dopachrome method. Broth microdilution technique was performed for the purposes of studying microbial growth inhibition against the isolated bacterial strains. Results: The essential oils of Elsholtzia stachyodes, Coleus amboinicus(I) and Trachyspermum ammi presented a high degree of potency in DPPH, ABTS and β-carotene bleaching assays. The Trachyspermum ammi oil, which mainly contained thymol(49.04%) and p-cymene(22.06%), proved to be the most effective in terms of antibacterial activity. The major compositions of Coleus amboinicus(I) were carvacrol(51.57%), γ-terpinene(18.04%) and p-cymene(7.81%); while thymol(43.76%) and γ-terpinene(24.61%) were identified as the major components of Elsholtzia stachyodes oil, with p-cymene(6.73%) being identified as a minor constituent. Moreover, Cuminum cyminum oil containing cuminaldehyde(49.07%) and Elsholtzia communis oil composed with geranial(44.74%) and neral(35.27%) as the major components displayed a specific ability for the inhibition of the mushroom tyrosinase enzyme. Conclusions: The results indicated that these bioactive essential oils obtained from indigenous herbs are of significant interest as alternative raw materials in food, cosmetic and medicinal products.

关键词： Essential oil Apiaceae Lamiaceae Antioxidant activity Antityrosinase activity Antibacterial activity

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Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 agonists as potential neuroprotective agents

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Neural Regeneration Research 2019年第5期14卷 745-748页

作者： Shaker A.Mousa Bassam M.Ayoub pharmaceutical Research Institute Albany College of Pharmacy and Health Sciences The Center for Drug Research and Development (CDRD) Pharmaceutical Chemistry Department Faculty of Pharmacy The British University in Egypt

Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists is a breakthrough in the field of neural regeneration research increasing glucagon like peptide-1 bioavailability, hence its neuroprotective activities. In this article, the authors suggest not only crossing blood-brain barrier and neurodegenerative disease as off target for dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists, but also for ophthalmic preparations for diabetic retinopathy, which may be the latest breakthrough in the field if prepared and used in an appropriate nano-formulation to target the retinal nerves. The relation of neurodegenerative diseases' different mechanisms to the dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists should be further examined in preclinical and clinical settings. The repositioning of already marketed antidiabetic drugs for neurodegenerative diseases should save the high cost of the time-consuming normal drug development process. Drug repositioning is a hot topic as an alternative to molecular target based drug discovery or therapeutic switching. It is a relatively inexpensive pathway due to availability of previous pharmacological and safety data. The glucagon like peptide-1 produced in brain has been linked to enhanced learning and memory functions as a physiologic regulator in central nervous system by restoring insulin signaling. Intranasal administration of all marketed gliptins(or glucagon like peptide-1 receptor agonists) may show enhanced blood-brain barrier crossing and increased glucagon like peptide-1 levels in the brain after direct crossing of the drug for the olfactory region, targeting the cerebrospinal fluid. Further blood-brain barrier crossing tests may extend dipeptidyl peptidase-4 inhibitors' effects beyond the anti-hyperglycemic control to intranasal spray, intranasal powder, or drops targeting the blood-brain barrier and neurodegenerative diseases wit

关键词： repositioning DPP-4 inhibitors GLP-1RA neural regeneration blood-brain barrier Parkinson’s disease Alzheimer’s disease diabetic retinopathy

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Design, synthesis and MAO inhibitory activity of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives

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Chinese Chemical Letters 2017年第7期28卷 1528-1532页

作者： Vishnu Nayak Badavath Chandrani Nath Narayana Murthy Ganta Gulberk Ucar Barij Nayan Sinha Venkatesan Jayaprakash Department of pharmaceutical sciences & Technology Birla Institute of Technology Department of Biochemistry Faculty of Pharmacy Hacettepe University

