Research on chemical constituents, anti-bacterial and anti-cancer effects of components isolated from Zingiber officinale Roscoe from Vietnam

Ginger, a commonly used spice and medicinal herb, is an abundant source of bioactive compounds. However, the utilization of ginger in the pharmaceutical industry is still moderate and not commensurate with the potential of the Vietnamese horticulture industry, mainly due to a lack of information about the quality of input materials. In this study, we compared the volatile compounds of gingers collected from 13 provinces of Vietnam using GC/MS and GC-FID analysis to provide a basis for selecting and standardizing input materials. Furthermore, ginger essential oil from Ben Tre province of Vietnam exhibited significant antibacterial activity particularly in inhibiting Gram-positive bacteria, including S. aureus and S. epidermidis, with inhibition zones of 30.00 ± 1.41 and 24.67 ± 3.30 mm, respectively. However, no significant inhibition was observed against Gram-negative bacteria P. aeruginosa and E. coli. We also isolated 5 non-volatile compounds from ginger extract, namely 6-shogaol (1), quercetin (2), rutin (3), beta-sitosterol (4) and beta-sitosterol-3-O-beta-D-glucopyranoside (5). Among them, compounds 1–3 displayed cytotoxicity against Hep3B, SK-LU-1, MCF-7, SK-LU-1, SW480 and HepG2 tumour cell lines, with an IC50 values ranging between 62.7 ± 2.1 and 97.6 ± 1.1 µM, using Ellipticine as a positive control. Compounds 4 and 5 showed cytotoxicity against Hep3B and HepG2 tumor cells, with the IC50 values ranging between 21.5 ± 5.1 and 46.9 ± 3.7 µM but did not exhibit any significant cytotoxicity against SW480 and SK-LU-1 cells. Compound 4 also demonstrated middling cytotoxicity against the MCF7 cell line, with an IC50 value of 43.6 ± 5.1 µM. These findings suggest further applications of Vietnamese ginger for the treatment of infectious and cancer-related diseases

Redox and pH Responsive Poly (Amidoamine) Dendrimer-Heparin Conjugates via Disulfide Linkages for Letrozole Delivery

Heparin (Hep) conjugated to poly (amidoamine) dendrimer G3.5 (P) via redox-sensitive disulfide bond (P-SS-Hep) was studied. The redox and pH dual-responsive nanocarriers were prepared by a simple method that minimized many complex steps as previous studies. The functional characterization of G3.5 coated Hep was investigated by the proton nuclear magnetic resonance spectroscopy. The size and formation were characterized by the dynamic light scattering, zeta potential, and transmission electron microscopy. P-SS-Hep was spherical in shape with average diameter about 11 nm loaded with more than 20% letrozole. This drug carrier could not only eliminate toxicity to cells and improve the drugs solubility but also increase biocompatibility of the system under reductive environment of glutathione. In particular, P-SS-Hep could enhance the effectiveness of cancer therapy after removing Hep from the surface. These results demonstrated that the P-SS-Hep conjugates could be a promising candidate as redox and pH responsive nanocarriers for cancer chemotherapy

Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment

Polyamidoamine dendrimer (PAMAM) with its unique characteristics emerges as a potential drug delivery system which can prolong releasing time, reduce the side effects but still retaining treatment efficiency. In this study, methoxy polyethylene glycol modified PAMAM generation 3.0 (G3.0@mPEG) is prepared and characterized via 1H-NMR, FT-IR, and TEM. Subsequently, two antiretroviral agents (ARV) including lamivudine (3TC) and zidovudine (AZT) are individually encapsulated into G3.0@mPEG. The drug-loading efficiency, drug release profile, cytotoxicity and anti-HIV activity are then evaluated. The results illustrate that G3.0@mPEG particles are spherical with a size of 34.5 ± 0.2 nm and a drug loading content of about 9%. Both G3.0@mPEG and [email protected]@mPEG show no cytotoxicity on BJ cells, and G3.0@mPEG loading 3TC and AZT performs sustained drug release behavior which is best fitted with the Korsmeyer–Peppas model. Finally, the anti-HIV activity of ARV via Enzymatic Assay of Pepsin is retained after being loaded into the G3.0@mPEG, in which about 36% of pepsin activity was inhibited by AZT at the concentration of 0.226 mM. Overall, PAMAM G3.0@mPEG is a promising nanocarrier system for loading ARV in HIV treatment and prevention

Silver Core-Shell Nanoclusters Exhibiting Strong Growth Inhibition of Plant-Pathogenic Fungi

