Botulizm, insan ve hayvanlari etkileyen ciddi bir noroparalitik hastaliktir. Hasta- lik, Clostrid... more Botulizm, insan ve hayvanlari etkileyen ciddi bir noroparalitik hastaliktir. Hasta- lik, Clostridium botulinum bakterisi tarafindan uretilen ve bilinen en potent tok- sinlerden biri olan botulinum norotoksininden kaynaklanir. Botulinum norotok- sini sinir fonksiyonlarini bloke ederek solunum ve kas felcine yol acabilmektedir. Literaturde botulizmin en yaygin gorulen bulasma yolu, botulinum norotoksini ile kontamine gidalarin tuketilmesi ile seyreden gida kaynakli botulizmdir. Gida kaynakli botulizm, dunyada oldugu gibi ulkemizde de son yillarda gorulen bazi ardisik vakalar nedeniyle dikkat cekmektedir. Vakalarin buyuk bir cogunlugunun evde dusuk sicakliklarda ve yetersiz pisirme suresiyle pisirilip konserve edilen besinlerin tuketilmesi sonucu olustugu bildirilmektedir. Bu nedenle botulizme dikkat cekebilmek icin cesitli kanallar araciligiyla halki bilinclendirmeye yonelik her turlu egitici materyale ihtiyac duyulmaktadir. Bu derlemede, botulizm tipleri, tedavisi, botulizmden korunm...
Current Topics in Medicinal Chemistry, Mar 1, 2023
: The prevalence of depression has increased dramatically over the past few decades. Alt-hough de... more : The prevalence of depression has increased dramatically over the past few decades. Alt-hough depression is categorized as a brain disorder, its symptomatology includes some behaviors that also occur during chronic inflammatory stress. According to research, cytokine production and immune system activation may have a role in depression, so this relationship has received much at-tention. Moreover, there is a bidirectional relationship between oxidative stress and inflammation. Oxidative stress plays a pathogenic role in chronic inflammatory diseases; depressive disorder is be-ing suggested as one of them. Recent research using several oxidative stress indicators demonstrates that antioxidant defenses are diminished and oxidative stress is elevated in depression. Another cy-tokine-related mechanism widely known for its association with inflammatory illnesses is the kynurenine pathway (KP). KP is responsible for maintaining the balance between neuroprotective and neurogenerative processes in the brain. Therefore, KP plays a role in the pathophysiology of depression. It is thought to impact neurological processes that stem the depression, making it one of the mainstays in explaining oxidative stress-depression-inflammation interrelation. The mechanism is thought to be driven by increasing the expression of proinflammatory cytokines, IDO, and thus the KYN/TRP ratio. This review aims to evaluate the relationship between oxidative stress, depres-sion, and inflammation through the kynurenine pathway through the current studies in the literature.
Journal of The Iranian Chemical Society, Jul 14, 2021
In this study, new carboxamides derived from the imidazo[2,1- b ]thiazole skeleton which are carr... more In this study, new carboxamides derived from the imidazo[2,1- b ]thiazole skeleton which are carrying the biologically active benzoxazole group and are terminated with polar group such as chloro/bromo/cyano as well as imidazothiazole-based methyl carboxylate derivative were synthesized in order to investigate anti-inflammatory and analgesic activities. The new molecules were characterized by FT-IR, 1 H-NMR, 13 C-NMR and ESI–MS spectrometry. New chloro-terminated imidazothiazole-based carboxamide ( 7a ) and imidazothiazole-based methyl carboxylate derivative ( 8 ) showed, respectively, 75.88% and 77.05% cell viability on RAW 264.7 cell line at dose of 1.5 μM and 50 μM whereas trifluoroacetylamino-substituted thiazole carboxylate ( 1 ), trifluoroacetylamino-substituted thiazole carboxamides ( 2 ) and amino-substituted thiazole carboxamides ( 3 ) exhibited non-cytotoxicity by the cell viability value which is higher than 80% at dose of 100 μM except for their brominated derivatives 2b and 3b with highest cytotoxicity. Anti-inflammatory assay of the compounds on RAW 267.7 cells revealed that the compounds N -(4-chlorophenyl)-2-[(trifluoroacetyl)amino]-1,3-thiazole-5-carboxamide ( 2a ) and 2-amino- N -(4-chlorophenyl)-1,3-thiazole-5-carboxamide ( 3a ) which are starting materials in the synthetic route of 7a significantly have similar nitrite reducing effect with indomethacin which is positive control compound. As regarding to analgesic activity, compound 3a showed the highest reducing activity on PGE 2 level induced by LPS than trifluoroacetylamino-substituted carboxamides 2a and 2b as compared with control group.
Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory... more Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with α-hydroxy aldehyde or α-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by 1H NMR, 13C NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 μM and 8.0 μM IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 μM IC50. Rest of the compounds (1, 3–9) showed 10.4–28.1 μM IC50 on COX-2 and 17.0–35.6 μM IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1–9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 μM for all compounds (1–9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.
Journal of Surfactants and Detergents, Jun 20, 2022
Osteoarthritis (OA) is the most prevalent kind of joint disease, affecting millions of individual... more Osteoarthritis (OA) is the most prevalent kind of joint disease, affecting millions of individuals worldwide. Allium sativum L. was used as a therapeutic agent in the microemulsion system against osteoarthritis due to allicin's high antioxidant and anti‐inflammatory effects. HPLC was used to evaluate the chemical components of the Allium sativum methanol extract. Water‐in‐oil (w/o) type of microemulsions loaded with Allium sativum extract was produced. To create the microemulsions, a titration approach was employed. The microemulsions were prepared using isopropyl myristate (IPM) as oil, Polysorbate 60, Sorbitan monolaurate 80 as surfactants, and Polyethylene glycol 400, ethanol as cosurfactants. The pH, droplet size, viscosity, polydispersity index values were measured to characterize of microemulsions. In addition, L929 healthy mouse fibroblasts and CHON‐001 healthy human cartilage fibroblast cells were tested for cytocompatibility in vitro. The therapeutic potential of Allium sativum microemulsion was investigated in rats that had osteoarthritis surgically simulated. HPLC analysis revealed a significant concentration of allicin in the extract. The titration approach was used to create an A. sativum microemulsion (AS) with a narrow droplet size and PDI range. In L929 and CHON‐001 cells, cytocompatibility experiments revealed that the maximum dosages of AS microemulsion 5% (v/v) exerted 93.41 ± 3.11% and 75.59 ±2.69% cell viabilities, respectively. Different concentrations of AS (1.25%, 2.5%, and 5% v/v) demonstrated cytoprotective efficacy against H2O2‐induced oxidative damage. When compared to the control group, in vivo investigations revealed fewer irregularities on the articular surface and typically arranged chondrocytes in the positive control and treated groups.
Abstract From the MeOH extract of the aerial parts of Scutellaria brevibracteata subsp. subveluti... more Abstract From the MeOH extract of the aerial parts of Scutellaria brevibracteata subsp. subvelutina 12 secondary metabolites including eight iridoid glycosides (1-8), three flavonoids (9-11) and one phenylethanoid glycoside (12) were isolated. Their structures were elucidated as catalpol (1), globularin (2), scutellarioside II (3), picroside III (4), pensteminoside (5), 8-epiloganic acid (6), albidoside (7), agnucastoside B (8), hispidulin (9), luteolin 7-O-glucuronide (10), hispidulin 7-O-glucuronide (11) and martynoside (12) by using extensive NMR and HR-MS analysis. All compounds are being reported for the first time from S. brevibracteata subsp. subvelutina while compound 5 is new for Lamiaceae family. The chemotaxonomic importance of the isolates was discussed in the detail. All the isolates were evaluated for their in vitro anti-inflammatory activities via their inhibitory actions on the release of nitrite oxide and IL-6 from LPS-induced RAW 264.7 macrophage cells. Compounds 9 and 11 exhibited significant NO reducing capacity at 100 μM concentration comparable to the positive controls, indomethacin and L-NAME. Moreover, 2, 9 and 10 significantly suppressed the release of IL-6 at the same concentration better than the positive controls.