A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were found to be selective towards h MAO-B, while two were non-selective（6 and 20） and one（18）selective towards h MAO-A. Compound 17（Ki = 0.10 0.01 mmol/L） was found to be equally potent and selective towards h MAO-B, when compared with the standard drug Selegiline（Ki = 0.12 0.01 mmol/L）.Nature and position of substitution in aryl ring at 2nd position of benzofuranone influences h MAO-B inhibitory potency, while their structural bulkiness influences selectivity between h MAO-A and h *** docking simulation was also carried out to understand the interaction of inhibitor with the enzyme at molecular level, and we found the docking results were in good agreement with the experimental values. Comparison of the activity profile of the aurones with their corresponding flavones reported earlier by our group revealed that there exists no difference in potency as well as selectivity.

关键词： 2-(Arylmethylidene)-2 3-dihydro-1-benzofuran-3-one derivatives hMAO inhibitors Molecular docking simulation Synthesis

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An edible green algae polysaccharide CRVP from Caulerpa racemosa var. peltate induced apoptosis of liver cancer cells Hepa1-6 by regulating glutathione metabolism

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Food Science and Human Wellness 2024年

作者： Xuewei Xia Heying Zhou Rongxin Zhang Xiaoyong Zhang Baojun Xu Io Nam Wong Riming Huang Guangdong Provincial Key Laboratory of Food Quality and Safety， College of Food Science， South China Agricultural university Department of pharmacy， Guangdong Second Provincial General Hospital Department of Colorectal Surgery， Sun Yat-sen university Cancer Center State Key Laboratory of Oncology in South China Joint Laboratory of Guangdong Province and Hong Kong Region on Marine Bioresource Conservation and Exploitation， College of Marine sciences， South China Agricultural university Food Science and Technology Program， BNU-HKBU United International College faculty of Medicine， Macau university of Science and Technology

Algal polysaccharides are an essential active substance in food nutrition and even pharmaceutical activity research due to wide sources， low toxicity， and no side effects. In our previous research， we identified the chemical structure and studied the immunomodulatory mechanism of the polysaccharide CRVP from edible green algae Caulerpa racemosa var. peltata. In this study， we further investigated the cytotoxicity and potential mechanism of CRVP against Hepa1-6 cells. Metabolomics analysis showed that CRVP might affect glutathione metabolism-related pathways. CRVP significantly up-regulated oxidized glutathione （GSSG） and down-regulated reduced glutathione （GSH） in Hepa1-6 cells， increasing the ratio of GSSG to GSH and intracellular reactive oxygen species. The potential anti-liver cancer mechanism is that CRVP may affect redox homeostasis and lead to apoptosis by inhibiting glutathione reductase or System Xc-. Based on the known immunomodulatory mechanism of CRVP， this study can provide a material basis for adjuvant therapeutic nutritional agents with immune-enhancing anti-cancer activity.

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Development of novel cationic microemulsion as parenteral adjuvant for influenza vaccine

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Asian Journal of pharmaceutical sciences 2020年第5期15卷 591-604页

作者： Sakalanunt Lamaisakul Angkana Tantituvanont Vimolmas Lipipun Garnpimol Ritthidej Department of Pharmaceutics and Industrial pharmacy Faculty of Pharmaceutical SciencesChulalongkorn UniversityBangkok 10330Thailand Department of Biochemistry and Microbiology Faculty of Pharmaceutical SciencesChulalongkorn UniversityBangkok 10330Thailand

