Designing multi-modal topical drug delivery nanocarriers using nano-hybrid particles has received... more Designing multi-modal topical drug delivery nanocarriers using nano-hybrid particles has received significant interest in targeted cancer therapy. In this study, magnetic Fe(salen)-conducting copolymer nanocomposites based on our previous iron salt-free synthesis method are surface-functionalized with methotrexate and transferrin proteins. The nano-hybrids show near-infrared-/magnetic field-responsive hyperthermal activity in vitro, which can be extraordinarily useful in magnetically guidable local cancer targeting as a versatile multi-modal therapeutic drug delivery system.
Skincare is very critical in preventing aging and skin trouble, which is difficult to recover if ... more Skincare is very critical in preventing aging and skin trouble, which is difficult to recover if progressed. However, the development of effective anti-aging solutions is still on the horizon. The purpose of this study was to evaluate the functional efficacy of Ceriporia lacerata exo-pharmaceutical substance (CLEPS) in view of its use in innovative skin care cosmetics. CLEPS was found to have no cytotoxicity against normal human dermal fibroblasts and B16 melanoma cells in a wide concentration range of 0.05–7 mg/mL. It exhibited a whitening effect by inhibiting melanin synthesis comparable to that of the respective reference compound (arbutin). Notably, CLEPS not only substantially increased collagen (65.4%) and filaggrin synthesis (36%), but also significantly inhibited the activity of collagenase (93.4%), suggesting that CLEPS could prevent skin barrier damage or skin wrinkles. In addition, it showed an excellent anti-inflammatory effect and wound-healing effect. Overall, CLEPS ex...
Bruton’s tyrosine kinase (BTK) is known as a direct regulator of inflammasome, which is an intrac... more Bruton’s tyrosine kinase (BTK) is known as a direct regulator of inflammasome, which is an intracellular target to therapeutically modulate innate immunity. Although there is great interest in developing small molecule-based drugs with BTK inhibition, there are only a few drugs available in the market, due to the difficulty of drug discovery and the potential side effects. To select suitable drug compounds to inhibit BTK signaling, molecular drug screening bioassay processes of single ginsenosides integrated with in silico molecular simulation were performed. The experimental results for the ginsenoside compositions (Rb2 and Rb3) exhibited showed that they effectively suppressed the activity of BTK expression in a rational agreement with molecular docking calculations of the compounds against the BTK binding site. They implemented a possible inhibiting effect of BTK signaling through increasing their molecular affinity for targeting BTK, enabling them to be useful in treating BTK-me...
N,N'-Bis(salicylidene)ethylenediamine iron (Fe(Salen)) is an anti-cancer agent with intrinsic mag... more N,N'-Bis(salicylidene)ethylenediamine iron (Fe(Salen)) is an anti-cancer agent with intrinsic magnetic property. Here, we covalently linked Fe(Salen) to paclitaxel (PTX), a widely used anti-cancer drug, to obtain a magnetized paclitaxel conjugate (M-PTX), which exhibited magnetic characteristics for magnet-guided drug delivery and MRI visualization. M-PTX increased apoptosis and G2/M arrest of cultured human oral cancer cell lines in the same manner as PTX. Furthermore, marked contrast intensity was obtained in magnetic resonance imaging (MRI) of M-PTX. In a mouse oral cancer model, a permanent magnet placed on the body surface adjacent to the tumor resulted in distinct accumulation of M-PTX, and the anti-cancer effect was greater than that of M-PTX without the magnet. We believe that this strategy may improve future cancer chemotherapy by providing conventional anti-cancer drugs with novel functionalities such as magnet-guided drug delivery or MRI-based visualization/ quantitation of drug distribution.
Iron-salen, i.e., μ-oxo-N,N'-bis(salicylidene)ethylenediamine iron (Fe(Salen)) was a recently... more Iron-salen, i.e., μ-oxo-N,N'-bis(salicylidene)ethylenediamine iron (Fe(Salen)) was a recently identified as a new anti-cancer compound with intrinsic magnetic properties. Chelation therapy has been widely used in management of metallic poisoning, because an administration of agents that bind metals can prevent potential lethal effects of particular metal. In this study, we confirmed the therapeutic effect of deferoxamine mesylate (DFO) chelation against Fe(Salen) as part of the chelator antidote efficacy. DFO administration resulted in reduced cytotoxicity and ROS generation by Fe(Salen) in cancer cells. DFO (25 mg/kg) reduced the onset of Fe(Salen) (25 mg/kg)-induced acute liver and renal dysfunction. DFO (300 mg/kg) improves survival rate after systematic injection of a fatal dose of Fe(Salen) (200 mg/kg) in mice. DFO enables the use of higher Fe(Salen) doses to treat progressive states of cancer, and it also appears to decrease the acute side effects of Fe(Salen). This makes ...
