Vitamin-D is known to promote innate immune responses by acting as a cofactor of VDR for induction of antimicrobial peptides like cathelicidin. Close household contacts of pulmonary tuberculosis patients are at high risk of active infection, Therefore, possible role of vitamin-D in TB prevention through cathelicidin production was studied in high-risk household contacts (HHCs) of pulmonary tuberculosis (PTB) patients. 20 HHCs of PTB patients were recruited and followed up for one year. Levels of vitamin-D (25(OH)D) and its associated molecules were evaluated at 3-months intervals for one year or until the development of active TB. 25(OH)D was measured using chemiluminescence method. Serum VDR and cathelicidin levels were measured by ELISA and VDR mRNA expression by qPCR. Throughout the study period mean range of serum 25(OH)D levels was 20.51 ± 5.12 ng/ml. VDR and cathelicidin levels however showed significant decline after six months suggesting decrease in bacterial exposure. None of the HHCs developed active infection even with high exposure to 2 + to 3 + AFB positive index cases. Mantoux positive household contacts had high levels of VDR and cathelicidin, suggestive of an early or latent phase of infection, did not develop active TB plausibly due to maintenance of adequate serum levels of vitamin-D. Optimal levels of 25(OH)D and its associated molecules during early stages of infection may serve as protective factor against development of active TB. Cohort of HHCs with severely deficient vitamin-D levels (10 ng/ml) could be followed up for a better risk assessment.
{"title":"Protective Role of Vitamin D Against Development of Active Tuberculosis in Close Household Contacts of Pulmonary Tuberculosis Patients: A Prospective Cohort Study.","authors":"Sudhasini Panda, Ambrish Tiwari, Vivek Kumar, Kalpana Luthra, Kuldeep Kumar, Archana Singh","doi":"10.1007/s12291-022-01110-3","DOIUrl":"10.1007/s12291-022-01110-3","url":null,"abstract":"<p><p>Vitamin-D is known to promote innate immune responses by acting as a cofactor of VDR for induction of antimicrobial peptides like cathelicidin. Close household contacts of pulmonary tuberculosis patients are at high risk of active infection, Therefore, possible role of vitamin-D in TB prevention through cathelicidin production was studied in high-risk household contacts (HHCs) of pulmonary tuberculosis (PTB) patients. 20 HHCs of PTB patients were recruited and followed up for one year. Levels of vitamin-D (25(OH)D) and its associated molecules were evaluated at 3-months intervals for one year or until the development of active TB. 25(OH)D was measured using chemiluminescence method. Serum VDR and cathelicidin levels were measured by ELISA and VDR mRNA expression by qPCR. Throughout the study period mean range of serum 25(OH)D levels was 20.51 ± 5.12 ng/ml. VDR and cathelicidin levels however showed significant decline after six months suggesting decrease in bacterial exposure. None of the HHCs developed active infection even with high exposure to 2 + to 3 + AFB positive index cases. Mantoux positive household contacts had high levels of VDR and cathelicidin, suggestive of an early or latent phase of infection, did not develop active TB plausibly due to maintenance of adequate serum levels of vitamin-D. Optimal levels of 25(OH)D and its associated molecules during early stages of infection may serve as protective factor against development of active TB. Cohort of HHCs with severely deficient vitamin-D levels (10 ng/ml) could be followed up for a better risk assessment.</p>","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"47 1","pages":"248-256"},"PeriodicalIF":2.1,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10987442/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89782037","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Compound Danshen Dripping Pills (CDDPs) have been used in clinical treatment to protect the heart from ischemia/reperfusion (IR) injury for many years. However, the underlying mechanism implicated in the protective effects remains to be explored. Here, we determined the effects of CDDPs in Sprague–Dawley rats with the IR model. Cardiac function in vivo was assessed by echocardiography. Transmission electron microscopy, histological and immunohistochemical techniques, Western blotting and recombinant adeno-associated virus 9 transfection were used to illustrate the effects of CDDPs on IR and autophagy. Our results showed that pretreatment with CDDPs decreased the level of serum myocardial enzymes and infarct size in rats after IR. Apoptosis evaluation showed that CDDPs significantly ameliorated the cardiac apoptosis level after IR. Meanwhile, CDDPs pretreatment increased myocardial autophagic flux, with upregulation of LC3B, downregulation of p62, and increased autophagosomes and autolysosomes. Moreover, the autophagic flux inhibitor chloroquine could increase IR injury, while CDDPs could partially reverse the effects. Furthermore, our results showed that the activation of AMPK/mTOR was involved in the cardioprotective effect exerted by CDDPs. Herein, we suggest that CDDPs partially protect the heart from IR injury by enhancing autophagic flux through the activation of AMPK/mTOR.