We introduced a novel method to prepare silver core-shell nanoclusters (NCs) in which 3,4-dihydroxyphenyl acetic-conjugated oligochitosan (DHPAC) reduced silver salt and subsequently protected the produced nanosilver via mussel adhesion mechanism. Results indicated that the degree of conjugation was 14 dihydroxyphenyl acetamide moieties over 100 glucosamine units of oligochitosan. We used chitosan-catechol derivative to prepare the well-defined silver core-shell NCs and applied UV-visible spectroscopy, transmission electron microscopy (TEM), and X-ray diffraction (XRD) techniques to characterize the NCs. The core-shell NCs exhibited strong growth inhibition of plant-pathogenic fungi such as Phytophthora capsici, Phytophthora nicotianae, and Phytophthora colocasiae. These positive results may offer great potential to produce silver core-DHPAC shell NCs for several biomedical applications

Nanoencapsulation Enhances Anticoagulant Activity of Adenosine and Dipeptide IleTrp

It is well-known that drugs administered into an organism intravenously or through the gastrointestinal tract are degraded by enzymes of the body, reducing their therapeutic effect. One of the ways to decrease this undesirable process is through the inclusion of drugs in nanomaterials. Earlier strong anticoagulant activity was demonstrated for dipeptide IleTrp (IW) and adenosine (Ado). In this work, the effect of inclusion in nanomaterials on the biological activity of IW and Ado was studied. For this purpose, Ado and IW were incorporated into thermosensitive nanogel composed of pluronic P123-grafted heparin. The prepared nanocarrier was characterized by transmission electron microscopy, dynamic light scattering, and ζ-potential. Biological activity was determined by measuring the bleeding time from mouse tail in vivo and the time of clot formation in vitro. It was found that encapsulation of Ado and IW into nanomaterial significantly increased their effects, resulting in an increase in the bleeding time from mouse tail and clot formation time. Thus, inclusion of low molecular weight anticoagulants Ado and IW into nanomaterials may be considered a way to increase their biological activity

Self-assembled poly(ethylene glycol) methyl ether-grafted gelatin nanogels for efficient delivery of curcumin in cancer treatment

Curcumin (CUR) is a natural active ingredient that attracted much attention for its chemotherapeutic activity against tumors without causing toxicity in healthy cells. However, it has certain limitations for being used in chemotherapy such as low aqueous solubility and hydrolytic instability in the physiological environment. In this study, self‐assembled poly(ethylene glycol) methyl ether‐grafted gelatin (Gel‐mPEG) nanogels were fabricated as delivery systems to improve the applicability of CUR in cancer treatment. CUR‐loaded Gel‐mPEG nanogels exhibited desired size range, relatively colloidal stability, and provided enhanced CUR stability in aqueous solutions. Especially, they showed significant high CUR loading capacity and better anticancer activity than free CUR as compared to previously reported CUR‐loaded nanogels according to the best of our knowledge. Moreover, the in vitro release of CUR from the nanogels was controlled and prolonged up to 96 h. These results demonstrated that Gel‐mPEG nanogels are the promising modality for the efficient delivery of CUR in cancer treatment

Modified Carboxyl-Terminated PAMAM Dendrimers as Great Cytocompatible Nano-Based Drug Delivery System

Polyamidoamine (PAMAM) dendrimers are extensively researched as potential drug delivery system thanks to their desirable features such as controlled and stable structures, and ease of functionalization onto their surface active groups. However, there have been concerns about the toxicity of full generation dendrimers and risks of premature clearance from circulation, along with other physical drawbacks presented in previous formulations, including large particle sizes and low drug loading efficiency. In our study, carboxyl-terminated PAMAM dendrimer G3.5 was grafted with poly (ethylene glycol) methyl ether (mPEG) to be employed as a nano-based drug delivery system with great cytocompatibility for the delivery of carboplatin (CPT), a widely prescribed anticancer drug with strong side effects so that the drug will be effectively entrapped and not exhibit uncontrolled outflow from the open structure of unmodified PAMAM G3.5. The particles formed were spherical in shape and had the optimal size range (around 36 nm) that accommodates high drug entrapment efficiency. Surface charge was also determined to be almost neutral and the system was cytocompatible. In vitro release patterns over 24 h showed a prolonged CPT release compared to free drug, which correlated to the cytotoxicity assay on malignant cell lines showing the lack of anticancer effect of CPT/mPEG-G3.5 compared with CPT