Patrick Maduabuchi Aja, Chinecherem Adanna Chukwu, Ugwu Okechukwu Paul-Chima, Boniface Anthony Ale, Peter Chinedu Agu, Tusubira Deusdedi, Darlington C Chukwu, Onyedika Gabriel Ani, Ezebuilo Ugbala Ekpono, Hilary Akobi Ogwoni, Joshua Nonso Awoke, Patience N Ogbu, Lucy Aja, Oliver Ugochukwu Ukachi, Obasi Uche Orji, Chinoso Peter Nweke, Chinedu Egwu, Ejike Ugbala Ekpono, Gift Onyinyechi Ewa, Ikechuku Okorie Igwenyi, Esther Ugo Alum, Daniel Ejim Uti, Christian Emeka Offor, Josiah E Ifie, Amaobichukwu Njoku, Maduagwunna Ekenechukwu Kenneth, Ejike Daniel Eze
Abstract OBJECTIVES This study looked at how CMSO affected male Wistar albino rats' liver damage caused by bisphenol A. METHODS The standard HPLC method was used to assess the CMSO's phenolic content. Then, six (n = 8) groups of forty-eight (48) male Wistar rats (150 20 g) each received either CMSO or olive oil before being exposed to BPA for 42 days. Groups: A (one milliliter of olive oil, regardless of weight), B (BPA 100 mg/kg body weight (BW)), C (CMSO 7.5 mg/kg BW), D (CMSO 7.5 mg/kg BW + BPA 100 mg/kg BW), E (CMSO 5.0 mg/kg BW + BPA 100 mg/kg BW), and F (CMSO 2.5 mg/kg BW + BPA 100 mg/kg BW). KEY FINDINGS A surprising abundance of flavonoids, totaling 17.8006 10.95 g/100 g, were found in the HPLC data. Malondialdehyde, liver enzymes, reactive oxygen species, total bilirubin, and direct bilirubin levels were all significantly elevated by BPA (p 0.05). Additionally, nuclear factor-B, interleukin-6, interleukin-1, tumor necrosis factor, and histological alterations were all considerably (p 0.05) caused by BPA. The altered biochemical markers and histology were, however, noticeably recovered by CMSO to a level that was comparable to the control. CONCLUSION Due to the abundance of flavonoid components in the oil, CMSO protects the liver from BPA-induced hepatotoxicity by lowering oxidative stress and inflammatory reactions.
{"title":"<i>Cucumeropsis mannii</i> seed oil protects against bisphenol A-induced hepatotoxicity by mitigating inflammation and oxidative stress in rats","authors":"Patrick Maduabuchi Aja, Chinecherem Adanna Chukwu, Ugwu Okechukwu Paul-Chima, Boniface Anthony Ale, Peter Chinedu Agu, Tusubira Deusdedi, Darlington C Chukwu, Onyedika Gabriel Ani, Ezebuilo Ugbala Ekpono, Hilary Akobi Ogwoni, Joshua Nonso Awoke, Patience N Ogbu, Lucy Aja, Oliver Ugochukwu Ukachi, Obasi Uche Orji, Chinoso Peter Nweke, Chinedu Egwu, Ejike Ugbala Ekpono, Gift Onyinyechi Ewa, Ikechuku Okorie Igwenyi, Esther Ugo Alum, Daniel Ejim Uti, Christian Emeka Offor, Josiah E Ifie, Amaobichukwu Njoku, Maduagwunna Ekenechukwu Kenneth, Ejike Daniel Eze","doi":"10.1093/rpsppr/rqad033","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad033","url":null,"abstract":"Abstract OBJECTIVES This study looked at how CMSO affected male Wistar albino rats' liver damage caused by bisphenol A. METHODS The standard HPLC method was used to assess the CMSO's phenolic content. Then, six (n = 8) groups of forty-eight (48) male Wistar rats (150 20 g) each received either CMSO or olive oil before being exposed to BPA for 42 days. Groups: A (one milliliter of olive oil, regardless of weight), B (BPA 100 mg/kg body weight (BW)), C (CMSO 7.5 mg/kg BW), D (CMSO 7.5 mg/kg BW + BPA 100 mg/kg BW), E (CMSO 5.0 mg/kg BW + BPA 100 mg/kg BW), and F (CMSO 2.5 mg/kg BW + BPA 100 mg/kg BW). KEY FINDINGS A surprising abundance of flavonoids, totaling 17.8006 10.95 g/100 g, were found in the HPLC data. Malondialdehyde, liver enzymes, reactive oxygen species, total bilirubin, and direct bilirubin levels were all significantly elevated by BPA (p 0.05). Additionally, nuclear factor-B, interleukin-6, interleukin-1, tumor necrosis factor, and histological alterations were all considerably (p 0.05) caused by BPA. The altered biochemical markers and histology were, however, noticeably recovered by CMSO to a level that was comparable to the control. CONCLUSION Due to the abundance of flavonoid components in the oil, CMSO protects the liver from BPA-induced hepatotoxicity by lowering oxidative stress and inflammatory reactions.","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"22 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135618301","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract Objectives Carotenoids are increasingly explored as nutraceuticals but their low bioavailability due to poor aqueous solubility limits their applications. This study discusses the development of a novel and organic solvent-free method to develop carotenoid-containing polymeric nanoparticles via temperature-induced phase transition (TIPT) of pluronic F-68 to obtain formulations with the improved dissolution of carotenoids. Methods The nanoencapsulation of carotenoids in pluronic F-68 was performed in supercritical carbon dioxide (scCO2) to avoid oxidative or temperature/solvent-induced degradation. The nanoencapsulates were prepared in scCO2 at 40 or 60 °C and 10 MPa without the aid