Botulizm, insan ve hayvanlari etkileyen ciddi bir noroparalitik hastaliktir. Hasta- lik, Clostrid... more Botulizm, insan ve hayvanlari etkileyen ciddi bir noroparalitik hastaliktir. Hasta- lik, Clostridium botulinum bakterisi tarafindan uretilen ve bilinen en potent tok- sinlerden biri olan botulinum norotoksininden kaynaklanir. Botulinum norotok- sini sinir fonksiyonlarini bloke ederek solunum ve kas felcine yol acabilmektedir. Literaturde botulizmin en yaygin gorulen bulasma yolu, botulinum norotoksini ile kontamine gidalarin tuketilmesi ile seyreden gida kaynakli botulizmdir. Gida kaynakli botulizm, dunyada oldugu gibi ulkemizde de son yillarda gorulen bazi ardisik vakalar nedeniyle dikkat cekmektedir. Vakalarin buyuk bir cogunlugunun evde dusuk sicakliklarda ve yetersiz pisirme suresiyle pisirilip konserve edilen besinlerin tuketilmesi sonucu olustugu bildirilmektedir. Bu nedenle botulizme dikkat cekebilmek icin cesitli kanallar araciligiyla halki bilinclendirmeye yonelik her turlu egitici materyale ihtiyac duyulmaktadir. Bu derlemede, botulizm tipleri, tedavisi, botulizmden korunm...
Current Topics in Medicinal Chemistry, Mar 1, 2023
: The prevalence of depression has increased dramatically over the past few decades. Alt-hough de... more : The prevalence of depression has increased dramatically over the past few decades. Alt-hough depression is categorized as a brain disorder, its symptomatology includes some behaviors that also occur during chronic inflammatory stress. According to research, cytokine production and immune system activation may have a role in depression, so this relationship has received much at-tention. Moreover, there is a bidirectional relationship between oxidative stress and inflammation. Oxidative stress plays a pathogenic role in chronic inflammatory diseases; depressive disorder is be-ing suggested as one of them. Recent research using several oxidative stress indicators demonstrates that antioxidant defenses are diminished and oxidative stress is elevated in depression. Another cy-tokine-related mechanism widely known for its association with inflammatory illnesses is the kynurenine pathway (KP). KP is responsible for maintaining the balance between neuroprotective and neurogenerative processes in the brain. Therefore, KP plays a role in the pathophysiology of depression. It is thought to impact neurological processes that stem the depression, making it one of the mainstays in explaining oxidative stress-depression-inflammation interrelation. The mechanism is thought to be driven by increasing the expression of proinflammatory cytokines, IDO, and thus the KYN/TRP ratio. This review aims to evaluate the relationship between oxidative stress, depres-sion, and inflammation through the kynurenine pathway through the current studies in the literature.
Journal of The Iranian Chemical Society, Jul 14, 2021
In this study, new carboxamides derived from the imidazo[2,1- b ]thiazole skeleton which are carr... more In this study, new carboxamides derived from the imidazo[2,1- b ]thiazole skeleton which are carrying the biologically active benzoxazole group and are terminated with polar group such as chloro/bromo/cyano as well as imidazothiazole-based methyl carboxylate derivative were synthesized in order to investigate anti-inflammatory and analgesic activities. The new molecules were characterized by FT-IR, 1 H-NMR, 13 C-NMR and ESI–MS spectrometry. New chloro-terminated imidazothiazole-based carboxamide ( 7a ) and imidazothiazole-based methyl carboxylate derivative ( 8 ) showed, respectively, 75.88% and 77.05% cell viability on RAW 264.7 cell line at dose of 1.5 μM and 50 μM whereas trifluoroacetylamino-substituted thiazole carboxylate ( 1 ), trifluoroacetylamino-substituted thiazole carboxamides ( 2 ) and amino-substituted thiazole carboxamides ( 3 ) exhibited non-cytotoxicity by the cell viability value which is higher than 80% at dose of 100 μM except for their brominated derivatives 2b and 3b with highest cytotoxicity. Anti-inflammatory assay of the compounds on RAW 267.7 cells revealed that the compounds N -(4-chlorophenyl)-2-[(trifluoroacetyl)amino]-1,3-thiazole-5-carboxamide ( 2a ) and 2-amino- N -(4-chlorophenyl)-1,3-thiazole-5-carboxamide ( 3a ) which are starting materials in the synthetic route of 7a significantly have similar nitrite reducing effect with indomethacin which is positive control compound. As regarding to analgesic activity, compound 3a showed the highest reducing activity on PGE 2 level induced by LPS than trifluoroacetylamino-substituted carboxamides 2a and 2b as compared with control group.
Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory... more Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with α-hydroxy aldehyde or α-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by 1H NMR, 13C NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 μM and 8.0 μM IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 μM IC50. Rest of the compounds (1, 3–9) showed 10.4–28.1 μM IC50 on COX-2 and 17.0–35.6 μM IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1–9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 μM for all compounds (1–9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.
Journal of Surfactants and Detergents, Jun 20, 2022
Osteoarthritis (OA) is the most prevalent kind of joint disease, affecting millions of individual... more Osteoarthritis (OA) is the most prevalent kind of joint disease, affecting millions of individuals worldwide. Allium sativum L. was used as a therapeutic agent in the microemulsion system against osteoarthritis due to allicin's high antioxidant and anti‐inflammatory effects. HPLC was used to evaluate the chemical components of the Allium sativum methanol extract. Water‐in‐oil (w/o) type of microemulsions loaded with Allium sativum extract was produced. To create the microemulsions, a titration approach was employed. The microemulsions were prepared using isopropyl myristate (IPM) as oil, Polysorbate 60, Sorbitan monolaurate 80 as surfactants, and Polyethylene glycol 400, ethanol as cosurfactants. The pH, droplet size, viscosity, polydispersity index values were measured to characterize of microemulsions. In addition, L929 healthy mouse fibroblasts and CHON‐001 healthy human cartilage fibroblast cells were tested for cytocompatibility in vitro. The therapeutic potential of Allium sativum microemulsion was investigated in rats that had osteoarthritis surgically simulated. HPLC analysis revealed a significant concentration of allicin in the extract. The titration approach was used to create an A. sativum microemulsion (AS) with a narrow droplet size and PDI range. In L929 and CHON‐001 cells, cytocompatibility experiments revealed that the maximum dosages of AS microemulsion 5% (v/v) exerted 93.41 ± 3.11% and 75.59 ±2.69% cell viabilities, respectively. Different concentrations of AS (1.25%, 2.5%, and 5% v/v) demonstrated cytoprotective efficacy against H2O2‐induced oxidative damage. When compared to the control group, in vivo investigations revealed fewer irregularities on the articular surface and typically arranged chondrocytes in the positive control and treated groups.
Abstract From the MeOH extract of the aerial parts of Scutellaria brevibracteata subsp. subveluti... more Abstract From the MeOH extract of the aerial parts of Scutellaria brevibracteata subsp. subvelutina 12 secondary metabolites including eight iridoid glycosides (1-8), three flavonoids (9-11) and one phenylethanoid glycoside (12) were isolated. Their structures were elucidated as catalpol (1), globularin (2), scutellarioside II (3), picroside III (4), pensteminoside (5), 8-epiloganic acid (6), albidoside (7), agnucastoside B (8), hispidulin (9), luteolin 7-O-glucuronide (10), hispidulin 7-O-glucuronide (11) and martynoside (12) by using extensive NMR and HR-MS analysis. All compounds are being reported for the first time from S. brevibracteata subsp. subvelutina while compound 5 is new for Lamiaceae family. The chemotaxonomic importance of the isolates was discussed in the detail. All the isolates were evaluated for their in vitro anti-inflammatory activities via their inhibitory actions on the release of nitrite oxide and IL-6 from LPS-induced RAW 264.7 macrophage cells. Compounds 9 and 11 exhibited significant NO reducing capacity at 100 μM concentration comparable to the positive controls, indomethacin and L-NAME. Moreover, 2, 9 and 10 significantly suppressed the release of IL-6 at the same concentration better than the positive controls.
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