Correlation between Chemical Composition of Curcuma domestica

The antioxidant activity of the curcuminoids of Curcuma domestica L. and C. xanthorrhiza Roxb. and eight compounds which are prevalent constituents of their rhizome oils were investigated in an effort to correlate human low-density lipoprotein (LDL) antioxidant activity with the effect of the herbs and their components. The antioxidant activity was examined using thiobarbituric acid reactive substances (TBARSs) assay with human LDL as the oxidation substrate. The methanol extracts and rhizome oils of C. xanthorrhiza and C. domestica showed strong inhibitory activity on copper-mediated oxidation of LDL. Curcumin, demethoxycurcumin, and bisdemethoxycurcumin, isolated from the methanol extracts of both plants, exhibited stronger activity than probucol (IC50 value 0.57 μmol/L) as reference, with IC50 values ranging from 0.15 to 0.33 μmol/L. Xanthorrhizol, the most abundant component (31.9%) of the oil of C. xanthorrhiza, showed relatively strong activity with an IC50 value of 1.93 μmol/L. The major components of C. domestica, ar-turmerone (45.8%) and zerumbone (3.5%), exhibited IC50 values of 10.18 and 24.90 μmol/L, respectively. The high levels of curcuminoids in the methanol extracts and xanthorrhizol, ar-turmerone and zerumbone in the oils, and in combination with the minor components were responsible for the high LDL antioxidant activity of the herbs

Green tea (Camellia sinensis) extract reduces peptic ulcer induced by Helicobacter pylori in sprague dawley rats

The study was conducted to evaluate the anti-peptic ulcer activity of ethanol extract of Camellia sinensis (green tea) induced by Helicobacter pylori in Sprague Dawley rats. The standard regimen of anti-peptic ulcer agents, clarithromycin 30 mg/kg, amoxicillin 30 mg/kg and esomeprazole 3 mg/kg used as the positive control. The rats divided into 6 groups (n = 6), normal control, vehicle control (2% of tragacanth suspension), positive control for preventive and treatment groups, preventive and treatment groups were given 50 mg/kg orally of green tea extract for 14 days before and after inoculation (as prevention and treatment, respectively) with 5×108 CFU/mL H. pylori suspension orally twice daily for 7 days. Anti-peptic ulcer activity was evaluated based on the pH of gastric juice, ulcer score and body weight of rats. The results demonstrated that the use of green tea for prevention or treatment showed a significant difference (p<0.001) in reducing the pH of gastric juice 3.88 ± 0.09 and 5.74 ± 0.08, respectively, compared to vehicle control 5.85 ± 0.12. Meanwhile, vehicle control rats had high significantly reduced body weight when compared with all groups treated. The preventive and the treatment groups showed significantly reduce in ulcer score to 0.50 ± 0.18 (p<0.01) and 0.83 ± 0.10 (p<0.05), respectively, compared to vehicle control 1.50 ± 0.22. Meanwhile, it was comparable to the positive control. In conclusion, H. pylori suspension 5×108 CFU/mL given orally twice daily for seven days able to induce ulcer in Sprague Dawley rats, and the green tea extract 50 mg/kg was comparable to the standard regimen as anti-peptic ulcer agent

Synthesis and evaluation of methacrylated poly(2-ethyl-2-oxazoline) as a mucoadhesive polymer for nasal drug delivery

Methacrylated poly(2-ethyl-2-oxazoline) (PEOZ) was synthesized by partial hydrolysis of 500 kDa PEOZ, and the resulting poly[(2-ethyl-2-oxazoline)-co-ethylenimine] P(EOZ-co-EI) was subsequently reacted with methacrylic anhydride. The successful synthesis of methacrylated PEOZ (MAPEOZ) was confirmed by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy, and differential scanning calorimetry. The degrees of hydrolysis and methacrylation were determined by 1H NMR spectra. MAPEOZ exhibited temperature-responsive properties, which were dependent on the degree of methacrylation. On that basis, three soluble MAPEOZ derivatives with different degrees of methacrylation were selected and investigated in cell toxicity studies, showing no significant cytotoxicity against the HEK293 cell line. A slug mucosal irritation assay showed that PEOZ and MAPEOZ do not cause mucosal irritation. The presence of methacryloyl groups and residual amines had a remarkable synergistic effect on the mucoadhesive properties of these polymers. These poly(2-ethyl-2-oxazoline) derivatives have excellent potential as mucoadhesive materials for developing formulations for drug delivery via mucosal routes of administration

Inhibitory effects of Gynura procumbens ethanolic extract on nitric oxide production and inducible nitric oxide synthase (iNOS) protein expression in macrophages