Squalene-based oil-in-water(O/W)emulsions have been used as effective and safe adjuvants in approved influenza ***,there are concerns regarding the safety and side effects of increasing risk of *** present study,novel O/W microemulsions(MEs)containing wheat germ oil,D-alpha tocopheryl polyethylene glycol 1000 succinate(TPGS)and Cremophor EL(CreEL)or Solutol HS15 were formulated with/without a cationic surfactant,cetyltrimethylammonium bromide(CTAB)and then sterilized by *** physical properties and biological efficacies were *** results demonstrated that autoclaving reduced the droplet size to^20 nm with narrow size distributions resulting in monodisperse systems with good stability up to 3 *** activity,viscosity,pH,and osmolality were appropriate for parenteral *** serum albumin(BSA),a model antigen,after mixing with MEs retained the protein integrity,assessed by SDS-PAGE and CD *** percentages of 28 SC cell viability were observed from CreEL-based *** of FITC-BSA-MEs increased with the increasing concentration of CTAB confirmed by CLSM ***,cationic CreEL-based MEs could induce Th1 cytokine synthesis with an increase in TNF-α and IL-12 levels and a decrease in IL-10 *** vivo immunization study in mice of adjuvants admixed with influenza virus solution revealed that nonionic and selected cationic CreEL-MEs enhanced immune responses as measured by influenza-specific serum antibody titers and hemagglutination inhibition ***,cationic CreEL-based ME showed better humoral and cellular immunity with higher IgG2 a titer than nonionic CreEL-based ME and antigen *** differences in immune responses were observed between mice immunized with selected cationic CreEL-based ME and marketed *** addition,the selected ME induced antigen-sparing while retained immune stimulating effects compared to antigen *** inflammatory change in muscle fibe

关键词： Cationic microemulsion Adjuvant Influenza virus Vaccine

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A systematic review of the efficacy and safety of herbal medicines used in the treatment of obesity

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World Journal of Gastroenterology 2009年第25期15卷 3073-3085页

作者： Shirin Hasani-Ranjbar Neda Nayebi Bagher Larijani Mohammad Abdollahi Endocrinology and Metabolism Research Center and Faculty of MedicineTehran University of Medical Sciences faculty of pharmacy and Pharmaceutical Sciences Research CentreTehran University of Medical Sciences

This review focuses on the efficacy and safety of effective herbal medicines in the management of obesity in humans and animals. PubMed, Scopus, Google Scholar, Web of Science, and IranMedex databases were searched up to December 30, 2008. The search terms were ＂obesity＂ and （＇herbal medicine＂ or ＂plant＂, ＂plant medicinal＂ or ＂medicine traditional＂） without narrowing or limiting search elements. All of the human and animal studies on the effects of herbs with the key outcome of change in anthropometric measures such as body weight and waist-hip circumference, body fat, amount of food intake, and appetite were included. In vitro studies, reviews, and letters to editors were excluded. Of the publications identified in the initial database, 915 results were identified and reviewed, and a total of 77 studies were included （19 human and 58 animal studies）. Studies with Cissus quadrangularis （CQ）, Sambucus nigra, Asparagus officinalis, Garcinia atroviridis, ephedra and caffeine, Slimax （extract of several plants including Zingiber officinale and Bofutsushosan） showed a significant decrease in body weight. In 41 animal studies, significant weight loss or inhibition of weight gain was found. No significant adverse effects or mortality were observed except in studies with supplements containing ephedra, caffeine and Bofutsushosan. In conclusion, compounds containing ephedra, CQr ginseng, bitter melon, and zingiber were found to be effective in the management of obesity. Attention to these natural compounds would open a new approach for novel therapeutic and more effective agents.

关键词： Animal Herbal medicine Human Obesity

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Profile of Multidrug Resistant Bacteria in Bukavu Hospitals and Antimicrobial Susceptibility to Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Staphylococcus aureus

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Advances in Microbiology 2024年第4期14卷 209-225页

作者： Christian Ahadi Irenge Freddy Bikioli Patient Birindwa Mulashe Félicien Mushagalusa Kasali Patient Wimba Aksanti Lwango Yves Coppieters Justin Ntokamunda Kadima Department of pharmacy and Public Health Official University of Bukavu Bukavu Democratic Republic of the Congo Department of Tropical Medecine Faculty of Medecine University of Kinshasa Kinshasa Democratic Republic of the Congo Department of Microbiology Faculty of Medicine Official University of Bukavu Bukavu Democratic Republic of the Congo Department of Medical Biology Higher Institute of Medical Technics Bukavu Democratic Republic of the Congo School of Public Health Free University of Bruxelles Bruxelles Belgium School of Medicine College of Medicine and Health Sciences University of Rwanda Huye Rwanda

