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Enhancement of intestinal tight junction assembly by Coffea arabica pulp aqueous extract: mechanism of action and role of SIRT-1
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-20 DOI: 10.1007/s13596-025-00817-x
Pichayapa Sukmak, Laongdao Thongnak, Wanapas Wachiradejkul, Jakkapong Inchai, Nichapa Chindaduangratn, Natnicha Kitti-udom, Thaam Limwattananon, Nuttakritta Choksukchalalai, Wilasinee Satianrapapong, Sunisa Hankan, Doungporn Amornlerdpison, Atcharaporn Ontawong, Nattaphong Akrimajirachoote, Chanat Aonbangkhen, Chatchai Muanprasat, Chutima S. Vaddhanaphuti, Pawin Pongkorpsakol

Intestinal tight junction disruption is considered as one of key pathogenic factors of several diseases including inflammatory bowel diseases. At present, there is no FDA-approved drug targeting intestinal tight junction recovery. Coffea arabica pulp is an agricultural waste but its aqueous extract contains a number of polyphenol-rich, bioactive compounds. The main aim of this study was to elucidate the pharmacological effects of Coffea arabica pulp aqueous extract (CPE) on intestinal tight junction re-assembly. Transepithelial electrical resistance (TER) measurement indicated that CPE significantly enhanced TER across the intestinal epithelial-like T84 cell monolayers in a time- and dose-dependent manner with a maximal effect being observed at 1,000 µg/ml. MTT assay and nuclear staining indicated that CPE had no cytotoxic effect on T84 cells. Fluorescein isothiocyanate (FITC)-dextran permeability assay demonstrated that CPE suppressed intestinal tight junction-dependent leak pathway permeability. In addition, the effect of CPE on enhancing intestinal tight junction assembly was not affected by inhibitors of calcium/calmodulin-dependent protein kinase kinase β (CaMKKβ), AMP-activated protein kinase (AMPK), and extracellular signal-regulated kinase (ERK). Surprisingly, sirtuin-1 (SIRT-1) inhibitors abrogated CPE-induced tight junction assembly in T84 cell monolayers. Furthermore, immunostaining indicated that CPE enhanced re-distribution of occludin and zonula occludens-1 (ZO-1) to cell junction region via SIRT-1-dependent mechanism. Collectively, CPE may be useful in the treatment of diseases related to intestinal tight junction disruption.