{"title":"Compound Danshen Dripping Pills pretreatment protects the heart from ischemia/reperfusion injury by enhancing autophagic flux","authors":"Haiqiong Liu, Qian Liang, Xiheng Mei, Hekai Li, Jing Yan, Man Long, Xili Yang, Wei Wang, Weijie Li, Aihua Chen, Yuanna Ling","doi":"10.1590/s2175-97902023e211035","DOIUrl":"https://doi.org/10.1590/s2175-97902023e211035","url":null,"abstract":"Compound Danshen Dripping Pills (CDDPs) have been used in clinical treatment to protect the heart from ischemia/reperfusion (IR) injury for many years. However, the underlying mechanism implicated in the protective effects remains to be explored. Here, we determined the effects of CDDPs in Sprague–Dawley rats with the IR model. Cardiac function in vivo was assessed by echocardiography. Transmission electron microscopy, histological and immunohistochemical techniques, Western blotting and recombinant adeno-associated virus 9 transfection were used to illustrate the effects of CDDPs on IR and autophagy. Our results showed that pretreatment with CDDPs decreased the level of serum myocardial enzymes and infarct size in rats after IR. Apoptosis evaluation showed that CDDPs significantly ameliorated the cardiac apoptosis level after IR. Meanwhile, CDDPs pretreatment increased myocardial autophagic flux, with upregulation of LC3B, downregulation of p62, and increased autophagosomes and autolysosomes. Moreover, the autophagic flux inhibitor chloroquine could increase IR injury, while CDDPs could partially reverse the effects. Furthermore, our results showed that the activation of AMPK/mTOR was involved in the cardioprotective effect exerted by CDDPs. Herein, we suggest that CDDPs partially protect the heart from IR injury by enhancing autophagic flux through the activation of AMPK/mTOR.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67738109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-09-04DOI: 10.1590/s2175-97902023e20200
Anubhav Kumar Singh, Niraj Kumar Singh, Ahsas Goyal, B. Semwal, H. Yadav
The renin-angiotensin-aldosterone system (RAAS) plays a key role in diabetic nephropathy (DN). Angiotensin-II secreted during the RAAS pathway increases nephropathy. It stimulates oxidative stress which can quench nitric oxide. Reduced nitric oxide level aggravates Ang-II-induced vasoconstriction. Ang-II has also emerged as a central mediator of the glomerular hemodynamic changes that are associated with renal injury. Deletion of ACE2 is also noted due to increased Ang-II level which leads to the development of DN. We hypothesize that nephropathy caused by Ang-II in the periphery may be controlled by brain RAAS. ACE inhibitors and ARBs may show the renoprotective effect when administered through ICV without crossing the blood-brain barrier. DN was observed after 8 weeks of diabetes induction through alloxan. Administration of captopril and valsartan once and in combined therapy for 2 weeks, significantly reduced urine output, blood urea nitrogen, total protein in the urine, serum cholesterol, serum creatinine, serum triglycerides, and kidney/body weight ratio as compared to diabetic control rats. Further, combination therapy significantly increased the body weight and serum nitrate level as compared to diabetic control animals. However, increased ACE2 levels in the brain may reduce the sympathetic outflow and might have decreased the peripheral activity of Ang-II which shows beneficial effects in DN.
