Antibacterial and Antifungal Activities of Different Parts of Tagetes patula.: Preparation of Patuletin Derivatives

Abstract

The current study evaluates the antibacterial and antifungal activities of extracts from different parts of Tagetes patula. Linn. (Asteraceae), reported for the first time in a single set of experiments. In the preliminary assay, the methanol extract of the flower (JFM) was found to possess antimicrobial activity against a number of bacteria with inhibition zone diameters ranging from 9 to 20 mm, the bioassay-guided fractionation of which led to the isolation of a flavonoid patuletin (3) in high yield as the active antibacterial principle with minimum inhibitory concentration (MIC) value of 12.5 μ g/disk against Corynebacterium. spp., Staphylococcus. spp., Streptococcus. spp., and Micrococcus luteus.. Its glucoside, patulitrin (4), was found to be weakly active, except against Staphylococcus saprophyticus., Streptococcus fecalis., and Streptococcus pyogenes. with inhibition zone diameters of 11, 16, and 12 mm, respectively. The cinnamate derivative (3b) of 3 showed antibacterial activity comparable with the parent flavonoid with a MIC value of 50 μ g/disk against Corynebacterium. spp., whereas benzoate derivative (3a) was found to be devoid of any activity; both the derivatives are new compounds. Moreover, the long-chain alcohol 5, which displayed antibacterial activity in the preliminary testing, was obtained in large quantity directly from the petroleum ether extract of the involucre of the flowers.     

Hypoxia and metastasis in an orthotopic cervix cancer xenograft model

Background

Hypoxia can promote tumor metastasis by mechanisms that are believed to result from changes in gene expression. The current study examined the role of putative metastatic genes regulated by cyclic hypoxia in relation to metastasis formation in orthotopic models of cervix cancer.

Methods

Orthotopic tumors derived from ME180 human cervix cancer cells or from early generation human cervix cancer xenografts were exposed to cyclic hypoxic conditions during growth in vivo and tumor growth and lymphnode metastases were monitored. Expression of the chemokine receptor CXCR4 and various genes in the Hedgehog (Hh) pathway were inhibited using genetic (inducible shRNA vs CXCR4) small molecule (AMD3100) or antibody (5E1) treatment (CXCR4 and Hh genes, respectively) during tumor growth.

Results

As reported previously, exposure of tumor bearing mice to cyclic hypoxia caused a reduction of tumor growth but a large increase in metastasis. Inhibition of CXCR4 or Hh gene activity during tumor growth further reduced primary tumor size and reduced lymphatic metastasis to levels below those seen in control mice exposed to normoxic conditions.

Conclusion

Blocking CXCR4 or Hh gene expression are potential therapeutic pathways for improving cervix cancer treatment.     

Modulation of wireless (2.45 GHz)-induced oxidative toxicity in laryngotracheal mucosa of rat by melatonin

It is well known that oxidative stress induces larynx cancer, although antioxidants induce modulator role on etiology of the cancer. It is well known that electromagnetic radiation (EMR) induces oxidative stress in different cell systems. The aim of this study was to investigate the possible protective role of melatonin on oxidative stress induced by Wi-Fi (2.45 GHz) EMR in laryngotracheal mucosa of rat. For this purpose, 32 male rats were equally categorized into four groups, namely controls, sham controls, EMR-exposed rats, EMR-exposed rats treated with melatonin at a dose of 10 mg/kg/day. Except for the controls and sham controls, the animals were exposed to 2.45 GHz radiation during 60 min/day for 28 days. The lipid peroxidation levels were significantly (p < 0.05) higher in the radiation-exposed groups than in the control and sham control groups. The lipid peroxidation level in the irradiated animals treated with melatonin was significantly (p < 0.01) lower than in those that were only exposed to Wi-Fi radiation. The activity of glutathione peroxidase was lower in the irradiated-only group relative to control and sham control groups but its activity was significantly (p < 0.05) increased in the groups treated with melatonin. The reduced glutathione levels in the mucosa of rat did not change in the four groups. There is an apparent protective effect of melatonin on the Wi-Fi-induced oxidative stress in the laryngotracheal mucosa of rats by inhibition of free radical formation and support of the glutathione peroxidase antioxidant system.     

