Magnolol and honokiol, main active compounds from the bark of Magnolia officinalis, have been found to have various pharmacological actions, including anti-oxidative, anti-inflammatory, anti-tumor, and anti-microbial properties, without appreciable toxicity. Recently, the anti-tumor activity of magnolol and honokiol has been extensively investigated. Magnolol and honokiol were found to possess anti-tumor activity by targeting the apoptosis pathways, which have been considered as targets for cancer therapies. This review will focus on the mechanisms by which magnolol and honokiol act on apoptosis pathways in cancer that have been characterized thus far, including the death receptormediated pathway, mitochondria-mediated pathway, caspase-mediated common pathway, and regulation of apoptosis-related proteins. These breakthrough findings may have important implications for targeted cancer therapy and modern applications of traditional Chinese medicine.
Near-infrared (NIR) absorbing dyes represent an intriguing avenue for extracting biological information from living subjects since they can be monitored with noninvasive optical imaging techniques. We designed and synthesized an imaging agent which contains a NIR fluorochrome (IR780) and peptidyl fluoromethyl ketone (FMK) for caspase-9 imaging of cells undergoing apoptosis. The IR780-FMK fluorescent probe had a Strokes shift of 79 nm and quantum yield 0.75. Prostate cancer DU145 cells undergoing apoptosis were successfully imaged using as little as 0.1 μM of IR780-FMK.
In the present study, a series of N(3)-substituted 2,4-imidazolidinediones and oxazolidinediones derivatives (1-16) were synthesized and tested for anticonvulsant activity using the maximal electroshock seizure test. Affinity towards receptor (5-HT1A/2A) was also studied. Their neurotoxicity was determined using the rotarod test. Structures of compounds were confirmed by spectroscopic methods. Compounds 1, 2, 5, 7, 9, and 10 exhibited significant anticonvulsant activity as compared to the standard drug phenytoin. Affinity toward receptor (5-HT1A/2A) was studied in vivo for compounds 1, 2, 5, 7, 9, and 10. Rectal body temperature, lower lip retractions and head twitch responses in Wistar rats/albino mice were determined for this purpose. The tested compounds showed affinity for 5-HT1A and 5-HT2A receptors (agonists/antagonists and presynaptic/postsynaptic). Replacement of piperazine by aniline derivatives provides good outcomes in terms of affinity for 5-HT1A/2A.
Essential oils of young and mature rhizomes, air-dried and steamed rhizomes, and seed rhizomes of Zingiber officinale Roscoe (ginger) were prepared, and their inhibition of filamentation by Candida albicans was examined. Ginger essential oils, and particularly those from seed and air-dried rhizomes, had potent inhibitory activity compared to ginger oleoresins obtained by ethanol and hypercritical carbon dioxide extraction and essential oils of 5 other plants in the family Zingiberaceae. Of the constituents, -shogaol was most active against filament formation and growth of C. albicans, followed by citral and -gingerol. Ginger oleoresin, and especially that obtained by ethanol extraction, with a high -gingerol content exhibited potent scavenging activity against 1,1-diphenyl-2-picrylhydrazyl radicals in comparison to essential oils of ginger and other Zingiberaceae plants.
The aim of this study is to develop a microemulsion product from a plant essential oil having the highest anti-tyrosinase activity. The in vitro anti-tyrosinase activity of six essential oils extracted from six edible plants was compared. The oil of Cymbopogon citratus demonstrated the highest activity which was significantly nontoxic to normal human cells. The GC-MS data indicated that geranial and neral are the major compounds in the oil. The phase diagram composed of C. citratus oil, water, and surfactant mixture was conducted by a titration method. Ethyl alcohol was found to be the most suitable cosurfactant for the C. citratus oil microemulsion. The results revealed that the amount of oil and water played an important role in microemulsion conductivity and type. The most desirable o/w type of C. citratus oil microemulsion was found to be composed of 20% oil, 30% water, and 50% surfactant mixture of a 2:1 weight ratio of Tween 20 and ethyl alcohol.
The purpose of this study is to characterize D-cycloserine (DCS) physicochemical properties to facilitate future formulation development of DCS for anxiety disorders. A stability-indicating HPLC assay method for the quantitation of DCS was developed and calibrated to be used for this study. The partition coefficient was determined and compared with the predicted value. The solution stability of DCS was studied under various pH (2-11.5) and ionic strengths of 10 and 20 mM at physiological temperature of 37°C. The 250 mg capsule was compounded to the nominal strength of 50 mg used for anxiety disorders. These capsules were then put under stability. The in vitro dissolution was also carried out at 37°C as per the United States Pharmacopeia (USP) guidelines. The partition coefficient value (Kp) determined for the DCS was log Kp = –2.89 ± 0.06 (n = 6). The pH-solution stability profile shows that DCS has maximum stability under alkaline conditions. The maximum rate of degradation was seen at pH of 4.7. The mean percent recovery of DCS from the capsules compounded to strength of 50 mg was 100.3 ± 1.4. The stability study of the reformulated capsules concluded that reformulated DCS is stable for at least one year at room temperature. The in vitro dissolution illustrates that all the DCS is released from the capsules in 10 min. The present characterization of DCS study will serve as guidance for the future directions regarding the reformulation of DCS in order to be used in anxiety disorders.