{"title":"Enhancement of intestinal tight junction assembly by Coffea arabica pulp aqueous extract: mechanism of action and role of SIRT-1","authors":"Pichayapa Sukmak,&nbsp;Laongdao Thongnak,&nbsp;Wanapas Wachiradejkul,&nbsp;Jakkapong Inchai,&nbsp;Nichapa Chindaduangratn,&nbsp;Natnicha Kitti-udom,&nbsp;Thaam Limwattananon,&nbsp;Nuttakritta Choksukchalalai,&nbsp;Wilasinee Satianrapapong,&nbsp;Sunisa Hankan,&nbsp;Doungporn Amornlerdpison,&nbsp;Atcharaporn Ontawong,&nbsp;Nattaphong Akrimajirachoote,&nbsp;Chanat Aonbangkhen,&nbsp;Chatchai Muanprasat,&nbsp;Chutima S. Vaddhanaphuti,&nbsp;Pawin Pongkorpsakol","doi":"10.1007/s13596-025-00817-x","DOIUrl":"10.1007/s13596-025-00817-x","url":null,"abstract":"<div><p>Intestinal tight junction disruption is considered as one of key pathogenic factors of several diseases including inflammatory bowel diseases. At present, there is no FDA-approved drug targeting intestinal tight junction recovery. <i>Coffea arabica</i> pulp is an agricultural waste but its aqueous extract contains a number of polyphenol-rich, bioactive compounds. The main aim of this study was to elucidate the pharmacological effects of <i>Coffea arabica</i> pulp aqueous extract (CPE) on intestinal tight junction re-assembly. Transepithelial electrical resistance (TER) measurement indicated that CPE significantly enhanced TER across the intestinal epithelial-like T84 cell monolayers in a time- and dose-dependent manner with a maximal effect being observed at 1,000 µg/ml. MTT assay and nuclear staining indicated that CPE had no cytotoxic effect on T84 cells. Fluorescein isothiocyanate (FITC)-dextran permeability assay demonstrated that CPE suppressed intestinal tight junction-dependent leak pathway permeability. In addition, the effect of CPE on enhancing intestinal tight junction assembly was not affected by inhibitors of calcium/calmodulin-dependent protein kinase kinase β (CaMKKβ), AMP-activated protein kinase (AMPK), and extracellular signal-regulated kinase (ERK). Surprisingly, sirtuin-1 (SIRT-1) inhibitors abrogated CPE-induced tight junction assembly in T84 cell monolayers. Furthermore, immunostaining indicated that CPE enhanced re-distribution of occludin and zonula occludens-1 (ZO-1) to cell junction region via SIRT-1-dependent mechanism. Collectively, CPE may be useful in the treatment of diseases related to intestinal tight junction disruption.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"319 - 329"},"PeriodicalIF":1.8,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466052","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}
引用次数: 0
Loranthus parasiticus extract ameliorates hyperglycemia and improves insulin sensitivity in C57BL/Ksj-db/db mice
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-02 DOI: 10.1007/s13596-024-00813-7
Jung Kyung Lee, Jae Eun Park, Ji Sook Han

Loranthus parasiticus Merr. (L. parasiticus) is a semiparasitic plant and it has antidiabetic effects. But potential application of L. parasiticus to improve insulin sensitivity in mice with type 2 diabetes remains unexplored.

Herein, we aimed to investigate the potential antidiabetic effects of L. parasiticus extract (LPE) on hyperglycemia and insulin sensitivity in C57BL/Ksj-db/db mice. C57BL/Ksj-db/db mice were divided into three groups: diabetic control, rosiglitazone, and LPE. Db/db-control group was fed a standard semi-synthetic diet (AIN-93 G), db/db-RG group was fed AIN-93 G supplemented with rosiglitazone (RG) (0.005%, w/w), and db/db-LPE group was fed AIN-93 G supplemented with LPE (0.5%, w/w) for 6 weeks. Mice supplemented with LPE exhibited significantly lower blood glucose and glycosylated hemoglobin levels than diabetic control mice. Compared with diabetic control mice, LPE-supplemented mice exhibited a significant reduction in the homeostatic index of insulin resistance. LPE supplementation stimulated the pIRS Tyr612 and AktSer473, as well as the activation of PI3K in the skeletal muscle insulin signaling pathway. Furthermore, LPE supplementation significantly increased the pAMPKThr172 and ACCSer79 and the expression of plasma membrane GLUT4. LPE supplementation improves insulin sensitivity and alleviates hyperglycemia in diabetic mice.