Objective: To evaluate the spread of Multidrug-Resistant (MDR) bacterial infections in Bukavu hospitals and test antimicrobial susceptibility patterns of some isolates to usual marketed antibiotics. Methods: The prevalence of MDR strains was determined by using general antimicrobial susceptibility data collected from 3 hospital laboratories. The susceptibility of some isolates to usual antibiotics was processed by agar diffusion method with standard E. coli ATCC8739 and standard antibiotics discs as controls. The tested antibiotics were ampicillin, ceftriaxone, gentamicin, chloramphenicol and ciprofloxacin. Results: At the 3 hospitals, 758 tests were realized in urine, pus, stool, FCV, blood, LCR, split and FU specimens;46 strains were unidentified and 712 strains were identified. Of 712 identified strains, 223 (31.4%) were MDR or XDR strains including Escherichia coli, Klebsiella pneumoniae, Enterobacter, Proteus mirabilis, Salmonella enterica, Pseudomonas aeruginosa, Citrobacter freundii, Morganella morganii, Enterococcus faecalis and E. faecium, Neisseria gonorrohoae, Staphylococcus aureus, coagulase-negative, staphylococci, Streptococcus pneumoniae and Streptococcus pyogenes. Of the infected patients, 36 (21.5%) children were under 16 years and 188 (78.5%) adults were predominately women (58.5%). The susceptibility test showed that all strains but S. aureus were resistant to ampicillin and amoxicillin and ciprofloxacin. Gentamicin, ceftriaxone, and chloramphenicol remain partially active (27% - 80%) against P. mirabilis, E. coli and P. aeruginosa. The resistance is more likely related to strain mutation than to pharmaceutical quality of the antibiotics prescribed. Conclusion: Both data from hospital laboratories and in vitro post-testing findings confirmed the ongoing elevated prevalence of MDR strains in Bukavu. The causes of antibiotic misuse and socio-economic determinants of the phenomenon of resistance should be scrutinized in order to take adequate strateg

关键词： Prevalence Antimicrobials Multi-Resistance Bacterial Sensitivity Bukavu DRC

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Multitarget therapeutic strategies for Alzheimer's disease

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Neural Regeneration Research 2019年第3期14卷 437-440页

作者： Mostafa M.Ibrahim Moustafa T.Gabr Department of Pharmacognosy Faculty of Pharmacy Mansoura University Department of Basic pharmaceutical and Toxicological sciences College of Pharmacy University of Louisiana at Monroe Department of Medicinal Chemistry Faculty of Pharmacy Mansoura University Department of Chemistry University of Iowa

Neurodegenerative diseases such as Alzheimer's, Huntington's and Parkinson's diseases have multifaceted nature because of the different factors contributing to their progression. The complex nature of neurodegenerative diseases has developed a pressing need to design multitarget-directed ligands to address the complementary pathways involved in these diseases. The major enzyme targets for development of therapeutics for Alzheimer's disease are cholinesterase and β-secretase enzymes. In this review, we discuss recent advances in profiling single target inhibitors based on these enzymes to multitarget-directed ligands as potential therapeutics for this devastating disease. In addition, therapeutics based on iron chelation strategy are discussed as well.

关键词： multitarget-directed ligands acetylcholinesterase β-secretase Alzheimer's disease hybridization neurodegenerative diseases tacrine brain permeability

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A Randomized,Double Blinded,Placebo-Controlled Clinical Trial of Silymarin in Ulcerative Colitis

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Chinese Journal of Integrative Medicine 2015年第12期21卷 902-906页

作者： Mansoor Rastegarpanah Reza Malekzadeh Homayoun Vahedi Maryam Mohammadi Elham Elahi Meghedi Chaharmahali Tahereh Safarnavadeh Mohammad Abdollahi Digestive Disease Research Center Tehran University of Medical Sciences faculty of pharmacy Tehran University of Medical Sciences pharmaceutical sciences Research Center Tehran University of Medical Sciences Islamic Azad university Pharmaceutical Branch