of any organic solvent. The formulations thereafter were characterised for particle size via dynamic light scattering (DLS), particle morphology via Scanning Electron Microscopy (SEM) and carotenoid content/release via high-performance liquid chromatography (HPLC). Key findings HPLC results showed carotenoid degradation to be negligible in freshly prepared formulations when prepared in scCO2 at 60 °C and 10 MPa. The developed particles were spheroidal with sizes ranging between 150-250 nm depending on carotenoid content in the preparation. An improvement in the aqueous solubility and storage stability (5 ºC) of carotenoids was also observed for the formulations prepared in scCO2. Conclusions These results suggest that TIPT under scCO2 can be applied to formulate nanoparticulates with improved dissolution rate and stability of thermosensitive molecules such as carotenoids without causing any degradation during the processing.
{"title":"Nanoencapsulation of carotenoid extract <i>via</i> the temperature-induced phase transition of triblock polymer in Supercritical Carbon dioxide (scCO2)","authors":"Chiziezi I Wosu, Patricia J Harvey, Vivek Trivedi","doi":"10.1093/rpsppr/rqad035","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad035","url":null,"abstract":"Abstract Objectives Carotenoids are increasingly explored as nutraceuticals but their low bioavailability due to poor aqueous solubility limits their applications. This study discusses the development of a novel and organic solvent-free method to develop carotenoid-containing polymeric nanoparticles via temperature-induced phase transition (TIPT) of pluronic F-68 to obtain formulations with the improved dissolution of carotenoids. Methods The nanoencapsulation of carotenoids in pluronic F-68 was performed in supercritical carbon dioxide (scCO2) to avoid oxidative or temperature/solvent-induced degradation. The nanoencapsulates were prepared in scCO2 at 40 or 60 °C and 10 MPa without the aid of any organic solvent. The formulations thereafter were characterised for particle size via dynamic light scattering (DLS), particle morphology via Scanning Electron Microscopy (SEM) and carotenoid content/release via high-performance liquid chromatography (HPLC). Key findings HPLC results showed carotenoid degradation to be negligible in freshly prepared formulations when prepared in scCO2 at 60 °C and 10 MPa. The developed particles were spheroidal with sizes ranging between 150-250 nm depending on carotenoid content in the preparation. An improvement in the aqueous solubility and storage stability (5 ºC) of carotenoids was also observed for the formulations prepared in scCO2. Conclusions These results suggest that TIPT under scCO2 can be applied to formulate nanoparticulates with improved dissolution rate and stability of thermosensitive molecules such as carotenoids without causing any degradation during the processing.","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135994814","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mona E Elbanan, Maggie E Amer, Mohamed A El-Missiry, Azza I Othman, Sameh M Shabana
Abstract Objectives This study will determine if melatonin (MLT) can be used with 5-fluorouracil (5-FU), an anticancer drug as "adjuvants" to reduce A549 lung cancer cell proliferation and sensitize those cells to 5-FU at lower doses while protecting mice from hepatotoxicity. Methods In vitro, MTT assays assessed cell proliferation, and Annexin-V flow cytometry measured A549 cell apoptosis. RT-qPCR measured apoptotic markers P53, KI67, Bax, Bcl-2, and caspase3; and immunoblotting evaluated cell cycle parameters p21, CDK2, and cyclin E. ELISA biochemical analysis examined liver function, ROS and antioxidant assays, and inflammatory markers, in vivo. Masson's trichome, hematoxylin, and eosin stains examined histopathological changes and fibrosis under a microscope. Key findings MLT combined with 5-FU elevated chemosensitization by decreasing A549 cell proliferation, lowering the IC50, increasing P21, P53, and BAX, decreasing Bcl-2, Ki-67, CDK2, and cyclin E, and inducing apoptosis and cell cycle arrest at G0/G1. After 5-FU (Intraperitoneal (IP))/MLT (oral) co-administration in vivo, all parameters improved and reversed. Liver enzymes (AST and ALT), bilirubin, albumin, total protein, albumin/globulin ratio, ROS, 4HNE, H2O2, and pro-inflammatory cytokines; IL-6, IL-1β, and TNFα declined while antioxidant enzymes like SOD, CAT, GSH, and GPx and IL-10 (anti-inflammatory) increased in combined MLT/5-FU treated groups compared to untreated and 5-FU alone treated groups. Histopathology confirmed these results. Conclusions MLT protected A549 cells from 5-FU-induced hepatotoxicity and enhanced 5-FU's antitumor effect in vitro. These results support MLT/5-FU's benefits, suggesting a more effective lung cancer treatment with fewer hepatotoxicity side effects. That could provide a novel therapeutic strategy for lung cancer.