{"title":"Loranthus parasiticus extract ameliorates hyperglycemia and improves insulin sensitivity in C57BL/Ksj-db/db mice","authors":"Jung Kyung Lee,&nbsp;Jae Eun Park,&nbsp;Ji Sook Han","doi":"10.1007/s13596-024-00813-7","DOIUrl":"10.1007/s13596-024-00813-7","url":null,"abstract":"<div><p><i>Loranthus parasiticus</i> Merr. (<i>L. parasiticus</i>) is a semiparasitic plant and it has antidiabetic effects. But potential application of <i>L. parasiticus</i> to improve insulin sensitivity in mice with type 2 diabetes remains unexplored.</p><p>Herein, we aimed to investigate the potential antidiabetic effects of <i>L. parasiticus</i> extract (LPE) on hyperglycemia and insulin sensitivity in C57BL/Ksj-db/db mice. C57BL/Ksj-db/db mice were divided into three groups: diabetic control, rosiglitazone, and LPE. Db/db-control group was fed a standard semi-synthetic diet (AIN-93 G), db/db-RG group was fed AIN-93 G supplemented with rosiglitazone (RG) (0.005%, w/w), and db/db-LPE group was fed AIN-93 G supplemented with LPE (0.5%, w/w) for 6 weeks. Mice supplemented with LPE exhibited significantly lower blood glucose and glycosylated hemoglobin levels than diabetic control mice. Compared with diabetic control mice, LPE-supplemented mice exhibited a significant reduction in the homeostatic index of insulin resistance. LPE supplementation stimulated the pIRS <sup>Tyr612</sup> and Akt<sup>Ser473</sup>, as well as the activation of PI3K in the skeletal muscle insulin signaling pathway. Furthermore, LPE supplementation significantly increased the pAMPK<sup>Thr172</sup> and ACC<sup>Ser79</sup> and the expression of plasma membrane GLUT4. LPE supplementation improves insulin sensitivity and alleviates hyperglycemia in diabetic mice.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"309 - 317"},"PeriodicalIF":1.8,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143465900","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}
引用次数: 0
Ginger-derived nanovesicles inhibit breast cancer cell proliferation by induction of apoptosis
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-18 DOI: 10.1007/s13596-024-00811-9
Vinayak Sharma, Eshu Singhal Sinha, Jagtar Singh

Breast cancer is a prevalent and life-threatening disease affecting women globally. Despite advances in cancer treatment, there is a pressing need for effective and low-toxicity anticancer agents. Recent research has highlighted the potential of nanosized extracellular vesicles derived from edible plants in modulating cell function and facilitating biomolecule transport between cells. Mounting evidences suggests the anticancer potential of nanovesicles derived various edible plants against different types of cancer. However, the potential of nanovesicles derived from ginger in treating breast cancer remains unexplored.

In this study, we aimed to investigate the therapeutic effects of ginger derived nanovesicles (GiDNVs) on breast cancer cell lines (MDA-MB-231 and MDA-MB-468). To accomplish our goal, we isolated nanovesicles from ginger using the differential centrifugation method and characterized their size and integrity by employing DLS and FESEM. Subsequently, we evaluated the therapeutic effects of these GiDNVs on breast cancer cells. Our results demonstrated that GiDNVs inhibited cancer cell proliferation in a dosage and time-dependent way. Furthermore, flow cytometry analyses and DAPI staining demonstrated that the anti-proliferative effect of GiDNVs was attributed to the induction of apoptosis in cancer cells. Additionally, western blotting analysis showed that the apoptotic effect of GiDNVs on breast cancer cell was mainly mediated modulation by bcl-2, bax and caspase-3. This study contributes to the development of novel and effective anticancer agents with minimal toxicity. In nutstell these findings highlight the ability of GiDNVs as a novel and effective anti-cancerous agent for breast cancer treatment.