Objective： To evaluate the clinical efficacy of silymarin in ulcerative colitis （UC） patients. Methods： A randomized double blinded placebo-controlled clinical trial was conducted in 80 UC patients whose disease had been documented and were in remission state between September 2009 and October 2010. Patients were assigned to silymarin group （42 cases） and placebo group （38 cases） using a random number table. Either silymarin （140 mg） or placebo （lactose mono-hydrate, corn starch magnesium stearate） tablets were given once daily for 6 months along with their standard therapy. The efficacies were assessed by disease activity index （DAI）, frequency difference of the disease flare-up, and paraclinical data. Results： Ten patients （4 in the silymarin group due to nausea and 6 in the placebo group due to disease flare-up and abdominal pain） discontinued the study. An improvement in hemoglobin level （11.8± 1.6 g/dL vs. 13.4± 1.2 g/dL, P〈0.05） and erythrocyte sedimentation rate （23.7 ＋_ 11.5 mm/h vs.10.8＋ 3.2 mm/h, P〈0.05） was observed in the silymarin group but not in the placebo group. DAI significantly decreased in the silymarin group and reached from 11.3 ± 3.5 to 10.7±2.8 （P〈0.05）. Thirty-five out of 38 patients in the silymarin group were in complete remission with no flare-up after 6 months as compared to 21 out of 32 patients in the placebo group （P=0.5000）. Conclusion： Silymarin as a natural supplement may be used in UC patients to maintain remission.

关键词： silymarin ulcerative colitis randomized controlled trial

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A review of the efficacy of traditional Iranian medicine forinflammatory bowel disease

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World Journal of Gastroenterology 2010年第36期16卷 4504-4514页

作者： Roja Rahimi Mohammad Abdollahi Mohammad Reza Shams-Ardekani faculty of Traditional Medicine Tehran University of Medical SciencesTehran ***Iran faculty of pharmacy Pharmaceutical Sciences Research CenterEndocrinology and Metabolism Research InstituteTehran University of Medical SciencesTehran ***Iran

The etiology of inflammatory bowel disease(IBD) is not yet known,but many factors such as defects in the immune system,oxidative stress,microbial content in the gastrointestinal tract,nuclear factor(NF)-κB,nitric oxide(NO),cyclooxygenase-2(Cox-2),and leukotriene B4(LB4) are thought to play a role in its *** traditional Iranian medicine(TIM),several medicinal plants are thought to be effective for the treatment of *** this study,information on all of these remedies were derived from all available old sources such as documents or notes and books and were added to the information derived from modern medical databases covering all in vitro,in vivo and clinical *** some of these plants,only one or two mechanisms of action have been found such as in Cassia fistula,Lepidium sativum,and Bunium ***,for some plants various mechanisms of action are *** example,Commiphora mukul is effective in IBD due to its immunomodulatory,antioxidant,and antibacterial properties and it decreases NF-κB,NO and *** herb,Plantago ovata,has immunomodulatory,antioxidant,anti-inflammatory and wound healing activities and decreases NO and *** the mechanisms of action of these plants,the combination of some of them may be useful because of their many mechanisms of action such as Pistacia lentiscus,Bunium persicum,Solanum nigrum,Plantago ovata,Boswellia,Solanum nigrum,Plantago ovata and Commiphora *** some of the herbal products used in TIM such as oleogum resin from Commiphora myrrha,seeds of Ocimum basilicum,seeds of Linum usitatissimum,gum resin of Dracaena cinnabari,seeds of Plantago major,seeds of Lallementia royleana,and seeds of Allium porrum,there is no or not enough studies to confirm their benefits in *** is suggested that an evaluation of the effects of these plants on different aspects of IBD should be performed.

关键词： Herbal medicine Inflammatory bowel disease Medicinal plants Traditional Iranian medicine

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