{"title":"Melatonin protects mice from 5-FU hepatotoxicity and improves 5-FU antitumor effects by an apoptotic pathway dependent on cell cycle arrest in A549 human lung cancer cells","authors":"Mona E Elbanan, Maggie E Amer, Mohamed A El-Missiry, Azza I Othman, Sameh M Shabana","doi":"10.1093/rpsppr/rqad034","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad034","url":null,"abstract":"Abstract Objectives This study will determine if melatonin (MLT) can be used with 5-fluorouracil (5-FU), an anticancer drug as \"adjuvants\" to reduce A549 lung cancer cell proliferation and sensitize those cells to 5-FU at lower doses while protecting mice from hepatotoxicity. Methods In vitro, MTT assays assessed cell proliferation, and Annexin-V flow cytometry measured A549 cell apoptosis. RT-qPCR measured apoptotic markers P53, KI67, Bax, Bcl-2, and caspase3; and immunoblotting evaluated cell cycle parameters p21, CDK2, and cyclin E. ELISA biochemical analysis examined liver function, ROS and antioxidant assays, and inflammatory markers, in vivo. Masson's trichome, hematoxylin, and eosin stains examined histopathological changes and fibrosis under a microscope. Key findings MLT combined with 5-FU elevated chemosensitization by decreasing A549 cell proliferation, lowering the IC50, increasing P21, P53, and BAX, decreasing Bcl-2, Ki-67, CDK2, and cyclin E, and inducing apoptosis and cell cycle arrest at G0/G1. After 5-FU (Intraperitoneal (IP))/MLT (oral) co-administration in vivo, all parameters improved and reversed. Liver enzymes (AST and ALT), bilirubin, albumin, total protein, albumin/globulin ratio, ROS, 4HNE, H2O2, and pro-inflammatory cytokines; IL-6, IL-1β, and TNFα declined while antioxidant enzymes like SOD, CAT, GSH, and GPx and IL-10 (anti-inflammatory) increased in combined MLT/5-FU treated groups compared to untreated and 5-FU alone treated groups. Histopathology confirmed these results. Conclusions MLT protected A549 cells from 5-FU-induced hepatotoxicity and enhanced 5-FU's antitumor effect in vitro. These results support MLT/5-FU's benefits, suggesting a more effective lung cancer treatment with fewer hepatotoxicity side effects. That could provide a novel therapeutic strategy for lung cancer.","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"14 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135804223","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
This study aimed to explore the analgesic effects of fosphenytoin (fPHT) on pain-related behaviors in mouse models of subacute herpetic neuralgia (subAHN) and postherpetic neuralgia (PHN). SubAHN refers to pain experienced immediately after the disappearance of a skin rash, while PHN is characterized by persistent pain long after skin rash resolution. Our experimental approach involved the induction of acute herpes zoster-like skin lesions and pain-related responses (mechanical allodynia and hyperalgesia) in the hind paws of mice through cutaneous inoculation with herpes simplex virus type 1 (HSV-1). Subsequently, subAHN and PHN developed in the mice. Intravenous administration of fPHT (30 mg/kg) effectively mitigated HSV-1-induced subAHN and PHN. The suppressive effect of fPHT on subAHN was comparable to that of pregabalin (3 mg/kg, oral), a commonly used positive control. However, fPHT exhibited a slightly more potent effect than pregabalin in alleviating PHN. These findings suggest that intravenous fPHT could serve as a promising alternative for pain relief in both subAHN and PHN.