{"title":"Role of Brain Angiotensin-II in Development of Experimental Diabetic Nephropathy in Wistar Rats","authors":"Anubhav Kumar Singh, Niraj Kumar Singh, Ahsas Goyal, B. Semwal, H. Yadav","doi":"10.1590/s2175-97902023e20200","DOIUrl":"https://doi.org/10.1590/s2175-97902023e20200","url":null,"abstract":"The renin-angiotensin-aldosterone system (RAAS) plays a key role in diabetic nephropathy (DN). Angiotensin-II secreted during the RAAS pathway increases nephropathy. It stimulates oxidative stress which can quench nitric oxide. Reduced nitric oxide level aggravates Ang-II-induced vasoconstriction. Ang-II has also emerged as a central mediator of the glomerular hemodynamic changes that are associated with renal injury. Deletion of ACE2 is also noted due to increased Ang-II level which leads to the development of DN. We hypothesize that nephropathy caused by Ang-II in the periphery may be controlled by brain RAAS. ACE inhibitors and ARBs may show the renoprotective effect when administered through ICV without crossing the blood-brain barrier. DN was observed after 8 weeks of diabetes induction through alloxan. Administration of captopril and valsartan once and in combined therapy for 2 weeks, significantly reduced urine output, blood urea nitrogen, total protein in the urine, serum cholesterol, serum creatinine, serum triglycerides, and kidney/body weight ratio as compared to diabetic control rats. Further, combination therapy significantly increased the body weight and serum nitrate level as compared to diabetic control animals. However, increased ACE2 levels in the brain may reduce the sympathetic outflow and might have decreased the peripheral activity of Ang-II which shows beneficial effects in DN.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67737103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e23075
Ana Carolina Menezes Mendonça Valente, Gustavo Henrique Lima de Farias, Ana Cristina Ribeiro Bernardo, C. Alves, Michelle Bueno de Moura Pereira, Raquel Tognon-Ribeiro
Focal Adhesion Kinase (FAK) protein participates in proliferation, migration, cell survival, and apoptosis process. It has been described as overexpressed in several neoplasms being a promising target for therapy. BCR-ABL negative chronic Myeloproliferative Neoplasms (MPN) are clonal disorders characterized by the excess of proliferation and apoptosis resistance. The identification of the acquired JAK2 V617F mutation in MPN patients allowed a better understanding of pathogenesis. However, there is still no pharmacological treatment that leads all patients to molecular remission, justifying new studies. The present study aimed to evaluate FAK involvement in the viability and apoptosis of HEL and SET-2 cells, both JAK2 V617F positive cell lines. The FAK inhibitor PF 562,271 was used. Cell viability was determined using MTT assay and apoptosis verified by cleaved PARP, cleaved Caspase 3 and Annexin-V/PI staining detection. FAK inhibition significantly reduced HEL and SET-2 cells viability and induced apoptosis. Considering the role of JAK/STAT pathway in MPN, further investigation of FAK participation in the MPN cells proliferation and apoptosis resistance, as well as possible crosstalk between JAK and FAK and downstream pathways may contribute to the knowledge of MPN pathophysiology, the discovery of new molecular targets, and JAK inhibitors resistance mechanisms.
{"title":"Focal adhesion kinase inhibition decreases cell viability and induces apoptosis of JAK2 V617F positive cells","authors":"Ana Carolina Menezes Mendonça Valente, Gustavo Henrique Lima de Farias, Ana Cristina Ribeiro Bernardo, C. Alves, Michelle Bueno de Moura Pereira, Raquel Tognon-Ribeiro","doi":"10.1590/s2175-97902023e23075","DOIUrl":"https://doi.org/10.1590/s2175-97902023e23075","url":null,"abstract":"Focal Adhesion Kinase (FAK) protein participates in proliferation, migration, cell survival, and apoptosis process. It has been described as overexpressed in several neoplasms being a promising target for therapy. BCR-ABL negative chronic Myeloproliferative Neoplasms (MPN) are clonal disorders characterized by the excess of proliferation and apoptosis resistance. The identification of the acquired JAK2 V617F mutation in MPN patients allowed a better understanding of pathogenesis. However, there is still no pharmacological treatment that leads all patients to molecular remission, justifying new studies. The present study aimed to evaluate FAK involvement in the viability and apoptosis of HEL and SET-2 cells, both JAK2 V617F positive cell lines. The FAK inhibitor PF 562,271 was used. Cell viability was determined using MTT assay and apoptosis verified by cleaved PARP, cleaved Caspase 3 and Annexin-V/PI staining detection. FAK inhibition significantly reduced HEL and SET-2 cells viability and induced apoptosis. Considering the role of JAK/STAT pathway in MPN, further investigation of FAK participation in the MPN cells proliferation and apoptosis resistance, as well as possible crosstalk between JAK and FAK and downstream pathways may contribute to the knowledge of MPN pathophysiology, the discovery of new molecular targets, and JAK inhibitors resistance mechanisms.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"67 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67743347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e21384
A. Haverić, S. Haverić, M. Hadzic, J. Ezić, T. Cetkovic, B. Galić
Biological activity of boron-containing compounds (BCCs) has been well-known. Growing interest and numerous applications for BCCs have been reported. Boron and boron-containing acids show low acute toxicity in mammals but data on halogenated boroxine (HB) - dipotassium-trioxohydroxytetrafluorotriborate, K 2 (B 3 O 3 F 4 OH) acute toxicity have not been reported before. This compound, characterized as a potential therapeutic for skin changes, exhibits no observable genotoxicity in doses lower that 0.1 mg/ml in vitro and 55 mg/kg in vivo. It has also been confirmed as an antitumour agent both in vitro and in vivo as well as an inhibitor of enzymes involved in antioxidant mechanisms. The aim of this study was to assess the acute toxicity of HB and to determine the maximum tolerated dose as well as a dose free of any signs of toxicity in different test organisms. Acute toxicity of HB was tested in Sprague-Dawley and Wistar rats and BALB/c mice after single parenteral application of different doses. We determined doses free of any sign of toxicity and LD 50 after single dose administration. LD 50 of HB ranges from 63 to 75 mg/kg in different test models, meaning that HB shows moderate toxicity.