Ultrafine Au quantum clusters (QCs) were synthesized by etching host Au nanoparticles in the pres... more Ultrafine Au quantum clusters (QCs) were synthesized by etching host Au nanoparticles in the presence of ethylenediamine (en) and exhibited both strong photoluminescence (PL) and specific anticancer activity. The cutting-edge feature of this QC compound comprises subnanometer-size rhombohedral Au8, which consists of 8 units of the anticancer motif, namely, an Au(+)(en) complex (Au(en)QCs), which contributes to photo- and physicochemical stability as well as subcellular theranostic activity in intracellular PL imaging and in situ targeting. Moreover, the Au(en)QCs can be surface-encapsulated by transferrins (Tf) to create TfAu(en)QCs as a multipurpose drug carrier owing to numerous merits, which include cancer-selective biolabeling, high loading/release efficiency, high activity against drug-resistant tumor cells, low toxicity to normal cells, and physiological stability against biothiols, e.g., glutathiones. These versatile features, which are due to intrinsic optical and anticancer...
Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in t... more Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in targeted drug delivery, contrast imaging and therapeutics. However, no simple synthetic method for magnetic DDS agents has been developed without the need to add magnetic nanoparticles. Here, we describe the one-step fabrication of 'all-in-one' magneto-assemblies using an 'inorganic-metal-salt-free' method, involving spontaneous self-assembly of the water-insoluble prodrug μ-oxo-bis(N,N 0-ethylenebis (salicylideniminato)iron) [Fe(salen)] (magnetic core) with polypyrrole (PPy)-b-polycaprolactone (PCL) smart diblock copolymers. In the system, PCL serves as a heat-responsive core scaffold, and PPy serves as an electronic core-size controller and pH-responsive shell. This core-shell nanocomposite has a high-loading capacity (~90%), and the core size is tunable by incorporating albumin or gum arabic as bio-coating agents, which also provide colloidal stability, biocompatibility and thermo-stability. Fe(salen), which has intrinsic antitumor activity, also has ubiquitous magnetic properties, which are dramatically enhanced in these molecular assemblies with magnetic coupling. Moreover, these multifunctional nanoassemblies can be delivered magnetically, can serve as magnetic resonance imaging contrast agents, can generate magneto-hyperthermal effects and can enable magnetic field-triggered release of Fe(salen) molecules under acidic conditions.
We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a m... more We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magnetic organic compound, has direct anti-tumor activity, and generates heat in an alternating magnetic field (AMF). We showed that Fe(Salen) nanoparticles are useful for combined hyperthermia-chemotherapy of tongue cancer. Here, we have examined the effect of Fe(Salen) on human glioblastoma (GB). Fe(Salen) showed in vitro anti-tumor activity towards several human GB cell lines. It inhibited cell proliferation, and its apoptosis-inducing activity was greater than that of clinically used drugs. Fe(Salen) also showed in vivo anti-tumor activity in the mouse brain. We evaluated the drug distribution and systemic side effects of intracerebrally injected Fe(Salen) nanoparticles in rats. Further, to examine whether hyperthermia, which was induced by exposing Fe(Salen) nanoparticles to AMF, enhanced the intrinsic anti-tumor effect of Fe(Salen), we used a mouse model grafted with U251 cells on t...
We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Sa... more We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Salen)) nanoparticles as a new anti-cancer agent for magnet-guided delivery with anti-cancer activity. Fe(Salen) nanoparticles should rapidly heat up in an alternating magnetic field (AMF), and we hypothesized that these single-drug nanoparticles would be effective for combined hyperthermia-chemotherapy. Conventional hyperthermic particles are usually made of iron oxide, and thus cannot exhibit anticancer activity in the absence of an AMF. We found that Fe(Salen) nanoparticles induced apoptosis in cultured cancer cells, and that AMF exposure enhanced the apoptotic effect. Therefore, we evaluated the combined threefold strategy, i.e., chemotherapy with Fe(Salen) nanoparticles, magnetically guided delivery of the nanoparticles to the tumor, and AMF-induced heating of the nanoparticles to induce local hyperthermia, in a rabbit model of tongue cancer. Intravenous administration of Fe(Salen) nanoparticles per se inhibited tumor growth before the other two modalities were applied. This inhibition was enhanced when a magnet was used to accumulate Fe(Salen) nanoparticles at the tongue. When an AMF was further applied (magnet-guided chemotherapy plus hyperthermia), the tumor masses were dramatically reduced. These results indicate that our strategy of combined hyperthermiachemotherapy using Fe(Salen) nanoparticles specifically delivered with magnetic guidance represents a powerful new approach for cancer treatment.