{"title":"Fosphenytoin alleviates subacute herpetic neuralgia and postherpetic neuralgia in mice","authors":"Ichiro Takasaki, Arata Inoue, Aoi Yoshida, Kimiyasu Shiraki, Y. Kitada, Saori Arai","doi":"10.1093/rpsppr/rqad030","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad030","url":null,"abstract":"\u0000 \u0000 \u0000 This study aimed to explore the analgesic effects of fosphenytoin (fPHT) on pain-related behaviors in mouse models of subacute herpetic neuralgia (subAHN) and postherpetic neuralgia (PHN). SubAHN refers to pain experienced immediately after the disappearance of a skin rash, while PHN is characterized by persistent pain long after skin rash resolution.\u0000 \u0000 \u0000 \u0000 Our experimental approach involved the induction of acute herpes zoster-like skin lesions and pain-related responses (mechanical allodynia and hyperalgesia) in the hind paws of mice through cutaneous inoculation with herpes simplex virus type 1 (HSV-1). Subsequently, subAHN and PHN developed in the mice.\u0000 \u0000 \u0000 \u0000 Intravenous administration of fPHT (30 mg/kg) effectively mitigated HSV-1-induced subAHN and PHN. The suppressive effect of fPHT on subAHN was comparable to that of pregabalin (3 mg/kg, oral), a commonly used positive control. However, fPHT exhibited a slightly more potent effect than pregabalin in alleviating PHN.\u0000 \u0000 \u0000 \u0000 These findings suggest that intravenous fPHT could serve as a promising alternative for pain relief in both subAHN and PHN.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42358128","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract Objective As plants are nature's panacea, mankind has used them for food and healing since the dawn of time. Currently, there are worldwide initiatives targeted at finding herbal treatments in plants and promoting them using a reliable drug delivery system for people. The fundamental idea underlying it is that each disease's cure can be found in nature. But the distribution of herbal medications also needs to be modified in order to promote patient compliance, achieve sustained discharge, etc. Key Findings Due to challenges with processing, standardisation, extraction, and identification, herbal medications traditionally could not convince scientists to modify novel drug delivery systems. Advanced approaches can be used to prevent toxicity, improve stability, increase the bioavailability of herbal formulations, and prevent physical and chemical deterioration. The various drug delivery systems indicated in this article are phytosomes, liposomes, nanoparticles, microspheres, microemulsions, niosomes, dendrimers, etc. Summary In order to enhance the delivery of herbal drugs by increasing their therapeutic benefits and reducing their toxicity, the need for innovative drug delivery systems has increased. This review provides information on numerous strategies used to increase the efficacy and safety of phytomedicines, as well as employing novel formulations. Conclusion By minimising toxicity and eliminating the need for repeated administration to overcome noncompliance, novel drug delivery systems increase therapeutic value. enhanced bioavailability, etc.
{"title":"Recent Development of Novel Drug Delivery of Herbal Drugs","authors":"Hardeep Singh, Gauri Sharma","doi":"10.1093/rpsppr/rqad028","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad028","url":null,"abstract":"Abstract Objective As plants are nature's panacea, mankind has used them for food and healing since the dawn of time. Currently, there are worldwide initiatives targeted at finding herbal treatments in plants and promoting them using a reliable drug delivery system for people. The fundamental idea underlying it is that each disease's cure can be found in nature. But the distribution of herbal medications also needs to be modified in order to promote patient compliance, achieve sustained discharge, etc. Key Findings Due to challenges with processing, standardisation, extraction, and identification, herbal medications traditionally could not convince scientists to modify novel drug delivery systems. Advanced approaches can be used to prevent toxicity, improve stability, increase the bioavailability of herbal formulations, and prevent physical and chemical deterioration. The various drug delivery systems indicated in this article are phytosomes, liposomes, nanoparticles, microspheres, microemulsions, niosomes, dendrimers, etc. Summary In order to enhance the delivery of herbal drugs by increasing their therapeutic benefits and reducing their toxicity, the need for innovative drug delivery systems has increased. This review provides information on numerous strategies used to increase the efficacy and safety of phytomedicines, as well as employing novel formulations. Conclusion By minimising toxicity and eliminating the need for repeated administration to overcome noncompliance, novel drug delivery systems increase therapeutic value. enhanced bioavailability, etc.","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134983105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
SARS-Cov-2 vaccines confer protection for about two months, hence the need for booster dose. Inefficiency of the vaccines may be attributed to mutated amino acids leading to change in structure and function of immunogenetic viral particles. Therefore literature search was carried out with a view to identifying problems of CoV-2 vaccine long term inefficiency, using missensed amino acids of the immunogens. Narrative review of six different COVID-19 vaccines administered at different centres to a total population of 98,979 individuals aged ≥18-95 years was adopted. Number of individuals that came down with infection post vaccination, vaccine dose administered, recorded mortality, post vaccinated infection-free individuals, immunogenicity status, missense mutation, incidence, probability and quality of mutation among amino acids sequences of the vaccinated viral particles were determined. Findings have shown that some live-attenuted vaccines such as BBIBP-CorV, WBIP, ChAdOxnCoV and Ad26.CoV2.5 are efficacious, but could induce mortal infection and mutation of amino acids such as aspartic acid, glycine, cysteine, aspartate, tyrosine, phenylalanine, threonine, serine, alanine, methionine, leucine and lysine. Mutation of some specific amino acids could be responsible for severe pathogenicity of SARS-CoV-2 and vaccine failure. Modalities that regulate synthesis of nucleobases and amino acids could be used to avert vaccine failure and improves immunogenicity of the vaccines.