Nitric oxide (NO) overproduction by inducible nitric oxide synthase (iNOS) may be associated with acute and chronic inflammations. Macrophages as important cells in the innate immune system are able to be stimulated and can lead to iNOS activation and excessive NO production. Gynura procumbens is a medicinal plant traditionally used in treating various ailments including inflammation but the mechanism of anti-inflammatory activity of this plant is still elusive. This study was carried out to investigate the anti-inflammatory therapeutic effects of Gynura procumbens ethanolic extract on NO production and iNOS protein expression in RAW 264.7 macrophages stimulated with lipopolysaccharide (LPS). Cell viability of RAW 264.7 macrophages treated with Gynura procumbens ethanolic extract was determined by MTT assay. NO production was determined by Griess assay following Gynura procumbens ethanolic extract treatment alone or in combination with LPS stimulation. Protein expression of iNOS was determined by western blot. RAW 264.7 macrophages viability of more than 90% was observed after 24 h treatment with Gynura procumbens ethanolic extract concentration range of 3.9 μg/mL to 500 μg/mL. Significant inhibition of NO production level has been identified in LPS-stimulated RAW 264.7 cells pre-treated with 250 μg/mL Gynura procumbens ethanolic extract (p<0.05) while all selected concentrations of Gynura procumbens ethanolic extract showed no significant alteration of NO production in the absence of LPS stimulation. Pre-treatment of 250 μg/mL Gynura procumbens ethanolic extract also demonstrated significant suppression of iNOS protein expression in LPS-stimulated RAW 264.7 cells (p<0.05). In conclusion, this study demonstrates that Gynura procumbens ethanolic extract exhibits anti-inflammatory potential through inhibition of NO production and iNOS protein expression in LPS-stimulated macrophages, suggesting that this plant could be further researched for its beneficial use in inflammatory disorders

Chemically modified hydroxyethyl cellulose as a new excipient for transmucosal delivery

In the pharmaceutical industry, excipients such as cellulose and its derivatives are often used in the formulation of dosage forms as binders for tablets, viscosity enhancers, gelling agents, coating agents, etc. In addition to its basic functionality, this polymer can be modified to provide additional properties that optimise its performance in a particular application. An example of properties that are of great interest is mucoadhesion. The mucoadhesive properties allow greater contact between the formulation and the oral mucosa for a slow release of the active ingredient. Among the cellulose derivatives, hydroxyethyl cellulose (HEC) has weak mucoadhesive properties. However, it can be improved by modification with unsaturated groups such as methacryloyl, maleimide, acryloyl and divinyl sulfone. The newly modified HEC can interact with mucin glycoproteins by forming covalent bonds between the electronegative unsaturated end groups of the modified polymer and the less electronegative parts of the mucin glycoprotein (cysteine) via the Michael addition reaction. In this thesis, we have synthesised HEC with methacryloyl, maleimide, acryloyl and divinyl sulfone groups. The successful synthesis of the new polymers was validated using 1H NMR and FTIR. It was further quantified by either 1H NMR, HPLC and/or elemental analysis. These modified polymers were developed into various blank dosage forms (wafers, films, spray-coated tablets and microparticles) to determine their mucoadhesiveness using a texture analyser. A safety study was performed using planarian acute toxicity assays and planarian fluorescent toxicity assays. The safety study was further supported by in vitro toxicity assay using Caco-2 cells. Our findings suggest that synthesis process of all HEC derivatives was successful and regardless of molar ratio, the modified HEC with methacryloyl, maleimide, acryloyl and sulfone groups has improved the mucoadhesiveness of the native HEC. Additionally, the newly modified excipients are water soluble, versatile in dosage form development and easy to synthesis (one�pot synthesis method) under normal environmental conditions. These results support the idea that non-ionic HEC modified with unsaturated groups such as methacryloyl, maleimide, acryloyl and sulfone groups significantly improves the mucoadhesive properties of native HEC. Therefore, modified HEC with methacryloyl, maleimide, acryloyl and sulfone groups has great potential as a new multifunctional excipient for transmucosal drug delivery, as it has the advantage of being mucoadhesive yet retaining the non-ionic nature of HEC derivatives. This may promote greater compatibility with charged drug molecules in dosage form formulations

Correlation between chemical composition of Curcuma domestica and Curcuma xanthorrhiza and their antioxidant effect on human lowdensity lipoprotein oxidation,” Evidence-Based Complementary and Alternative Medicine, vol