Inspired by the responsive characteristics of natural fibrous counterparts, triple stimuli, pH-, ... more Inspired by the responsive characteristics of natural fibrous counterparts, triple stimuli, pH-, drug-, and near-infrared (NIR) light-responsive Janus composite nanosheets (JCNs) were investigated.
The porous MgO shell inhibited the sintering/coalescence of the Pd nanoparticles, while preservin... more The porous MgO shell inhibited the sintering/coalescence of the Pd nanoparticles, while preserving their catalytic activity.
The present invention bio as synthetic and biological material labeling circle of nanocrystals ha... more The present invention bio as synthetic and biological material labeling circle of nanocrystals having a multiple electric oxidation-reduction potential of - relates to a nano-polymer, CdS, metal sulfide (MS) nanocrystals, such as PbS or ZnS is aqueous phosphoric acid solution (PBS) in a state that is combined with an antibody or DNA forms a water-soluble metal sulfide (MS) a quantum dot (QD) nano-crystal composite material, (a) to multiple antibodies are introduced into the coated magnetic beads; (B) were incubated with antigen herein; (C) The water-soluble metal sulfide (MS) a quantum dot (QD) was incubated nanocrystal complex; (D) the water-soluble MS QD nanocrystal the Square Wave Stripping negative voltage was dissolved in nitric acid solution to the complex (Square wave anodic stripping voltammetric: SWASV) method by then performing an electrochemical analysis; Is the case, QD- nanoparticles thing by electrical coding method of the target protein - (E) where a multi (Multi) of the obtained analog signal to the magnetic bead, characterized in that goes through the digital signal processing step in order to switch to the Bar Code Output implementing multiple proteins can simultaneously measure the analyte by electrical analysis at a time, by a defect in the bar code and mobile systems and enabling rapid significantly the prediction and analysis of disease agents and proceeds easily digital mobile, a small medical sensor systems by the signal generating source can. Nanocrystals, stripping sensor, a quantum dot, a mobile medical communication
Ginsenosides have offered a wide array of beneficial roles in the pharmacological regulation of h... more Ginsenosides have offered a wide array of beneficial roles in the pharmacological regulation of hepatic metabolic syndromes, including non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), and obesity. Of the numerous ginsenosides, Rg3 has been widely investigated, but there have been few studies of gypenosides (Gyp). Particularly, no study on Gyp LXXV has been reported to date. Here, to firstly explore the pharmacological effects of Gyp LXXV against NASH and the related mechanism, methionine- and choline-deficient (MCD) diet-induced NASH mice and hepatic cells (stellate cells, hepatic macrophages, and hepatocytes) were selected. Gyp LXXV exhibited markedly alleviated MCD diet-induced hepatic injury, inflammation, and fibrosis by down-regulating hepatic fibrosis markers such as α-smooth muscle actin(α-SMA), collagen1, transforming growth factors-β (TGF-β1), tumor necrosis factor-α (TNF-α), MCP-1, interleukin (IL)-1β, nuclear factor κB (NFκB), and GRP78. Re...
Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in t... more Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in targeted drug delivery, contrast imaging and therapeutics. However, no simple synthetic method for magnetic DDS agents has been developed without the need to add magnetic nanoparticles. Here, we describe the one-step fabrication of 'all-in-one' magneto-assemblies using an 'inorganic-metal-salt-free' method, involving spontaneous self-assembly of the water-insoluble prodrug μ-oxo-bis(N,N 0-ethylenebis (salicylideniminato)iron) [Fe(salen)] (magnetic core) with polypyrrole (PPy)-b-polycaprolactone (PCL) smart diblock copolymers. In the system, PCL serves as a heat-responsive core scaffold, and PPy serves as an electronic core-size controller and pH-responsive shell. This core–shell nanocomposite has a high-loading capacity (~90%), and the core size is tunable by incorporating albumin or gum arabic as bio-coating agents, which also provide colloidal stability, biocompatibility and thermo-stability. Fe(salen), which has intrinsic antitumor activity, also has ubiquitous magnetic properties, which are dramatically enhanced in these molecular assemblies with magnetic coupling. Moreover, these multifunctional nanoassemblies can be delivered magnetically, can serve as magnetic resonance imaging contrast agents, can generate magneto-hyperthermal effects and can enable magnetic field-triggered release of Fe(salen) molecules under acidic conditions.