{"title":"Mutation Of Amino Acids In Sars-Cov-2 May Be Responsible For Cov-2 Vaccine Long Term Inefficiency","authors":"Saganuwan Alhaji Saganuwan","doi":"10.1093/rpsppr/rqad027","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad027","url":null,"abstract":"\u0000 \u0000 \u0000 SARS-Cov-2 vaccines confer protection for about two months, hence the need for booster dose. Inefficiency of the vaccines may be attributed to mutated amino acids leading to change in structure and function of immunogenetic viral particles. Therefore literature search was carried out with a view to identifying problems of CoV-2 vaccine long term inefficiency, using missensed amino acids of the immunogens.\u0000 \u0000 \u0000 \u0000 Narrative review of six different COVID-19 vaccines administered at different centres to a total population of 98,979 individuals aged ≥18-95 years was adopted. Number of individuals that came down with infection post vaccination, vaccine dose administered, recorded mortality, post vaccinated infection-free individuals, immunogenicity status, missense mutation, incidence, probability and quality of mutation among amino acids sequences of the vaccinated viral particles were determined.\u0000 \u0000 \u0000 \u0000 Findings have shown that some live-attenuted vaccines such as BBIBP-CorV, WBIP, ChAdOxnCoV and Ad26.CoV2.5 are efficacious, but could induce mortal infection and mutation of amino acids such as aspartic acid, glycine, cysteine, aspartate, tyrosine, phenylalanine, threonine, serine, alanine, methionine, leucine and lysine.\u0000 \u0000 \u0000 \u0000 Mutation of some specific amino acids could be responsible for severe pathogenicity of SARS-CoV-2 and vaccine failure. Modalities that regulate synthesis of nucleobases and amino acids could be used to avert vaccine failure and improves immunogenicity of the vaccines.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43604914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Cedrus deodara (Roxb.) Loud. commonly called as deodar, belongs to family Pinaceae is a species of cedar native to the Western Himalayas in Eastern Afghanistan, Northern Pakistan, North-Central India, South Western Tibet and Western Nepal. The current review summarized and presents an up-to-date article on the medicinal uses, phytochemistry and biological activities of Cedrus deodara plant It is a medicinal tree and used traditionally to treat various diseases like microbial infection, joint disorder, asthma, skin diseases, kidney stone, peptic ulcer, brain disorders and inflammatory disorders. The chemical constituents obtained from different parts of plant include α-himachalene (12.5%) and β-himachalene (43%) associated with them are sesquiterpene alcohols (himachalol, allohimachalol, himadarol, isocentdarol, centdarol and cedrin(6-methyldihydromyricetin). Methylacetophenone, atlantonl. Deodarin, toxifolin, terpenoids, flavonoids and glycosides. Wikstromal, matairesinol, dibenzylbutyrolactol, bergapten, isopimpinellin, benzofuranoid neo lignan, isohemacholone Its chemical constituents are mostly responsible for the pharmacological actions. In recent in-vivo and in-vitro studies shows that Cedrus deodara have anti-inflammatory, analgesic, anti-hyperglycemic, anti-spasmodic, insecticidal, anti-apoptotic, anti-cancer, immmunomodulatory, molluscidal, anxiolytic and anticonvulsant properties. However, immediate efforts must be made to determine its mode of action, efficacy, dose range, and safety in addressing various disease situations