{"title":"Moderate Toxicity of Potential Boron-containing Therapeutic, Dipotassium-trioxohydroxytetrafl uorotriborate -K2(B3O3F4OH) in Rats and Mice","authors":"A. Haverić, S. Haverić, M. Hadzic, J. Ezić, T. Cetkovic, B. Galić","doi":"10.1590/s2175-97902023e21384","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21384","url":null,"abstract":"Biological activity of boron-containing compounds (BCCs) has been well-known. Growing interest and numerous applications for BCCs have been reported. Boron and boron-containing acids show low acute toxicity in mammals but data on halogenated boroxine (HB) - dipotassium-trioxohydroxytetrafluorotriborate, K 2 (B 3 O 3 F 4 OH) acute toxicity have not been reported before. This compound, characterized as a potential therapeutic for skin changes, exhibits no observable genotoxicity in doses lower that 0.1 mg/ml in vitro and 55 mg/kg in vivo. It has also been confirmed as an antitumour agent both in vitro and in vivo as well as an inhibitor of enzymes involved in antioxidant mechanisms. The aim of this study was to assess the acute toxicity of HB and to determine the maximum tolerated dose as well as a dose free of any signs of toxicity in different test organisms. Acute toxicity of HB was tested in Sprague-Dawley and Wistar rats and BALB/c mice after single parenteral application of different doses. We determined doses free of any sign of toxicity and LD 50 after single dose administration. LD 50 of HB ranges from 63 to 75 mg/kg in different test models, meaning that HB shows moderate toxicity.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739499","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e22718
L. A. Gama, Mariana Pirani Rocha Machado, L. Corá, A. P. S. Beckmann, Wellington David Luz Alves, J. Miranda, M. Américo
Our aim was to evaluate the effects of cisplatin and dexamethasone alone and combined on gastric contractility and histomorphometry of BALB/c and C57BL/6 mice. BALB/c and C57BL/6 male mice (8-week-old) were randomly separated into: Control; Cisplatin (7.5 mg/Kg); Dexamethasone (2.0 mg/Kg); and Dexamethasone plus Cisplatin (2.0 mg/Kg of dexamethasone 1-hour prior to 7.5 mg/Kg of cisplatin). Drugs were administered intraperitoneally for three days. Body weight and food intake were evaluated on 2nd day. Alternating Current Biosusceptometry technique was employed to measure gastric contractions on 3rd day. Afterward, mice were killed for gastric histomorphometric analysis. Cisplatin decreased food intake and caused bradygastria in BALB/c mice; however, the amplitude of gastric contractions decreased in both BALB/c and C57BL/6. Dexamethasone and cisplatin combined restored the gastric frequency and food intake only in BALB/c, but drug combination reduced the gastric amplitude of contractions in both strains. Dexamethasone alone increased gastric mucosa thickness in C57BL/6 and decreased muscular thickness in BALB/c. In conclusion, the mouse strains presented differences in acute effects of cisplatin and dexamethasone alone and combined on gastric function. This reinforces the importance of choosing the appropriate mouse strain for studying the acute effects of drugs on the gastrointestinal tract.