{"title":"Ginger-derived nanovesicles inhibit breast cancer cell proliferation by induction of apoptosis","authors":"Vinayak Sharma,&nbsp;Eshu Singhal Sinha,&nbsp;Jagtar Singh","doi":"10.1007/s13596-024-00811-9","DOIUrl":"10.1007/s13596-024-00811-9","url":null,"abstract":"<div><p>Breast cancer is a prevalent and life-threatening disease affecting women globally. Despite advances in cancer treatment, there is a pressing need for effective and low-toxicity anticancer agents. Recent research has highlighted the potential of nanosized extracellular vesicles derived from edible plants in modulating cell function and facilitating biomolecule transport between cells. Mounting evidences suggests the anticancer potential of nanovesicles derived various edible plants against different types of cancer. However, the potential of nanovesicles derived from ginger in treating breast cancer remains unexplored.</p><p>In this study, we aimed to investigate the therapeutic effects of ginger derived nanovesicles (GiDNVs) on breast cancer cell lines (MDA-MB-231 and MDA-MB-468). To accomplish our goal, we isolated nanovesicles from ginger using the differential centrifugation method and characterized their size and integrity by employing DLS and FESEM. Subsequently, we evaluated the therapeutic effects of these GiDNVs on breast cancer cells. Our results demonstrated that GiDNVs inhibited cancer cell proliferation in a dosage and time-dependent way. Furthermore, flow cytometry analyses and DAPI staining demonstrated that the anti-proliferative effect of GiDNVs was attributed to the induction of apoptosis in cancer cells. Additionally, western blotting analysis showed that the apoptotic effect of GiDNVs on breast cancer cell was mainly mediated modulation by bcl-2, bax and caspase-3. This study contributes to the development of novel and effective anticancer agents with minimal toxicity. In nutstell these findings highlight the ability of GiDNVs as a novel and effective anti-cancerous agent for breast cancer treatment.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"297 - 308"},"PeriodicalIF":1.8,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466038","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}
引用次数: 0
Eggplant (Solanum melongena L.) extract improves glucose uptake in LPS-induced inflammation in Caco-2/macrophages co-culture model
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-04 DOI: 10.1007/s13596-024-00806-6
Atcharaporn Ontawong, Doungporn Amornlerdpison, Teerawat Rattanaphot, Sirinat Pengnet, Kullanat Kuntakhut

The inflammatory bowel disease (IBD) patients have increased intestinal glucose absorption associated with hyperglycemia and diabetes mellitus. Thus, IBD treatment might minimize diabetic mellitus risk. Eggplant extract is frequently prescribed in traditional Chinese medicine and is effective against various diseases, including cancer, cardiovascular disease, and respiratory infections. It contains active compounds; chlorogenic acid (CGA) exhibits anti-inflammatory and anti-hyperglycemic effects. However, the effect of eggplant extract (EPE) on intestinal glucose uptake in IBD is unknown. Thus, this study uses LPS-induced inflammation in a co-culture model to mimic IBD. This work determined the impact of EPE glucose transport in the inflammatory co-culture model—the caco-2 cells in a transwell insert plate on LPS-induced inflammatory THP-1-derived macrophages. Caco-2 cells were treated with various doses of EPE. Inflammatory parameters and intestinal glucose transport function of Caco-2 cells were studied. It was observed that EPE inhibited proinflammatory cytokine gene expression and production. Furthermore, EPE inhibited intestinal glucose absorption under inflammatory conditions. These data suggested that EPE may attenuate inflammatory conditions and glucose absorption in the inflammatory co-cultures model; however, the molecular mechanisms underlying the effects of EPE must be evaluated through further investigation.

Graphical Abstract

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引用次数: 0
Exploring the therapeutic potential of Ixora extract: a comprehensive review of mediated studies
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-13 DOI: 10.1007/s13596-024-00797-4
Rabiyah Nadeem, Muhammad Imran, Zohaib Saeed, Muhammad Pervaiz, Umer Younas

Traditional Herbal Medicine Systems, commonly known as Complementary and Alternative Systems of Medicine, is currently one of the most extensively researched subjects. The genus Ixora belongs to the family Rubiaceae, which is commonly referred to as the Madder family. It comprises 500 species and is one of the most investigated herbs today. For centuries, ethnic groups have incorporated various parts of the Ixora plant (flowers, leaves, stems, and roots) into Ayurvedic medicine to treat a range of ailments, including hepatic disorders, diarrhea, cancer, tumors, microbial infections, antioxidants, pain, ulcers, anti-tumor properties, and anti-inflammatory effects. Due to the extensive use of the Ixora genus in traditional medicine, researchers were compelled to examine the phytochemical composition of its various species. Multiple studies on the genus Ixora, which belongs to the Rubiaceae family, have uncovered a rich assortment of phenolic compounds. These include flavonoids, tannins, aromatic acrid oils, poly-sterols, saponins, carbohydrates, fatty acids, peptides, and terpenoids. Over the past 50 years, extensive phytochemical studies have been conducted on the genus Ixora, these studies have not only revealed the composition of the plant extract, but they have also helped to develop a comprehensive pharmacological profile. In doing so, these studies have provided scientific evidence supporting the ethno-medicinal uses of the plant. Every part of various Ixora species is said to possess beneficial properties which have added to its value as a medicinal plant. The purpose of this review is to thoroughly analyze the phytochemical and pharmacological properties of the Ixora genus. Along the way present an updated and categorized compilation of the scientific evidence of its medicinal properties. As a result, it aims to inspire scholars to pursue additional research on this particular genus.