{"title":"CEDRUS DEODARA (ROXB.): A REVIEW ON THE RECENT UPDATE ON ITS PHARMACOLOGICAL AND PHYTOCHEMICAL PROFILE","authors":"Harsh Pathak, Sakshi Pathania, Shradha Metha, Ramica Sharma","doi":"10.1093/rpsppr/rqad026","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad026","url":null,"abstract":"\u0000 \u0000 \u0000 Cedrus deodara (Roxb.) Loud. commonly called as deodar, belongs to family Pinaceae is a species of cedar native to the Western Himalayas in Eastern Afghanistan, Northern Pakistan, North-Central India, South Western Tibet and Western Nepal. The current review summarized and presents an up-to-date article on the medicinal uses, phytochemistry and biological activities of Cedrus deodara plant\u0000 \u0000 \u0000 \u0000 It is a medicinal tree and used traditionally to treat various diseases like microbial infection, joint disorder, asthma, skin diseases, kidney stone, peptic ulcer, brain disorders and inflammatory disorders. The chemical constituents obtained from different parts of plant include α-himachalene (12.5%) and β-himachalene (43%) associated with them are sesquiterpene alcohols (himachalol, allohimachalol, himadarol, isocentdarol, centdarol and cedrin(6-methyldihydromyricetin). Methylacetophenone, atlantonl. Deodarin, toxifolin, terpenoids, flavonoids and glycosides. Wikstromal, matairesinol, dibenzylbutyrolactol, bergapten, isopimpinellin, benzofuranoid neo lignan, isohemacholone\u0000 \u0000 \u0000 \u0000 Its chemical constituents are mostly responsible for the pharmacological actions. In recent in-vivo and in-vitro studies shows that Cedrus deodara have anti-inflammatory, analgesic, anti-hyperglycemic, anti-spasmodic, insecticidal, anti-apoptotic, anti-cancer, immmunomodulatory, molluscidal, anxiolytic and anticonvulsant properties. However, immediate efforts must be made to determine its mode of action, efficacy, dose range, and safety in addressing various disease situations\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49206635","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Saganuwan Alhaji Saganuwan, Atanu Samuel Junior, Agu Solomon Tsekohol, N. Wanmi
The use of vegetables in Nigeria as nutraceutical cannot be over emphasized. However many vegetables are associated with toxicity effects at both low and high doses. Hence the study was aimed at investigating acute toxicity, haematological, biochemical, histopathological effects of Allium porrum (Leek),Cucurbita maxima (Pumpkin) and Brassica oleracea var capitata (Cabbage) in female Rattus norvegicus. The LD50 of the three plants were determined. The LD50 of aqueous extract of Cabbage, Leek, and Pumpkin was 6,585 mg/kg body weight. Cabbaged caused decrease in packed cell volume, erythrocytes counts, haemoglobin concentration, white blood cells, neutrophils and monocytes counts, increased basophils and eosinophils counts at dose levels of 5.79 mg/kg and 57.93 mg/kg body weight. At dose levels of 5.79-579.3 mg/kg body weight, the extract caused hypoalbuminaemia, hypoglycaemia, hypercholesterolaemia, increased levels of alanine amino transferase (ALT) and alkaline phosphatase (ALP). Cabbage also caused necrosis of hepatocytes, glomerular and tubular necrosis, cylinduria and perivascular cuffing in the brain. At dose level of 5.79 mg/kg and above, Cabbage may cause abortion during early stage of pregnancy due to possible loss of endometrial gland. The combined extract of Pumpkin and Leek caused haematopoiesis, neutropenia, lymphocytosis, eosinophilia, hypoglycaemia, hypocholesterolaemia , elevation of ALT levels, necrosis of hepatocytes and brain tissues, kidney damage and suppression of the development of ovarian follicle. Brassica oleracea var capitata may cause anaemia, immunosuppression, hypoglycaemia, hypercholesterolaemia, abortion, liver and kidney damage. The combined extract of leek and pumpkin may cause haematopoeisis, immunostimulation, hypoglycaemia, hypocholesterolaemia, brain problem and infertility.