We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magne... more We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magnetic organic compound, has direct anti-tumor activity, and generates heat in an alternating magnetic field (AMF). We showed that Fe(Salen) nanoparticles are useful for combined hyperthermia-chemotherapy of tongue cancer. Here, we have examined the effect of Fe(Salen) on human glioblastoma (GB). Fe(Salen) showed in vitro anti-tumor activity towards several human GB cell lines. It inhibited cell proliferation, and its apoptosis-inducing activity was greater than that of clinically used drugs. Fe(Salen) also showed in vivo anti-tumor activity in the mouse brain. We evaluated the drug distribution and systemic side effects of intracerebrally injected Fe(Salen) nanoparticles in rats. Further, to examine whether hyperthermia, which was induced by exposing Fe(Salen) nanoparticles to AMF, enhanced the intrinsic anti-tumor effect of Fe(Salen), we used a mouse model grafted with U251 cells on the left leg. Fe(Salen), BCNU, or normal saline was injected into the tumor in the presence or absence of AMF exposure. The combination of Fe(Salen) injection and AMF exposure showed a greater anti-tumor effect than did either Fe(Salen) or BCNU alone. Our results indicate that hyperthermia and chemotherapy with single-drug nanoparticles could be done for GB treatment. Glioblastoma (GB: WHO Grade IV) is the most common and most aggressive brain tumor in adults. It has a very poor prognosis, because of its invasiveness, its resistance to treatment, and the difficulty of total resec-tion 1–3. Temozolomide (TMZ) combined with extended focal radiotherapy is considered the standard treatment of GB, but median overall survival of GB is still less than 15 months and has changed little in recent decades 3–6. Alternative therapeutic approaches have produced some promising results. For example, wafers of 1,3-bis(2-chlorethyl)-1-nitrosourea; BCNU; carmustine placed directly in the resection cavity following operation significantly improved survival 4,7–9. The treatment with BCNU wafers and TMZ has a significant survival benefit compared to the conventional standard therapy 10–13 .
We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Sa... more We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Salen)) nanoparticles as a new anti-cancer agent for magnet-guided delivery with anti-cancer activity. Fe(Salen) nanoparticles should rapidly heat up in an alternating magnetic field (AMF), and we hypothesized that these single-drug nanoparticles would be effective for combined hyperthermia-chemotherapy. Conventional hyperthermic particles are usually made of iron oxide, and thus cannot exhibit anti-cancer activity in the absence of an AMF. We found that Fe(Salen) nanoparticles induced apoptosis in cultured cancer cells, and that AMF exposure enhanced the apoptotic effect. Therefore, we evaluated the combined threefold strategy, i.e., chemotherapy with Fe(Salen) nanoparticles, magnetically guided delivery of the nanoparticles to the tumor, and AMF-induced heating of the nanoparticles to induce local hyperthermia, in a rabbit model of tongue cancer. Intravenous administration of Fe(Salen) nanoparticles per se inhibited tumor growth before the other two modalities were applied. This inhibition was enhanced when a magnet was used to accumulate Fe(Salen) nanoparticles at the tongue. When an AMF was further applied (magnet-guided chemotherapy plus hyperthermia), the tumor masses were dramatically reduced. These results indicate that our strategy of combined hyperthermia-chemotherapy using Fe(Salen) nanoparticles specifically delivered with magnetic guidance represents a powerful new approach for cancer treatment. Head and neck cancer is the sixth most common cancer, accounting for 3% of all cancers worldwide. The incidence of new patients is increasing, particularly in developing countries 1,2. Tumors are located in the oral cavity in 48% of cases, and 90% of these are oral squamous cell carcinoma. Oral malignancy, including tongue cancer, is associated with severe morbidity and has a long-term survival of less than 50%, in spite of advances in the treatment of oral cancer by surgery, chemotherapy, and radiation. The survival ratio of patients remains very low, mainly due to lymph node metastasis 2. Surgical removal of the cancer tissues is the gold standard, but involves various complications, such as dysphagia or dysarthria. Therefore, more effective treatment for oral cancer, with fewer complications, needs to be developed.