Graphical abstract

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引用次数: 0
Anti-diarrhoea properties of ethanol extract of Citrullus colocynthis fruit pulp: in vivo and in silico studies
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-16 DOI: 10.1007/s13596-024-00783-w
Asiat Na’Allah, Simbiat Bashir, Mutiu Alabi, Fatai A. Kareem, Gabriel O. Olaifa, Femi J. Afolabi, Sesan Abiodun Aransiola, Chandra Shekhar Seth, Naga Raju Maddela, Ram Prasad

This study aimed to establish anti-diarrhoea agents, through in vivo and in silico molecular modelling from the phytoconstituents of Citrullus colocynthis ethanol fruit pulp extract (CCEFPE). The crystal structure of µ (mu) opioid and aquaporin 4 (AQP4) receptors were retrieved from the RCSB database, while the identified compounds from C. colocynthis ethanol fruit pulp extract were sequentially docked via Schrödinger suite. In CCEFPE in vivo anti-diarrhoea studies, control received distilled water (2 mL/kg, p.o.), diarrhoea was administered with castor oil or MgSO4 (2 mL/kg, p.o.), standard drug was administered 2 mg/kg, p.o. loperamide, while CCEFPE (50, 100 and 150 mg/kg, p.o.) was administered to the treated groups. Seven hit compounds out of which 54 displayed relatively higher free binding energy for mu opioid and AQP4. Swiss ADME predicted compounds 54 to be blood–brain impermeant, have low gastrointestinal absorption, strong druglike-ness, and safety profile among the hits. In the in vivo study, the onset of diarrhoea was significantly (p < 0.05) delayed by CCEFPE. A significant reduction (p < 0.05) in gastrointestinal motility, enteropooling and PGE2 in diarrhoea-induced groups was also observed after CCEFPE administration. Compound 54, even though it has drug-like properties, displayed a weak interaction with the receptor and hence can be structurally modified to an analogue of loperamide for a better ligand-receptor interaction while the in vivo studies confirmed the anti-diarrhoea activities of C. colocynthis ethanol fruit pulp extract.