{"title":"Acute Toxicity Study, Haematological, Biochemical And Histopathological Effects Of Brassica Oleracea Var Capitata, Allium Porrum And Cucurbita Maxima In Rattus Norvegicus","authors":"Saganuwan Alhaji Saganuwan, Atanu Samuel Junior, Agu Solomon Tsekohol, N. Wanmi","doi":"10.1093/rpsppr/rqad025","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad025","url":null,"abstract":"\u0000 \u0000 \u0000 The use of vegetables in Nigeria as nutraceutical cannot be over emphasized. However many vegetables are associated with toxicity effects at both low and high doses.\u0000 \u0000 \u0000 \u0000 Hence the study was aimed at investigating acute toxicity, haematological, biochemical, histopathological effects of Allium porrum (Leek),Cucurbita maxima (Pumpkin) and Brassica oleracea var capitata (Cabbage) in female Rattus norvegicus. The LD50 of the three plants were determined.\u0000 \u0000 \u0000 \u0000 The LD50 of aqueous extract of Cabbage, Leek, and Pumpkin was 6,585 mg/kg body weight. Cabbaged caused decrease in packed cell volume, erythrocytes counts, haemoglobin concentration, white blood cells, neutrophils and monocytes counts, increased basophils and eosinophils counts at dose levels of 5.79 mg/kg and 57.93 mg/kg body weight. At dose levels of 5.79-579.3 mg/kg body weight, the extract caused hypoalbuminaemia, hypoglycaemia, hypercholesterolaemia, increased levels of alanine amino transferase (ALT) and alkaline phosphatase (ALP). Cabbage also caused necrosis of hepatocytes, glomerular and tubular necrosis, cylinduria and perivascular cuffing in the brain. At dose level of 5.79 mg/kg and above, Cabbage may cause abortion during early stage of pregnancy due to possible loss of endometrial gland. The combined extract of Pumpkin and Leek caused haematopoiesis, neutropenia, lymphocytosis, eosinophilia, hypoglycaemia, hypocholesterolaemia , elevation of ALT levels, necrosis of hepatocytes and brain tissues, kidney damage and suppression of the development of ovarian follicle.\u0000 \u0000 \u0000 \u0000 Brassica oleracea var capitata may cause anaemia, immunosuppression, hypoglycaemia, hypercholesterolaemia, abortion, liver and kidney damage. The combined extract of leek and pumpkin may cause haematopoeisis, immunostimulation, hypoglycaemia, hypocholesterolaemia, brain problem and infertility.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41358856","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
V. Valkanioti, A. Kapourani, Melina Chatzitheodoridou, Maria-Emmanouela Anagnostaki, Ioannis Gkougkourelas, K. Kontogiannopoulos, A. Assimopoulou, P. Barmpalexis
This study investigates a new nanoparticulate (NP) formulation for local buccal administration of pilocarpine (PIL) to treat xerostomia, aiming to improve patient compliance and reduce side effects. PIL-loaded NPs were prepared using poly (d,l-lactic-co-glycolic acid) (PLGA) as a matrix/carrier and carbopol (CRB) as a mucoadhesive agent at various concentrations at ratios of 0.05%, 0.10% and 0.15% w/v. The NPs were characterized in terms of size, morphology, drug loading, thermophysical and physicochemical properties, in vitro dissolution performance, and mucoadhesion. Smooth spherical drug-loaded NPs (200-300 nm) were prepared in all cases. CRB coating did not impact particle size or polydispersity index (PDI) but increased NPs’ negative surface charges. Good storage stability, high production yields (72.0%-83.7%), and adequate drug loading efficiencies (9.0%-9.7%) were achieved, in all cases. DSC and pXRD measurements confirmed the amorphous drug dispersion, while ATR-FTIR studies revealed strong molecular interactions between the matrix/carrier and the mucoadhesive agent. In vitro drug release studies showed sustained release profiles for all NPs, whereas the application of a CRB-coating enhanced mucoadhesion performance through the formation of electrostatic ionic interactions and physical entanglement with mucin. The preparation of a new PLGA-based NP formulation may present itself as a promising strategy for the buccal administration of PIL, while the use of CRB coating could be considered as a useful approach for enhancing the mucus adhesion of NPs.
{"title":"Carbopol coated mucoadhesive PLGA nanoparticles for the sustained delivery of pilocarpine in the buccal cavity","authors":"V. Valkanioti, A. Kapourani, Melina Chatzitheodoridou, Maria-Emmanouela Anagnostaki, Ioannis Gkougkourelas, K. Kontogiannopoulos, A. Assimopoulou, P. Barmpalexis","doi":"10.1093/rpsppr/rqad024","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad024","url":null,"abstract":"\u0000 \u0000 \u0000 This study investigates a new nanoparticulate (NP) formulation for local buccal administration of pilocarpine (PIL) to treat xerostomia, aiming to improve patient compliance and reduce side effects.\u0000 \u0000 \u0000 \u0000 PIL-loaded NPs were prepared using poly (d,l-lactic-co-glycolic acid) (PLGA) as a matrix/carrier and carbopol (CRB) as a mucoadhesive agent at various concentrations at ratios of 0.05%, 0.10% and 0.15% w/v. The NPs were characterized in terms of size, morphology, drug loading, thermophysical and physicochemical properties, in vitro dissolution performance, and mucoadhesion.