Designing multi-modal topical drug delivery nanocarriers using nano-hybrid particles has received... more Designing multi-modal topical drug delivery nanocarriers using nano-hybrid particles has received significant interest in targeted cancer therapy. In this study, magnetic Fe(salen)-conducting copolymer nanocomposites based on our previous iron salt-free synthesis method are surface-functionalized with methotrexate and transferrin proteins. The nano-hybrids show near-infrared-/magnetic field-responsive hyperthermal activity in vitro, which can be extraordinarily useful in magnetically guidable local cancer targeting as a versatile multi-modal therapeutic drug delivery system.
Skincare is very critical in preventing aging and skin trouble, which is difficult to recover if ... more Skincare is very critical in preventing aging and skin trouble, which is difficult to recover if progressed. However, the development of effective anti-aging solutions is still on the horizon. The purpose of this study was to evaluate the functional efficacy of Ceriporia lacerata exo-pharmaceutical substance (CLEPS) in view of its use in innovative skin care cosmetics. CLEPS was found to have no cytotoxicity against normal human dermal fibroblasts and B16 melanoma cells in a wide concentration range of 0.05–7 mg/mL. It exhibited a whitening effect by inhibiting melanin synthesis comparable to that of the respective reference compound (arbutin). Notably, CLEPS not only substantially increased collagen (65.4%) and filaggrin synthesis (36%), but also significantly inhibited the activity of collagenase (93.4%), suggesting that CLEPS could prevent skin barrier damage or skin wrinkles. In addition, it showed an excellent anti-inflammatory effect and wound-healing effect. Overall, CLEPS ex...
Bruton’s tyrosine kinase (BTK) is known as a direct regulator of inflammasome, which is an intrac... more Bruton’s tyrosine kinase (BTK) is known as a direct regulator of inflammasome, which is an intracellular target to therapeutically modulate innate immunity. Although there is great interest in developing small molecule-based drugs with BTK inhibition, there are only a few drugs available in the market, due to the difficulty of drug discovery and the potential side effects. To select suitable drug compounds to inhibit BTK signaling, molecular drug screening bioassay processes of single ginsenosides integrated with in silico molecular simulation were performed. The experimental results for the ginsenoside compositions (Rb2 and Rb3) exhibited showed that they effectively suppressed the activity of BTK expression in a rational agreement with molecular docking calculations of the compounds against the BTK binding site. They implemented a possible inhibiting effect of BTK signaling through increasing their molecular affinity for targeting BTK, enabling them to be useful in treating BTK-me...
N,N'-Bis(salicylidene)ethylenediamine iron (Fe(Salen)) is an anti-cancer agent with intrinsic mag... more N,N'-Bis(salicylidene)ethylenediamine iron (Fe(Salen)) is an anti-cancer agent with intrinsic magnetic property. Here, we covalently linked Fe(Salen) to paclitaxel (PTX), a widely used anti-cancer drug, to obtain a magnetized paclitaxel conjugate (M-PTX), which exhibited magnetic characteristics for magnet-guided drug delivery and MRI visualization. M-PTX increased apoptosis and G2/M arrest of cultured human oral cancer cell lines in the same manner as PTX. Furthermore, marked contrast intensity was obtained in magnetic resonance imaging (MRI) of M-PTX. In a mouse oral cancer model, a permanent magnet placed on the body surface adjacent to the tumor resulted in distinct accumulation of M-PTX, and the anti-cancer effect was greater than that of M-PTX without the magnet. We believe that this strategy may improve future cancer chemotherapy by providing conventional anti-cancer drugs with novel functionalities such as magnet-guided drug delivery or MRI-based visualization/ quantitation of drug distribution.
Iron-salen, i.e., μ-oxo-N,N'-bis(salicylidene)ethylenediamine iron (Fe(Salen)) was a recently... more Iron-salen, i.e., μ-oxo-N,N'-bis(salicylidene)ethylenediamine iron (Fe(Salen)) was a recently identified as a new anti-cancer compound with intrinsic magnetic properties. Chelation therapy has been widely used in management of metallic poisoning, because an administration of agents that bind metals can prevent potential lethal effects of particular metal. In this study, we confirmed the therapeutic effect of deferoxamine mesylate (DFO) chelation against Fe(Salen) as part of the chelator antidote efficacy. DFO administration resulted in reduced cytotoxicity and ROS generation by Fe(Salen) in cancer cells. DFO (25 mg/kg) reduced the onset of Fe(Salen) (25 mg/kg)-induced acute liver and renal dysfunction. DFO (300 mg/kg) improves survival rate after systematic injection of a fatal dose of Fe(Salen) (200 mg/kg) in mice. DFO enables the use of higher Fe(Salen) doses to treat progressive states of cancer, and it also appears to decrease the acute side effects of Fe(Salen). This makes ...