{"title":"BALB/c and C57BL/6 mouse strains influence gastric function outcomes with administration of cisplatin and dexamethasone","authors":"L. A. Gama, Mariana Pirani Rocha Machado, L. Corá, A. P. S. Beckmann, Wellington David Luz Alves, J. Miranda, M. Américo","doi":"10.1590/s2175-97902023e22718","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22718","url":null,"abstract":"Our aim was to evaluate the effects of cisplatin and dexamethasone alone and combined on gastric contractility and histomorphometry of BALB/c and C57BL/6 mice. BALB/c and C57BL/6 male mice (8-week-old) were randomly separated into: Control; Cisplatin (7.5 mg/Kg); Dexamethasone (2.0 mg/Kg); and Dexamethasone plus Cisplatin (2.0 mg/Kg of dexamethasone 1-hour prior to 7.5 mg/Kg of cisplatin). Drugs were administered intraperitoneally for three days. Body weight and food intake were evaluated on 2nd day. Alternating Current Biosusceptometry technique was employed to measure gastric contractions on 3rd day. Afterward, mice were killed for gastric histomorphometric analysis. Cisplatin decreased food intake and caused bradygastria in BALB/c mice; however, the amplitude of gastric contractions decreased in both BALB/c and C57BL/6. Dexamethasone and cisplatin combined restored the gastric frequency and food intake only in BALB/c, but drug combination reduced the gastric amplitude of contractions in both strains. Dexamethasone alone increased gastric mucosa thickness in C57BL/6 and decreased muscular thickness in BALB/c. In conclusion, the mouse strains presented differences in acute effects of cisplatin and dexamethasone alone and combined on gastric function. This reinforces the importance of choosing the appropriate mouse strain for studying the acute effects of drugs on the gastrointestinal tract.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742530","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e21179
Francine Alves Nogueira de Almeida, P. V. Oliveira, Natan Silva Matos, Verônica Luiza Silveira Fialho, M. D. Lugon, M. C. Vieira, M. F. S. Ferreira, G. G. Paneto
Hebanthe eriantha (Martius) Kuntze and Pfaffia glomerata (Spreng) Pedersen are medicinal plants popularly known as “Brazilian Ginseng” due to their similarity to Panax ginseng . In Brazil, they are sold as the same herb, despite their different pharmacological and toxicological properties. The morphological identification is difficult, which facilitates their adulteration. We report the application of the Barcode DNA High-Resolution Melting (Bar-HRM) using matK gene to differentiate both species in samples sold in the Brazilian market. Using the proposed method, we could discriminate and identify both species. Bar-HRM analysis allowed discriminating and identifying both species. It allowed the identification of H. eriantha and P. glomerata in 43.6% and 56.4% of the amplified samples, respectively. Of these, only seven samples were authenticated and, in 71.4% of the cases, adulterated. We concluded that Bar-HRM has proven to be a fast alternative method to authenticate plants under the common name “Brazilian Ginseng”.
{"title":"Authentication of Brazilian Ginseng using Bar-HRM analysis","authors":"Francine Alves Nogueira de Almeida, P. V. Oliveira, Natan Silva Matos, Verônica Luiza Silveira Fialho, M. D. Lugon, M. C. Vieira, M. F. S. Ferreira, G. G. Paneto","doi":"10.1590/s2175-97902023e21179","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21179","url":null,"abstract":"Hebanthe eriantha (Martius) Kuntze and Pfaffia glomerata (Spreng) Pedersen are medicinal plants popularly known as “Brazilian Ginseng” due to their similarity to Panax ginseng . In Brazil, they are sold as the same herb, despite their different pharmacological and toxicological properties. The morphological identification is difficult, which facilitates their adulteration. We report the application of the Barcode DNA High-Resolution Melting (Bar-HRM) using matK gene to differentiate both species in samples sold in the Brazilian market. Using the proposed method, we could discriminate and identify both species. Bar-HRM analysis allowed discriminating and identifying both species. It allowed the identification of H. eriantha and P. glomerata in 43.6% and 56.4% of the amplified samples, respectively. Of these, only seven samples were authenticated and, in 71.4% of the cases, adulterated. We concluded that Bar-HRM has proven to be a fast alternative method to authenticate plants under the common name “Brazilian Ginseng”.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739118","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e22330
Gizem Rüya Topal, Berrin Küçüktürkmen, U. Öz, Erva Özkan, Filiz Bakar-Ates, A. Bozkır
symptomatic treatment of Alzheimer’s disease (AD) and has many side effects. In this study, to reduce the side effects of Donepezil-HCl and increase the penetration of the drug through the blood-brain barrier, we aimed to design a solid lipid nanoparticle (SLN) formulation. The effects of the different formulation parameters, such as homogenization speed, sonication time, lipid and drug concentration, surfactant type and concentration, and volume of the aqueous phase, were assessed for optimization. The particle size and PDI increased with increasing lipid concentration but decreased with increasing amounts of surfactant (Tween 80) and co-surfactant (lecithin). When the homogenization rate and sonication time increased, the particle size decreased and the encapsulation efficiency increased. The optimized formulation exhibited particle size, PDI, encapsulation efficiency, and zeta potential of 87.2±0.11 nm; 0.22±0.02; 93.84±0.01 %; -17.0±0.12 mV respectively. The in vitro release investigation revealed that approximately 70% of Donepezil-HCl was cumulatively released after 24 hours. TEM analysis proved that spherical and smooth particles were obtained and formulations had no toxic effect on cells. The final optimized formulation could be a candidate for Donepezil-HCl application in Alzheimer’s treatment with reduced side effects and doses for patients.
