scholarly journals Impact of Sodium N-[8-(2-Hydroxybenzoyl)amino]-caprylate on Intestinal Permeability for Notoginsenoside R1 and Salvianolic Acids in Caco-2 Cells Transport and Rat Pharmacokinetics

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2990 ◽  
Author(s):  
Ying Li ◽  
Dandan Yang ◽  
Chunyan Zhu
Keyword(s):  
Membrane Permeability ◽  
Cell Monolayer ◽  
Salvianolic Acid B ◽  
Absorption Enhancement ◽  
Enhancement Effect ◽  
Absorption Enhancers ◽  
Salvianolic Acid ◽  
Salvianolic Acids

For drugs with high hydrophilicity and poor membrane permeability, absorption enhancers can promote membrane permeability and improve oral bioavailability. Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) is a new kind of absorption enhancer that has good safety. To investigate the absorption enhancement effect of SNAC on non-polar charged and polar charged drugs and establish the absorption enhancement mechanism of SNAC, SNAC was synthesized and characterized. Two representative hydrophilic drugs—notoginsenoside R1 (R1) and salvianolic acids (SAs)—were selected as model drugs. In vitro Caco-2 cells transport and in vivo rat pharmacokinetics studies were conducted to examine the permeation effect of SNAC on R1 and SAs. R1, rosmarinic acid (RA), salvianolic acid B (SA-B) and salvianolic acid B (SA-A) were determined to compare the permeation enhancement of different drugs. The MTT assay results showed that SNAC had no toxicity to Caco-2 cells. The transepithelial electrical resistance (TEER) of Caco-2 cell monolayer displayed that SNAC facilitated passive transport of polar charged SAs through the membrane of epithelial enterocytes. The pharmacokinetics results demonstrated that area under the curve (AUC) of RA, SA-B and SA-A with administration of SAs containing SNAC was 35.27, 8.72 and 9.23 times than administration of SAs. Tmax of RA, SA-B and SA-A were also prolonged. The AUC of R1 with administration of R1 containing SNAC was 2.24-times than administration of R1. SNAC is more effective in promoting absorption of SAs than R1. The study demonstrated that SNAC significantly improved bioavailability of R1 and SAs. What’s more, the effect of SNAC on absorption enhancement of charged drugs was larger than that of non-charged drugs. The current findings not only confirm the usefulness of SNAC for the improved delivery of R1 and SAs but also demonstrate the importance of biopharmaceutics characterization in the dosage form development of drugs.

Salvianolic acid B exerts anti-liver fibrosis effects via inhibition of MAPK-mediated phospho-Smad2/3 at linker regions in vivo and in vitro

Life Sciences ◽  
2019 ◽  
Vol 239 ◽  
pp. 116881 ◽  
Author(s):  
Chao Wu ◽  
Weiyang Chen ◽  
Hanyan Ding ◽  
Dong Li ◽  
Guanghua Wen ◽  
...  
Keyword(s):  
Liver Fibrosis ◽  
Salvianolic Acid B ◽  
Salvianolic Acid

scholarly journals Salvianolic acid-B improves fat graft survival by promoting proliferation and adipogenesis

2021 ◽  
Author(s):  
Jia-Ming Sun ◽  
Chia-Kang Ho ◽  
Ya Gao ◽  
Chio-Hou Chong ◽  
Dan-Ning Zheng ◽  
...  
Keyword(s):  
Stem Cells ◽  
Graft Survival ◽  
Salvia Miltiorrhiza ◽  
Salvianolic Acid B ◽  
Fat Graft ◽  
Fat Transplantation ◽  
Salvianolic Acid ◽  
Fat Grafts