Ultrafine Au quantum clusters (QCs) were synthesized by etching host Au nanoparticles in the pres... more Ultrafine Au quantum clusters (QCs) were synthesized by etching host Au nanoparticles in the presence of ethylenediamine (en) and exhibited both strong photoluminescence (PL) and specific anticancer activity. The cutting-edge feature of this QC compound comprises subnanometer-size rhombohedral Au8, which consists of 8 units of the anticancer motif, namely, an Au(+)(en) complex (Au(en)QCs), which contributes to photo- and physicochemical stability as well as subcellular theranostic activity in intracellular PL imaging and in situ targeting. Moreover, the Au(en)QCs can be surface-encapsulated by transferrins (Tf) to create TfAu(en)QCs as a multipurpose drug carrier owing to numerous merits, which include cancer-selective biolabeling, high loading/release efficiency, high activity against drug-resistant tumor cells, low toxicity to normal cells, and physiological stability against biothiols, e.g., glutathiones. These versatile features, which are due to intrinsic optical and anticancer...
Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in t... more Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in targeted drug delivery, contrast imaging and therapeutics. However, no simple synthetic method for magnetic DDS agents has been developed without the need to add magnetic nanoparticles. Here, we describe the one-step fabrication of 'all-in-one' magneto-assemblies using an 'inorganic-metal-salt-free' method, involving spontaneous self-assembly of the water-insoluble prodrug μ-oxo-bis(N,N 0-ethylenebis (salicylideniminato)iron) [Fe(salen)] (magnetic core) with polypyrrole (PPy)-b-polycaprolactone (PCL) smart diblock copolymers. In the system, PCL serves as a heat-responsive core scaffold, and PPy serves as an electronic core-size controller and pH-responsive shell. This core-shell nanocomposite has a high-loading capacity (~90%), and the core size is tunable by incorporating albumin or gum arabic as bio-coating agents, which also provide colloidal stability, biocompatibility and thermo-stability. Fe(salen), which has intrinsic antitumor activity, also has ubiquitous magnetic properties, which are dramatically enhanced in these molecular assemblies with magnetic coupling. Moreover, these multifunctional nanoassemblies can be delivered magnetically, can serve as magnetic resonance imaging contrast agents, can generate magneto-hyperthermal effects and can enable magnetic field-triggered release of Fe(salen) molecules under acidic conditions.
We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a m... more We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magnetic organic compound, has direct anti-tumor activity, and generates heat in an alternating magnetic field (AMF). We showed that Fe(Salen) nanoparticles are useful for combined hyperthermia-chemotherapy of tongue cancer. Here, we have examined the effect of Fe(Salen) on human glioblastoma (GB). Fe(Salen) showed in vitro anti-tumor activity towards several human GB cell lines. It inhibited cell proliferation, and its apoptosis-inducing activity was greater than that of clinically used drugs. Fe(Salen) also showed in vivo anti-tumor activity in the mouse brain. We evaluated the drug distribution and systemic side effects of intracerebrally injected Fe(Salen) nanoparticles in rats. Further, to examine whether hyperthermia, which was induced by exposing Fe(Salen) nanoparticles to AMF, enhanced the intrinsic anti-tumor effect of Fe(Salen), we used a mouse model grafted with U251 cells on t...
We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Sa... more We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Salen)) nanoparticles as a new anti-cancer agent for magnet-guided delivery with anti-cancer activity. Fe(Salen) nanoparticles should rapidly heat up in an alternating magnetic field (AMF), and we hypothesized that these single-drug nanoparticles would be effective for combined hyperthermia-chemotherapy. Conventional hyperthermic particles are usually made of iron oxide, and thus cannot exhibit anticancer activity in the absence of an AMF. We found that Fe(Salen) nanoparticles induced apoptosis in cultured cancer cells, and that AMF exposure enhanced the apoptotic effect. Therefore, we evaluated the combined threefold strategy, i.e., chemotherapy with Fe(Salen) nanoparticles, magnetically guided delivery of the nanoparticles to the tumor, and AMF-induced heating of the nanoparticles to induce local hyperthermia, in a rabbit model of tongue cancer. Intravenous administration of Fe(Salen) nanoparticles per se inhibited tumor growth before the other two modalities were applied. This inhibition was enhanced when a magnet was used to accumulate Fe(Salen) nanoparticles at the tongue. When an AMF was further applied (magnet-guided chemotherapy plus hyperthermia), the tumor masses were dramatically reduced. These results indicate that our strategy of combined hyperthermiachemotherapy using Fe(Salen) nanoparticles specifically delivered with magnetic guidance represents a powerful new approach for cancer treatment.