{"title":"Investigation on formulation parameters of donepezil HCl loaded solid lipid nanoparticles","authors":"Gizem Rüya Topal, Berrin Küçüktürkmen, U. Öz, Erva Özkan, Filiz Bakar-Ates, A. Bozkır","doi":"10.1590/s2175-97902023e22330","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22330","url":null,"abstract":"symptomatic treatment of Alzheimer’s disease (AD) and has many side effects. In this study, to reduce the side effects of Donepezil-HCl and increase the penetration of the drug through the blood-brain barrier, we aimed to design a solid lipid nanoparticle (SLN) formulation. The effects of the different formulation parameters, such as homogenization speed, sonication time, lipid and drug concentration, surfactant type and concentration, and volume of the aqueous phase, were assessed for optimization. The particle size and PDI increased with increasing lipid concentration but decreased with increasing amounts of surfactant (Tween 80) and co-surfactant (lecithin). When the homogenization rate and sonication time increased, the particle size decreased and the encapsulation efficiency increased. The optimized formulation exhibited particle size, PDI, encapsulation efficiency, and zeta potential of 87.2±0.11 nm; 0.22±0.02; 93.84±0.01 %; -17.0±0.12 mV respectively. The in vitro release investigation revealed that approximately 70% of Donepezil-HCl was cumulatively released after 24 hours. TEM analysis proved that spherical and smooth particles were obtained and formulations had no toxic effect on cells. The final optimized formulation could be a candidate for Donepezil-HCl application in Alzheimer’s treatment with reduced side effects and doses for patients.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e221000
Daniel Ribeiro Grijó, Edvalkia Magna Teobaldo da Rocha, Vitor de Cinque Almeida, C. Amado, J. E. Olivo, Oswaldo Curty da Motta Lima
Cannabidiol (CBD) is a bioactive compound with promising anti-inflammatory results but has low aqueous solubility. Complexation of drugs with this characteristic in carriers is an alternative to improve their efficiency. This study aimed to prepare and characterize CBD complexes in different carriers, and to evaluate the anti-inflammatory effect of such preparations using an experimental model of edema induction in rat paws. The results were compared to a reference drug, ibuprofen (IBU). The carriers evaluated were beta cyclodextrin (bCD) and activated charcoal (AC). Quantification of the drugs in the complexes was determined, and different qualitative analyses were also performed. Oral treatments in single doses with CBD showed inhibitory effects similar to that of IBU, potentiating its bioactivity without significant adverse effects. CBD*bCD doses at 4.375, 8.75, 17.5, and 35 mg/kg significantly reduced the intensity of edema compared to equivalent doses of pure bioactive. In contrast, CBD*AC did not generate benefits. There was no significant inhibitory effect on myeloperoxidase activity, requiring more specific analyses to assess this parameter. The results suggest that the CBD*bCD complexation is perfectly feasible, increasing its anti-edematogenic efficacy in the experimental model used.