Abstract Background: Our previous study proved that Salvia miltiorrhiza could enhance fat graft survival by promoting adipogenesis. However, the effect of salvianolic acid B (Sal-B), the most abundant and bioactive water-soluble compound in Salvia miltiorrhiza, on fat graft survival has not yet been investigated.Objective: This study aims to investigate whether salvianolic acid B could improve fat graft survival and promote preadipocyte differentiation. The underlying mechanism has also been studied.Methods: In vivo, 0.2 ml of Coleman fat was transplanted into nude mice with salvianolic acid B. The grafts were evaluated by HE and IF at 2 and 4 weeks posttransplantation and by micro-CT at 4 weeks posttransplantation. In vitro, the adipogenesis and proliferative activities of salvianolic acid B were analyzed in cultured human adipose-derived stem cells (h-ADSCs) and 3T3-L1 cells to detect the mechanism by which salvianolic acid B affects graft survival.Results: In vivo, the weights and volumes of the fat grafts in the Sal-B-treated groups were significantly higher than those of the fat grafts in the control group. In addition, higher fat integrity and more viable adipocytes were observed in the Sal-B-treated groups. In vitro, salvianolic acid B showed the ability to promote 3T3-L1 and h-ADSC proliferation and adipogenesis.Conclusions: Our in vitro experiments demonstrated that salvianolic acid B can promote the proliferation of adipose stem cells and enhance the differentiation of adipose stem cells. Simultaneously, in vivo experiments showed that salvianolic acid B can improve the survival rate of fat transplantation. Therefore, our research shed light on the potential therapeutic usage of salvianolic acid B in improving the survival rate of fat transplantation.

Salvianolic acid B exerts a protective effect in acute liver injury by regulating the Nrf2/HO-1 signaling pathway

2020 ◽  
Vol 98 (3) ◽  
pp. 162-168 ◽  
Author(s):  
Yong-mei Jin ◽  
Xiang-ming Tao ◽  
Yi-ning Shi ◽  
Youjin Lu ◽  
Jin-yu Mei
Keyword(s):  
Liver Injury ◽  
Signaling Pathway ◽  
Acute Liver Injury ◽  
Damage Model ◽  
Underlying Mechanism ◽  
Salvianolic Acid B ◽  
Salvianolic Acid ◽  
Injury Model

Salvianolic acid B (Sal B) exerts strong antioxidant activity and eliminates the free radical effect. However, how it affects the antioxidant pathway is not very clear. The objective of this study was to investigate the underlying mechanism of Sal B in CCl4-induced acute liver injury, especially its effect on the Nrf2/HO-1 signaling pathway. For the in vivo experiment, an acute liver injury model was induced using CCl4 and treated with Sal B. For the in vitro experiment, an oxidative damage model was established followed by Sal B treatment. Serum biochemical indicators and reactive oxygen species activity were detected using corresponding kits. Oxidant/antioxidant status was determined based on the levels of malondialdehyde, glutathione, and superoxide dismutase. Nrf2 and HO-1 levels were analyzed by Western blotting and immunohistochemical staining. Sal B treatment improved liver histology, decreased the aminotransferase levels, and attenuated oxidative stress in the acute liver injury model. Nrf2 and HO-1 levels were increased both in vivo and in vitro. Sal B suppresses acute liver injury and Nrf2/HO-1 signaling plays a key role in this process.

scholarly journals Absorption enhancement effect of piperine and chitosan on ganciclovir sol-id lipid nanoparticles: formulation, optimization and invivo pharmacoki-netics

2019 ◽  
Vol 10 (2) ◽  
pp. 1143-1151
Author(s):  
Ravindra Babu M ◽  
Ravi Prakash P ◽  
Devanna N
Keyword(s):  
Elimination Rate ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Absorption Enhancement ◽  
Enhancement Effect ◽  
Pharmacokinetic Studies ◽  
Class Iii ◽  
Absorption Enhancers ◽  
Pure Drug

The purpose of the present study was to formulate Solid Lipid Nanoparticles (SLNs) of Ganciclovir (GCV) in combination with Chitosan and Piperine for absorption enhancement effect. GCV loaded SLNs were prepared by hot homogenization method, optimized and characterized. Formulated SLNs were incorporated with absorption enhancers and characterized for invitro absorption (with chicken intestine), histopathological and invivo pharmacokinetic studies. Invitro absorption studies revealed that the permeability coefficient of the prepared formulation is more when compared to the pure drug, so the permeability is more for prepared formulation. In vivo pharmacokinetic study showed a significant increase in the Cmax, AUC, biological half-life and decrease in elimination rate constant for prepared formulation compared to pure drug. Histopathological studies also showed mild reversible damage of epithelial cells with Chitosan which indicates the safety and efficacy of the formulation. Thus, GCV loaded SLNs prepared with Chitosan can be clinically promising for enhancing the oral, intestinal absorption of the said BCS Class-III drug.