The antioxidant activity of the curcuminoids of Curcuma domestica L. and C. xanthorrhiza Roxb. and eight compounds which are prevalent constituents of their rhizome oils were investigated in an effort to correlate human low-density lipoprotein (LDL) antioxidant activity with the effect of the herbs and their components. The antioxidant activity was examined using thiobarbituric acid reactive substances (TBARSs) assay with human LDL as the oxidation substrate. The methanol extracts and rhizome oils of C. xanthorrhiza and C. domestica showed strong inhibitory activity on copper-mediated oxidation of LDL. Curcumin, demethoxycurcumin, and bisdemethoxycurcumin, isolated from the methanol extracts of both plants, exhibited stronger activity than probucol (IC 50 value 0.57 μmol/L) as reference, with IC 50 values ranging from 0.15 to 0.33 μmol/L. Xanthorrhizol, the most abundant component (31.9%) of the oil of C. xanthorrhiza, showed relatively strong activity with an IC 50 value of 1.93 μmol/L. The major components of C. domestica, ar-turmerone (45.8%) and zerumbone (3.5%), exhibited IC 50 values of 10.18 and 24.90 μmol/L, respectively. The high levels of curcuminoids in the methanol extracts and xanthorrhizol, ar-turmerone and zerumbone in the oils, and in combination with the minor components were responsible for the high LDL antioxidant activity of the herbs

Antiperspirant and Antibacterial Activities of <i>Curcuma xanthorrhiza</i> Extract as a Potential Alternative Treatment for Hyperhidrosis

Hyperhidrosis is a condition characterized by excessive sweating that affects at least 5% of the world’s population. It is normally associated with unpleasant body odour which requires continuous maintenance throughout life. Antiperspirants and deodorants are the first-line treatments for hyperhidrosis. However, association of this class of product with the risk of other diseases has increased the search for an effective antiperspirant from natural sources. This study aimed to investigate the antibacterial and antiperspirant activities of Curcuma xanthorrhiza Roxb. Using an in vitro microbial assay against specific bacteria responsible for body odour and rat foot pad analysis. Quality control of the fractionated extract was conducted using reversed-phase HPLC based on two active markers: xanthorrhiza and curcumin. Toxicity tests were conducted based on the OECD guidelines (50–2000 mg/kg). Inhibition zone, MIC, and MBC values of the hexane fraction of C. xanthorrhiza showed equivalent antibacterial activity to positive control (p > 0.05). No swelling, redness, or rashes were observed at the injection area throughout the study. Treatment with 40, 80, and 160 mg/kg of the extract significantly decreased the sweat excretion up to 79.34% (p C. xanthorrhiza is able to reduce sweat excretion in a rat model and inhibit the growth of bacteria causing body odour

Synthesis of Methacryloylated Hydroxyethylcellulose and Development of Mucoadhesive Wafers for Buccal Drug Delivery

Non-ionic hydroxyethylcellulose (HEC) has limited mucoadhesive properties for application in transmucosal drug delivery. In this study, HEC was chemically modified by reaction with glycidyl methacrylate. This allowed introducing the methacryloyl groups to HEC structure to make it capable of forming covalent bonds with the sulfhydryl groups present in the mucin glycoprotein to achieve enhanced mucoadhesive properties. The results showed a successful modification of HEC as confirmed by 1H NMR and FTIR spectroscopies. The quantification of methacryloyl moieties was conducted using HPLC. The toxicity studies using in vivo planaria acute toxicity assay, in vivo planaria fluorescent test, and in vitro MTT assay with Caco-2 cell line confirmed that the chemical modification of HEC does not result in any toxicological effects. Mucoadhesive wafers were developed based on parent and modified HEC as a model dosage form for buccal delivery. The mucoadhesive properties of modified HEC assessed using a tensile test were found to be significantly better compared to unmodified HEC

Hydroxyethyl cellulose functionalised with maleimide groups as a new excipient with enhanced mucoadhesive properties

Hydroxyethylcellulose (HEC) is a non-ionic water-soluble polymer with poor mucoadhesive properties. The mucoadhesive properties of hydroxyethylcellulose can be improved by modifying it through conjugation with molecules containing maleimide groups. Maleimide groups interact with the thiol groups present in cysteine domains in the mucin via Michael addition reaction under physiological conditions to form a strong mucoadhesive bond. This will prolong the residence time of a dosage form containing this modified polymer and drug on mucosal surfaces. In this study HEC was modified by reaction with 4-bromophenyl maleimide in varying molar ratios and the successful synthesis was confirmed using 1H NMR and FTIR spectroscopies. The safety of the newly synthesised polymer derivatives was assessed with in vivo planaria assays and in vitro MTT assay utilising Caco-2 cell line. The synthesized maleimide-functionalised HEC solutions were sprayed onto blank tablets to develop a model dosage form. The physical properties and mucoadhesive behavior of these tablets were evaluated using a tensile test with sheep buccal mucosa. The maleimide-functionalised HEC exhibited superior mucoadhesive properties compared to unmodified HEC