Inspired by the responsive characteristics of natural fibrous counterparts, triple stimuli, pH-, ... more Inspired by the responsive characteristics of natural fibrous counterparts, triple stimuli, pH-, drug-, and near-infrared (NIR) light-responsive Janus composite nanosheets (JCNs) were investigated.
The porous MgO shell inhibited the sintering/coalescence of the Pd nanoparticles, while preservin... more The porous MgO shell inhibited the sintering/coalescence of the Pd nanoparticles, while preserving their catalytic activity.
The present invention bio as synthetic and biological material labeling circle of nanocrystals ha... more The present invention bio as synthetic and biological material labeling circle of nanocrystals having a multiple electric oxidation-reduction potential of - relates to a nano-polymer, CdS, metal sulfide (MS) nanocrystals, such as PbS or ZnS is aqueous phosphoric acid solution (PBS) in a state that is combined with an antibody or DNA forms a water-soluble metal sulfide (MS) a quantum dot (QD) nano-crystal composite material, (a) to multiple antibodies are introduced into the coated magnetic beads; (B) were incubated with antigen herein; (C) The water-soluble metal sulfide (MS) a quantum dot (QD) was incubated nanocrystal complex; (D) the water-soluble MS QD nanocrystal the Square Wave Stripping negative voltage was dissolved in nitric acid solution to the complex (Square wave anodic stripping voltammetric: SWASV) method by then performing an electrochemical analysis; Is the case, QD- nanoparticles thing by electrical coding method of the target protein - (E) where a multi (Multi) of the obtained analog signal to the magnetic bead, characterized in that goes through the digital signal processing step in order to switch to the Bar Code Output implementing multiple proteins can simultaneously measure the analyte by electrical analysis at a time, by a defect in the bar code and mobile systems and enabling rapid significantly the prediction and analysis of disease agents and proceeds easily digital mobile, a small medical sensor systems by the signal generating source can. Nanocrystals, stripping sensor, a quantum dot, a mobile medical communication
Ginsenosides have offered a wide array of beneficial roles in the pharmacological regulation of h... more Ginsenosides have offered a wide array of beneficial roles in the pharmacological regulation of hepatic metabolic syndromes, including non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), and obesity. Of the numerous ginsenosides, Rg3 has been widely investigated, but there have been few studies of gypenosides (Gyp). Particularly, no study on Gyp LXXV has been reported to date. Here, to firstly explore the pharmacological effects of Gyp LXXV against NASH and the related mechanism, methionine- and choline-deficient (MCD) diet-induced NASH mice and hepatic cells (stellate cells, hepatic macrophages, and hepatocytes) were selected. Gyp LXXV exhibited markedly alleviated MCD diet-induced hepatic injury, inflammation, and fibrosis by down-regulating hepatic fibrosis markers such as α-smooth muscle actin(α-SMA), collagen1, transforming growth factors-β (TGF-β1), tumor necrosis factor-α (TNF-α), MCP-1, interleukin (IL)-1β, nuclear factor κB (NFκB), and GRP78. Re...
Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in t... more Nanoparticulate agents for magnetic drug delivery systems (DDSs) have extensive applications in targeted drug delivery, contrast imaging and therapeutics. However, no simple synthetic method for magnetic DDS agents has been developed without the need to add magnetic nanoparticles. Here, we describe the one-step fabrication of 'all-in-one' magneto-assemblies using an 'inorganic-metal-salt-free' method, involving spontaneous self-assembly of the water-insoluble prodrug μ-oxo-bis(N,N 0-ethylenebis (salicylideniminato)iron) [Fe(salen)] (magnetic core) with polypyrrole (PPy)-b-polycaprolactone (PCL) smart diblock copolymers. In the system, PCL serves as a heat-responsive core scaffold, and PPy serves as an electronic core-size controller and pH-responsive shell. This core–shell nanocomposite has a high-loading capacity (~90%), and the core size is tunable by incorporating albumin or gum arabic as bio-coating agents, which also provide colloidal stability, biocompatibility and thermo-stability. Fe(salen), which has intrinsic antitumor activity, also has ubiquitous magnetic properties, which are dramatically enhanced in these molecular assemblies with magnetic coupling. Moreover, these multifunctional nanoassemblies can be delivered magnetically, can serve as magnetic resonance imaging contrast agents, can generate magneto-hyperthermal effects and can enable magnetic field-triggered release of Fe(salen) molecules under acidic conditions.