scholarly journals Salvianolic Acid B Improves the Effect of Fat Grafts by Inhibiting the NF-kB Signalling Pathway in Macrophages

2021 ◽  
Author(s):  
Jia-Ming Sun ◽  
Chia-Kang Ho ◽  
Ya Gao ◽  
Chio-Hou Chong ◽  
Yang-Dan Liu ◽  
...  
Keyword(s):  
Graft Survival ◽  
Salvia Miltiorrhiza ◽  
Salvianolic Acid B ◽  
Raw264.7 Cells ◽  
Fat Transplantation ◽  
Salvianolic Acid ◽  
Fat Grafts ◽  
Anti Inflammatory

Abstract Background Autologous fat grafting (AFG), although an appealing approach to repair soft tissue defects, has various complications. Excessive inflammation at the transplant site is one of the main reasons for the poor effect of fat transplantation and occurrence of complications. Our previous study proved that Salvia miltiorrhiza can enhance fat graft survival. Salvianolic acid B (Sal-B) is the most abundant and bioactive water-soluble compound in Salvia miltiorrhiza and has anti-inflammatory effects on other diseases. Therefore, we hypothesized that salvianolic acid B could improve the effect of fat grafts by inhibiting inflammation. Methods In vivo, 0.2 ml of Coleman fat was transplanted into nude mice with salvianolic acid B. The grafts were evaluated by HE and IF at 2, 4 and 12 weeks posttransplantation and by micro-CT at 4 weeks posttransplantation. In vitro, the proliferative and anti-inflammatory activities of salvianolic acid B were analyzed in cultured RAW264.7 cells to detect the mechanism by which salvianolic acid B affects graft survival by inhibiting inflammation. Results In vivo, the degree of adipose tissue fibrosis and inflammatory cell infiltration in the salvianolic acid B treatment group was lower, and the infiltration of M1 macrophages in fat grafts was also less than that in the control group. In vitro, salvianolic acid B inhibited the proliferation and activation of inflammatory pathways in RAW264.7 cells. Conclusions This study demonstrates the use of salvianolic acid B as a possible treatment to improve the effect of fat transplantation.

scholarly journals Salvianolic acid B: In vitro and in vivo effects on the immune system

2017 ◽  
Vol 69 (4) ◽  
pp. 658-663 ◽  
Author(s):  
Milica Vujicic ◽  
Tamara Saksida ◽  
Ivana Stojanovic
Keyword(s):  
Autoimmune Diabetes ◽  
Autoimmune Disorder ◽  
Salvianolic Acid B ◽  
Salvianolic Acid ◽  
Other Substances ◽  
Autoreactive Cells ◽  
Antiinflammatory Effects ◽  
In Vivo Effects

Type 1 diabetes (T1D) is an autoimmune disorder with a strong inflammatory component. Autoreactive cells specifically target insulin-producing ?-cells, which leads to loss of glucose homeostasis. T1D remains incurable and versatile; potentially beneficial therapeutics are being tested worldwide. Possible candidates for the treatment of autoimmune diabetes are plants and their extracts since they are rich in biophenols, substances that act as secondary metabolites, and have verified antioxidant and antiinflammatory effects. Salvianolic acid B (SalB) is a biophenol and one of the major constituents of Origanum vulgare ssp. hirtum (Greek oregano) extracts which in our previous studies was shown to exhibit an antidiabetic effect in mice. The aim of the present study was to determine whether SalB is responsible for the observed effects of Greek oregano extracts. SalB was applied in vitro to macrophages and lymphocytes isolated from C57BL/6 mice, as well as in vivo in the model of T1D induced by multiple low doses (MLD) of streptozotocin (STZ). SalB did not affect the viability of cells, but it significantly decreased secretion of nitric oxide (NO) and TNF in lipopolysaccharide (LPS)-stimulated macrophages, as well as the secretion of IFN-? in concanavalin A (ConA)-stimulated lymphocytes. However, when applied in vivo, SalB at a dose of 2.5 mg/kg b.w., applied for 10 consecutive days, failed to protect mice from diabetes development. In conclusion, SalB exerts immunomodulatory effects in vitro, but is not effective in prevention of T1D in vivo. It probably requires cooperation with some other substances for the maximum efficacy exhibited by oregano extracts.

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