{"title":"Experimental acute anti-inflammatory activity of preparations with complexed cannabidiol in carriers","authors":"Daniel Ribeiro Grijó, Edvalkia Magna Teobaldo da Rocha, Vitor de Cinque Almeida, C. Amado, J. E. Olivo, Oswaldo Curty da Motta Lima","doi":"10.1590/s2175-97902023e221000","DOIUrl":"https://doi.org/10.1590/s2175-97902023e221000","url":null,"abstract":"Cannabidiol (CBD) is a bioactive compound with promising anti-inflammatory results but has low aqueous solubility. Complexation of drugs with this characteristic in carriers is an alternative to improve their efficiency. This study aimed to prepare and characterize CBD complexes in different carriers, and to evaluate the anti-inflammatory effect of such preparations using an experimental model of edema induction in rat paws. The results were compared to a reference drug, ibuprofen (IBU). The carriers evaluated were beta cyclodextrin (bCD) and activated charcoal (AC). Quantification of the drugs in the complexes was determined, and different qualitative analyses were also performed. Oral treatments in single doses with CBD showed inhibitory effects similar to that of IBU, potentiating its bioactivity without significant adverse effects. CBD*bCD doses at 4.375, 8.75, 17.5, and 35 mg/kg significantly reduced the intensity of edema compared to equivalent doses of pure bioactive. In contrast, CBD*AC did not generate benefits. There was no significant inhibitory effect on myeloperoxidase activity, requiring more specific analyses to assess this parameter. The results suggest that the CBD*bCD complexation is perfectly feasible, increasing its anti-edematogenic efficacy in the experimental model used.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742203","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-28DOI: 10.1590/s2175-97902023e23059
Marcelle Leandro da Silva Pereira, Rita de Cássia Paulino de Souza, Juliana Vilar Furtado de Medeiros, George Queiroz de Brito, A. Schwarz
The addition of linseed ( Linum usitatissimum Linn) in the diet, as a functional food, has increased over the years. However, it possesses cyanogenic glycosides. This study aimed to quantify and compare cyanide concentration in whole seed and bran of brown and golden types to establish a safe limit of intake. Three commercial labels, from brown and golden whole seed types (Ab, Ag, Bb, Bg, Cb and Cg), and six commercial labels of brown and golden bran (1b, 2g, 3g, 4b, 5g, and 6b), were selected, totalizing twelve samples. Total cyanide concentration was quantified by a colorimetric method employing alkaline picrate, after acid hydrolysis. The whole seed cyanide values were between 348.4 and 473.20 µg/g and the bran cyanide values were between 459.53 and 639.35 μg/g. The analyzed bran presented increased cyanide concentrations than the whole seeds with no differences between brown and golden types. Food able to produce cyanide less than 90 µg/kg body weight, daily, is considered secure for consumption. Considering this limit and analyzed samples, it is safe to eat approximately two tablespoons of seeds or one tablespoon of bran. These results point out the importance of cyanide amount daily intake information to be in linseed packaging, to ensure secure consumption.
{"title":"Determination of cyanide in whole seeds and brans of linseed (Linum usitatissimum Linn) by molecular spectrophotometry","authors":"Marcelle Leandro da Silva Pereira, Rita de Cássia Paulino de Souza, Juliana Vilar Furtado de Medeiros, George Queiroz de Brito, A. Schwarz","doi":"10.1590/s2175-97902023e23059","DOIUrl":"https://doi.org/10.1590/s2175-97902023e23059","url":null,"abstract":"The addition of linseed ( Linum usitatissimum Linn) in the diet, as a functional food, has increased over the years. However, it possesses cyanogenic glycosides. This study aimed to quantify and compare cyanide concentration in whole seed and bran of brown and golden types to establish a safe limit of intake. Three commercial labels, from brown and golden whole seed types (Ab, Ag, Bb, Bg, Cb and Cg), and six commercial labels of brown and golden bran (1b, 2g, 3g, 4b, 5g, and 6b), were selected, totalizing twelve samples. Total cyanide concentration was quantified by a colorimetric method employing alkaline picrate, after acid hydrolysis. The whole seed cyanide values were between 348.4 and 473.20 µg/g and the bran cyanide values were between 459.53 and 639.35 μg/g. The analyzed bran presented increased cyanide concentrations than the whole seeds with no differences between brown and golden types. Food able to produce cyanide less than 90 µg/kg body weight, daily, is considered secure for consumption. Considering this limit and analyzed samples, it is safe to eat approximately two tablespoons of seeds or one tablespoon of bran. These results point out the importance of cyanide amount daily intake information to be in linseed packaging, to ensure secure consumption.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"12 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67743019","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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