{"title":"Anti-diarrhoea properties of ethanol extract of Citrullus colocynthis fruit pulp: in vivo and in silico studies","authors":"Asiat Na’Allah,&nbsp;Simbiat Bashir,&nbsp;Mutiu Alabi,&nbsp;Fatai A. Kareem,&nbsp;Gabriel O. Olaifa,&nbsp;Femi J. Afolabi,&nbsp;Sesan Abiodun Aransiola,&nbsp;Chandra Shekhar Seth,&nbsp;Naga Raju Maddela,&nbsp;Ram Prasad","doi":"10.1007/s13596-024-00783-w","DOIUrl":"10.1007/s13596-024-00783-w","url":null,"abstract":"<div><p>This study aimed to establish anti-diarrhoea agents, through in vivo and in silico molecular modelling from the phytoconstituents of <i>Citrullus colocynthis</i> ethanol fruit pulp extract (CCEFPE). The crystal structure of µ (mu) opioid and aquaporin 4 (AQP4) receptors were retrieved from the RCSB database, while the identified compounds from <i>C. colocynthis</i> ethanol fruit pulp extract were sequentially docked via Schrödinger suite. In CCEFPE in vivo anti-diarrhoea studies, control received distilled water (2 mL/kg, p.o.), diarrhoea was administered with castor oil or MgSO<sub>4</sub> (2 mL/kg, p.o.), standard drug was administered 2 mg/kg, p.o. loperamide, while CCEFPE (50, 100 and 150 mg/kg, p.o.) was administered to the treated groups. Seven hit compounds out of which 54 displayed relatively higher free binding energy for mu opioid and AQP4. Swiss ADME predicted compounds 54 to be blood–brain impermeant, have low gastrointestinal absorption, strong druglike-ness, and safety profile among the hits. In the in vivo study, the onset of diarrhoea was significantly (<i>p</i> &lt; 0.05) delayed by CCEFPE. A significant reduction (<i>p</i> &lt; 0.05) in gastrointestinal motility, enteropooling and PGE<sub>2</sub> in diarrhoea-induced groups was also observed after CCEFPE administration. Compound 54, even though it has drug-like properties, displayed a weak interaction with the receptor and hence can be structurally modified to an analogue of loperamide for a better ligand-receptor interaction while the in vivo studies confirmed the anti-diarrhoea activities of <i>C. colocynthis</i> ethanol fruit pulp extract.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"269 - 285"},"PeriodicalIF":1.8,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143465996","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}
引用次数: 0
Therapeutic potential of freeze-dried Kaempferia galanga herbal formulation in alleviating hyperglycemia in diabetic mice: an in-vivo and in-silico investigation
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-27 DOI: 10.1007/s13596-024-00784-9
Flavius Phrangsngi Nonglang, Revelbornstar Snaitang, Dhritiman Roy, Shankupar Rynjah, Surya Bhan

A never-ending search is being made for a natural remedy to cure diabetes, which is one of the biggest worldwide health concerns. Kaempferia galanga (K. galanga), an important medicinal herb, is reported to have various pharmacological effects. This study aims to conduct in-depth research on the antihyperglycemic activity of K galanga in streptozotocin (STZ)-induced diabetic mice and the mechanism by which it elicits its response. For 21 days, various dosages of freeze-dried K. galanga ethanolic extract (KGE) therapy were given intraperitoneally in STZ-induced diabetic mice. KGE at 350 mg/kg b.w. was selected as the ideal dose. Acute toxicology studies have shown that KGE is non-toxic. Protein and gene expression studies targeting various metabolic pathways show that in the diabetic mice treated with KGE, there was stimulation of AKT, inhibition of glycogen synthase kinase-3, stimulation of glucokinase (GK), and inhibition of phosphoenolpyruvate carboxykinase (PEPCK) expression. Histopathological studies show the protective effect of herbal KGE on the integrity of the mice's pancreas. Molecular docking studies was performed in which the bio-active compound ethyl-p-methoxy cinnamate (EPMC) found in KGE shows good binding energy with the target protein AKT, GSK3, insulin receptor (IR), protein-tyrosine phosphatase 1B (PTB1B), GK, and PEPCK, indicating a good binding interaction. ADMET studies also revealed that EPMC has desirable physicochemical and pharmacokinetic properties and very low toxicity (LD 50 7900 mg/kg) compared to standard metformin (LD50 680 mg/kg). Herbal KGE and EPMC show a pleiotropic therapeutic effect and may be a potent adjunct and drug, respectively, in attenuating diabetes.