Acid phosphatases from the liver of Labeo rohita: purification and characterization

Low molecular weight acid phosphatase (LM-ACP) peak 2 (the isoenzyme corresponding to isoform 2, IF-2) from the liver of fish Rahu (Labeo rohita) was purified to homogeneity. 900 times purification resulted with specific activity of 35 U/mg of protein and recovery of 0.2%. The enzyme was found homogeneous on sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS-PAGE). Molecular weight of 18 killo Daltons (kDa) was obtained. The peak 1 isoenzyme corresponding to isoform1 (IF-1) was partially purified about 160 times with specific activity of 7 U/mg of protein. Major protein band corresponding to 18 kDa was seen along with other protein faint bands. High molecular weight acid phosphatase (HM-ACP) was also partially purified. The molecular weight was estimated to be a 100 kDa by gel filtration on Sephadex G-100. LM-ACP isoenzymes and HM-ACP enzyme were studied for their substrate specificity, sensitivity to inhibitors or activators and other kinetic parameters. LM-ACP isoenzymes were not inhibited by tartrate and fluoride but were inhibited by sulfhydryl reagent whereas high molecular weight enzyme was strongly inhibited by fluoride and tartrate. Phosphate vanadate and molybdate inhibited both types of enzymes competitively, but their action was more pronounced in HM-ACP enzyme. LM-ACP was effectively activated by purine compounds whereas HM-ACP was not. LM-ACP showed strict substrate specificity while HM-ACP showed broad substrate specificity. The two types of acid phosphatases also differed in their rate of hydrolysis of alpha-naphthyl phosphate and beta-glyerophosphate.     

Cystic schwannoma of the pelvis

Schwannomas are benign tumours that arise from the Schwann cells of nerve fibres. They commonly occur in the head and neck, mediastinum and extremities. They are extremely rare in the pelvis. These are usually slow growing tumours and are often detected incidentally. Pre-operative diagnosis is extremely difficult as there are no definitive signs on imaging. Aspiration biopsy is often inconclusive or misleading. Surgical excision is both diagnostic and therapeutic. As these tumours are often large in size, open excision is most commonly performed. We describe a case of a large, cystic schwannoma of the pelvis causing bladder outlet obstruction and bilateral hydroureteronephrosis. Complete surgical excision was performed laparoscopically.     

Adaptive analysis of cortical plasticity with fMRI in full face and arm transplants

The aim of this study is to examine cortical plasticity and to analyze cortical reorganization following hand and facial transplantation, using functional magnetic resonance imaging. Patients who had undergone full-face transplantation, hand transplantation and scapular arm replantation, as well as healthy controls, participated in the study. The perioral area and volar surfaces of the index finger and thumb were stimulated and images were acquired using 3 T functional MRI. The areas of the somatosensory cortex representing the hand and face are different in size and shape due to experience-dependent plasticity. Therefore, a new and more adaptive volume of interest analysis was created whereby the radiuses of the VOI masks were defined by the peak intensity of subsequent clusters. For each control subject, the distribution of activated voxels was observed for various cluster defining thresholds in order to determine the mean number of activated voxels for each stimulation inside the defined region. The determined numbers of voxels per subject were extracted from the defined regions using a binary search algorithm. Subsequently, the distances between the weighted centers of the extracted regions were calculated and compared. In transplant patients, the weighted centers of the hand and face clusters were separated at same-sized volumes. Two of the rehabilitated full-face transplant patients converge to the range of the controls. As a result, the weighted distribution of somatotopy indicated previous and present cortical reorganization. Additionally, referred sensation was assessed in two full-face transplant and one replant patient with activation clusters partially in BA40 in the Inferior Parietal Lobule.