\u0000 \u0000 \u0000 \u0000 Smooth spherical drug-loaded NPs (200-300 nm) were prepared in all cases. CRB coating did not impact particle size or polydispersity index (PDI) but increased NPs’ negative surface charges. Good storage stability, high production yields (72.0%-83.7%), and adequate drug loading efficiencies (9.0%-9.7%) were achieved, in all cases. DSC and pXRD measurements confirmed the amorphous drug dispersion, while ATR-FTIR studies revealed strong molecular interactions between the matrix/carrier and the mucoadhesive agent. In vitro drug release studies showed sustained release profiles for all NPs, whereas the application of a CRB-coating enhanced mucoadhesion performance through the formation of electrostatic ionic interactions and physical entanglement with mucin.\u0000 \u0000 \u0000 \u0000 The preparation of a new PLGA-based NP formulation may present itself as a promising strategy for the buccal administration of PIL, while the use of CRB coating could be considered as a useful approach for enhancing the mucus adhesion of NPs.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49073272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Over 40% of dialysis patients have above-target phosphate. The efficacy and safety of oxylanthanum carbonate(OLC), a novel phosphate binder that forms the same insoluble phosphate complex as lanthanum carbonate, were assessed in 2 animal models. 3 groups of nephrectomized cats(n=4 per group) received 0.0466 g OLC/kg body weight, 0.2330 g OLC/kg body weight, or placebo. 6 groups of rats (n=6 per group) received placebo or 0.049, 0.099, 0.197, 0.394, or 0.788 g OLC/day. Endpoints included phosphate concentrations(urine, fecal, plasma) and serum lanthanum concentrations. All animals were observed for tolerance, injury, and mortality. In cats, urine phosphorus concentrations decreased across treatment groups and fecal phosphorus excretion increased in higher dose groups compared to control and lower dose groups. A clear but non-significant decline in plasma phosphate was observed. In rats, urinary phosphorus concentrations also decreased in all groups. The majority of serum lanthanum concentrations for rats in treatment groups were not significantly different from those in control groups. The study drug was well-tolerated in both models. OLC was effective for phosphate management and efficacy may be dose-dependent. OLC was safe and well-tolerated, indicating that it should be evaluated in the target population of patients with hyperphosphatemia.
超过40%的透析患者有高于目标的磷酸盐。碳酸氧镧(OLC)是一种新型磷酸盐粘合剂，与碳酸镧形成相同的不溶性磷酸盐复合物，我们在2种动物模型中评估了OLC的有效性和安全性。3组肾切除猫(每组n=4)分别给予0.0466 g OLC/kg体重、0.2330 g OLC/kg体重或安慰剂。6组大鼠(每组n=6)服用安慰剂或0.049、0.099、0.197、0.394或0.788 g OLC/天。终点包括磷酸盐浓度(尿、粪、血浆)和血清镧浓度。观察所有动物的耐受性、损伤和死亡率。在猫中，与对照组和低剂量组相比，高剂量组的尿磷浓度降低，高剂量组的粪磷排泄量增加。观察到血浆磷酸盐明显但不显著下降。在大鼠中，所有组的尿磷浓度也有所下降。各治疗组大鼠血清镧浓度与对照组无显著性差异。研究药物在两种模型中都有良好的耐受性。OLC对磷酸盐管理是有效的，其效果可能是剂量依赖性的。OLC是安全且耐受性良好的，表明它应该在高磷血症患者的目标人群中进行评估。
{"title":"Novel Phosphate Binder Oxylanthanum Carbonate Effectively Reduced Serum & Urine Phosphorus Concentrations in Animal Models","authors":"P. Gupta, Atul Khare, G. Reddy","doi":"10.1093/rpsppr/rqad022","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad022","url":null,"abstract":"\u0000 \u0000 \u0000 Over 40% of dialysis patients have above-target phosphate. The efficacy and safety of oxylanthanum carbonate(OLC), a novel phosphate binder that forms the same insoluble phosphate complex as lanthanum carbonate, were assessed in 2 animal models.\u0000 \u0000 \u0000 \u0000 3 groups of nephrectomized cats(n=4 per group) received 0.0466 g OLC/kg body weight, 0.2330 g OLC/kg body weight, or placebo. 6 groups of rats (n=6 per group) received placebo or 0.049, 0.099, 0.197, 0.394, or 0.788 g OLC/day. Endpoints included phosphate concentrations(urine, fecal, plasma) and serum lanthanum concentrations. All animals were observed for tolerance, injury, and mortality.\u0000 \u0000 \u0000 \u0000 In cats, urine phosphorus concentrations decreased across treatment groups and fecal phosphorus excretion increased in higher dose groups compared to control and lower dose groups. A clear but non-significant decline in plasma phosphate was observed. In rats, urinary phosphorus concentrations also decreased in all groups. The majority of serum lanthanum concentrations for rats in treatment groups were not significantly different from those in control groups. The study drug was well-tolerated in both models.\u0000 \u0000 \u0000 \u0000 OLC was effective for phosphate management and efficacy may be dose-dependent. OLC was safe and well-tolerated, indicating that it should be evaluated in the target population of patients with hyperphosphatemia.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42756300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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