We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magne... more We previously reported that μ-oxo N,N'-bis(salicylidene)ethylenediamine iron [Fe(Salen)], a magnetic organic compound, has direct anti-tumor activity, and generates heat in an alternating magnetic field (AMF). We showed that Fe(Salen) nanoparticles are useful for combined hyperthermia-chemotherapy of tongue cancer. Here, we have examined the effect of Fe(Salen) on human glioblastoma (GB). Fe(Salen) showed in vitro anti-tumor activity towards several human GB cell lines. It inhibited cell proliferation, and its apoptosis-inducing activity was greater than that of clinically used drugs. Fe(Salen) also showed in vivo anti-tumor activity in the mouse brain. We evaluated the drug distribution and systemic side effects of intracerebrally injected Fe(Salen) nanoparticles in rats. Further, to examine whether hyperthermia, which was induced by exposing Fe(Salen) nanoparticles to AMF, enhanced the intrinsic anti-tumor effect of Fe(Salen), we used a mouse model grafted with U251 cells on the left leg. Fe(Salen), BCNU, or normal saline was injected into the tumor in the presence or absence of AMF exposure. The combination of Fe(Salen) injection and AMF exposure showed a greater anti-tumor effect than did either Fe(Salen) or BCNU alone. Our results indicate that hyperthermia and chemotherapy with single-drug nanoparticles could be done for GB treatment. Glioblastoma (GB: WHO Grade IV) is the most common and most aggressive brain tumor in adults. It has a very poor prognosis, because of its invasiveness, its resistance to treatment, and the difficulty of total resec-tion 1–3. Temozolomide (TMZ) combined with extended focal radiotherapy is considered the standard treatment of GB, but median overall survival of GB is still less than 15 months and has changed little in recent decades 3–6. Alternative therapeutic approaches have produced some promising results. For example, wafers of 1,3-bis(2-chlorethyl)-1-nitrosourea; BCNU; carmustine placed directly in the resection cavity following operation significantly improved survival 4,7–9. The treatment with BCNU wafers and TMZ has a significant survival benefit compared to the conventional standard therapy 10–13 .
We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Sa... more We previously investigated the utility of μ-oxo N,N′-bis(salicylidene)ethylenediamine iron (Fe(Salen)) nanoparticles as a new anti-cancer agent for magnet-guided delivery with anti-cancer activity. Fe(Salen) nanoparticles should rapidly heat up in an alternating magnetic field (AMF), and we hypothesized that these single-drug nanoparticles would be effective for combined hyperthermia-chemotherapy. Conventional hyperthermic particles are usually made of iron oxide, and thus cannot exhibit anti-cancer activity in the absence of an AMF. We found that Fe(Salen) nanoparticles induced apoptosis in cultured cancer cells, and that AMF exposure enhanced the apoptotic effect. Therefore, we evaluated the combined threefold strategy, i.e., chemotherapy with Fe(Salen) nanoparticles, magnetically guided delivery of the nanoparticles to the tumor, and AMF-induced heating of the nanoparticles to induce local hyperthermia, in a rabbit model of tongue cancer. Intravenous administration of Fe(Salen) nanoparticles per se inhibited tumor growth before the other two modalities were applied. This inhibition was enhanced when a magnet was used to accumulate Fe(Salen) nanoparticles at the tongue. When an AMF was further applied (magnet-guided chemotherapy plus hyperthermia), the tumor masses were dramatically reduced. These results indicate that our strategy of combined hyperthermia-chemotherapy using Fe(Salen) nanoparticles specifically delivered with magnetic guidance represents a powerful new approach for cancer treatment. Head and neck cancer is the sixth most common cancer, accounting for 3% of all cancers worldwide. The incidence of new patients is increasing, particularly in developing countries 1,2. Tumors are located in the oral cavity in 48% of cases, and 90% of these are oral squamous cell carcinoma. Oral malignancy, including tongue cancer, is associated with severe morbidity and has a long-term survival of less than 50%, in spite of advances in the treatment of oral cancer by surgery, chemotherapy, and radiation. The survival ratio of patients remains very low, mainly due to lymph node metastasis 2. Surgical removal of the cancer tissues is the gold standard, but involves various complications, such as dysphagia or dysarthria. Therefore, more effective treatment for oral cancer, with fewer complications, needs to be developed.
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Papers by Jeong-Hwan Kim