Graphical Abstract

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引用次数: 0
Investigation of biological activities of in vitro grown Sesamum orientale plant extract on the cell cultures: wound healing and antiproliferation
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-22 DOI: 10.1007/s13596-024-00791-w
Sevil Yeniocak, Selin Galatalı, İrem Demir, Aysel Uğur, Nurdan Saraç, Ergun Kaya

Sesame has gained significant attention in the pharmaceutical industry for its antifungal, antiproliferative, antioxidant, and antiproliferative properties, as well as its use as a nutritional supplement. Additionally, sesame is a good source of vitamins B and E and has shown potential as a food that can lower serum cholesterol, balance blood pressure, and aid wound healing. In vitro grown Sesamum orientale L. cv. "Gökova" are presently undergoing tests to determine their cytotoxic, wound-healing, and antiproliferative properties using L929 fibroblasts, A549 lung epithelial, and MCF-7 breast cell lines. The IC50 values for A549 were 922.73 g ml−1 (extract) and 33.09 g ml−1 (cisplatin), 1837.07 g ml−1 (extract) and 19.27 g ml−1 (cisplatin), and for L929 they were 154.70 g ml−1 (extract). The subcytotoxic dosages of the extract demonstrated wound healing in L929 fibroblast cell cultures within 48 h. The transcripts of the BCL-XL gene, which exhibit an inverse correlation with the apoptotic pathway, and the transcripts of the Cas3 and Cas9, which show a positive correlation with the apoptotic pathway, were scrutinized to ascertain the anti-cancer properties. The study revealed a significant increase in gene expression in A549 and MCF-7 lines after exposure to plant extract or cisplatin. The findings suggest that sesame extract can promote wound healing at lower doses and exhibit antiproliferative activity at higher doses. The study provides a promising foundation for the development of a pharmacological drug that offers wound-healing and/or antiproliferative effects. The product has potential applications across a range of future projects and can be utilised with numerous cell lines.

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引用次数: 0
The synthesis, application and therapeutic perspectives of medicinal plants-based solid lipid nanoparticles: a comprehensive review
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-21 DOI: 10.1007/s13596-024-00787-6
MohammadSadeq Mottaqi, Mohammad Amin Langarizadeh, Neda Molaali, Masoud Rezaei, Alieh Ameri, Hamid Forootanfar

Lipid-based drug carriers have gained massive amounts of interest in the last two-decade period as a way to deliver drugs that are not particularly water-soluble. Pharmaceutical uses of lipid nanocarriers include carrying and administering a wide range of therapeutic ingredients. Solid lipid nanoparticles (SLNs) were designed and formulated to rise above the disadvantages of existing colloidal systems, including microemulsions, liposomes and polymeric nanoparticles, by offering benefits such as a favorable release profile and targeted medication distribution while having great physical integrity. We sought to evaluate the recent findings on the current issue to provide a comprehensive perspective of the subject utilizing an extensive literature search to pinpoint the latest scientific reports on this subject. The focus of this paper is on the research employing SLNs for delivery of medicinal plants and testing them in vitro and in vivo. There are a number various standard variables affecting the release of compounds from SLNs throughout all administration routes. Further, the current paper comprehensively elucidates assorted prospects of SLNs. Next, the investigated SLNs encapsulating herbal compounds in scientific articles are reviewed in details. As many herbal compounds are hydrophobic substances, the SLNs encapsulating them can be beneficial in various therapeutic applications. The most studies herbal compounds are Curcumin, followed by Silibinin and Artemisinin.

{"title":"The synthesis, application and therapeutic perspectives of medicinal plants-based solid lipid nanoparticles: a comprehensive review","authors":"MohammadSadeq Mottaqi,&nbsp;Mohammad Amin Langarizadeh,&nbsp;Neda Molaali,&nbsp;Masoud Rezaei,&nbsp;Alieh Ameri,&nbsp;Hamid Forootanfar","doi":"10.1007/s13596-024-00787-6","DOIUrl":"10.1007/s13596-024-00787-6","url":null,"abstract":"<div><p>Lipid-based drug carriers have gained massive amounts of interest in the last two-decade period as a way to deliver drugs that are not particularly water-soluble. Pharmaceutical uses of lipid nanocarriers include carrying and administering a wide range of therapeutic ingredients. Solid lipid nanoparticles (SLNs) were designed and formulated to rise above the disadvantages of existing colloidal systems, including microemulsions, liposomes and polymeric nanoparticles, by offering benefits such as a favorable release profile and targeted medication distribution while having great physical integrity. We sought to evaluate the recent findings on the current issue to provide a comprehensive perspective of the subject utilizing an extensive literature search to pinpoint the latest scientific reports on this subject. The focus of this paper is on the research employing SLNs for delivery of medicinal plants and testing them in vitro and in vivo. There are a number various standard variables affecting the release of compounds from SLNs throughout all administration routes. Further, the current paper comprehensively elucidates assorted prospects of SLNs. Next, the investigated SLNs encapsulating herbal compounds in scientific articles are reviewed in details. As many herbal compounds are hydrophobic substances, the SLNs encapsulating them can be beneficial in various therapeutic applications. The most studies herbal compounds are Curcumin, followed by Silibinin and Artemisinin.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"69 - 105"},"PeriodicalIF":1.8,"publicationDate":"2024-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143465973","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}
引用次数: 0
Chemical, elemental, morphological and toxicological characteristics of traditional Indian Siddha formulation: Kasthuri Karuppu
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-18 DOI: 10.1007/s13596-024-00790-x
N. Kannan, Anil Kumar NV, S. Balaji

The chemical, elemental, morphological and toxicological characteristics of organometallic formulation (Kasthuri Karuppu) were assessed using UV-spectrophotometer, X-ray photoelectron spectroscopy, Fourier transform infrared spectroscopy, ICP-OES, Energy dispersive X-ray, XRD and Zeta potential. The physical properties such as size (10–80 nm), surface area (3.1 m2/g), surface charge (-36mV), and bandgap energy (3.6 eV) were correlated with reactivity. Based on the elemental distribution of Hg, As and S, the proportion favours HgS that is less toxic and reactive. There were no toxic effects of the tested formulation at concentration 60 µg/mL against normal and cancer cells (observed during 24 h). However, the increase in time duration (72 h) had lethal effects in both the cells. The developmental toxicity of the organometallic formulation was assessed in Zebrafish embryos. The safe dosage was found to be 100 µg/mL. The toxicity of the formulation in vitro and in vivo is based on the exposure time and dosage.

{"title":"Chemical, elemental, morphological and toxicological characteristics of traditional Indian Siddha formulation: Kasthuri Karuppu","authors":"N. Kannan,&nbsp;Anil Kumar NV,&nbsp;S. Balaji","doi":"10.1007/s13596-024-00790-x","DOIUrl":"10.1007/s13596-024-00790-x","url":null,"abstract":"<div><p>The chemical, elemental, morphological and toxicological characteristics of organometallic formulation (<i>Kasthuri Karuppu</i>) were assessed using UV-spectrophotometer, X-ray photoelectron spectroscopy, Fourier transform infrared spectroscopy, ICP-OES, Energy dispersive X-ray, XRD and Zeta potential. The physical properties such as size (10–80 nm), surface area (3.1 m<sup>2</sup>/g), surface charge (-36mV), and bandgap energy (3.6 eV) were correlated with reactivity. Based on the elemental distribution of Hg, As and S, the proportion favours HgS that is less toxic and reactive. There were no toxic effects of the tested formulation at concentration 60 µg/mL against normal and cancer cells (observed during 24 h). However, the increase in time duration (72 h) had lethal effects in both the cells. The developmental toxicity of the organometallic formulation was assessed in Zebrafish embryos. The safe dosage was found to be 100 µg/mL. The toxicity of the formulation in vitro and in vivo is based on the exposure time and dosage.</p></div>","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 1","pages":"221 - 231"},"PeriodicalIF":1.8,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13596-024-00790-x.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143465929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Advances in Traditional Medicine
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