Background
The present study was aimed to evaluate the molecular level anticaries effect of different medicinal plants against
Streptococcus mutans
(
S.mutans)
glucosyltransferases (gtf).
Methods
A total of six natural sources named as
Terminalia chebula (T.chebula), Psidium guajava (P.guajava), Azadirachta indica (A.indica) and Pongamia pinnata (P.pinnata)
; two essential oils, clove (
Syzygium aromaticum
) and peppermint oil (
Mentha piperita
) were selected as test samples. Hydroalcoholic plant extracts and essential oils were examined for their inhibitory potential on
gtf
isolated from
S.mutans.
Polyherbal mouth wash was prepared and its effect on
gtf
activity was compared with commercial chlorhexidine mouth wash (5%w/v). Enzyme kinetic study was carried out in order to explore the molecular mechanism of enzyme action.
Results
Out of six natural sources tested,
A.indica
has shown maximum inhibitory effect of 91.647% on
gtf
and
T.chebula
has shown IC
50
of 1.091 mg/ml which is significant when compared to standard chlorhexidine. From the final result of kinetic analysis it was found that
T.chebula, P.guajava
and
P.pinnata
have show uncompetitive inhibition where as
A.indica has shown non-competitive inhibition.
Surprisingly, both essential oils have shown allosteric inhibition (sigmoidal response). The polyherbal moutwash has shown significant inhibitory potential on
gtf
(95.936%) when compared to commercial chlorhexidine mouthwash (
p
< 0.05).
Conclusion
All the tested samples have shown considerable
gtf
inhibitory action. Moreover polyherbal mouth wash has shown promising noncompetitive inhibitory activity against
gtf
and it could be the future formulation to combat dental caries.
Background: Cancer is one of the leading causes of death and globally the numbers of cases of cancer are increasing gradually. However, surgeries, chemotherapies have become safer, but these treatments have debilitating side effects. Flavonoids present in the human diet comprise many polyphenolic secondary metabolites with broad-spectrum pharmacological activities including their potential role as anti-cancer agents. Objective: The objective of the present study was to extract, orange peel flavonoids (Orange Peel Extract) and to screen anticancer potential of OPF. Methods: In the present study tryphan blue dye exclusion, clonogenic assay and nuclear damage studies by ethidium bromide staining were performed to estimate in vitro antitumor properties of Orange Peel Extract and subsequently in vivo studies also performed using the Dalton Lymphoma Ascites (DLA) tumor model in Swiss albino mice. Results: In vitro studies revealed the moderate toxicity, high regenerative capacity of Orange Peel Extract and also showed changes in nuclear morphology similar to that of apoptotic cells which is one of the important aspect of an anticancer drug. In vivo studies confirmed the anticancer activity of Orange Peel Extract and has increased the average life span of treated animals and restored the antioxidant enzyme levels and hematological parameters to normal which was comparable to that of standard methotrexate. Conclusion: Overall, these findings have proved that out of the two doses (50mg/kg bw and 200mg/kg bw) employed for the study lower dose (50mg/kg) was found to be more effective than higher dose (200mg/ kg). Hence flavonoid fraction of orange peels can be the better alternative to treat cancer.
Background:Transdermal drug delivery system (TDDS) was designed to sustain the release and improve the bioavailability of drug and patient compliance. Among the various types of transdermal patches, matrix dispersion type systems disperse the drug in the solvent along with the polymers and solvent is allowed to evaporate forming a homogeneous drug-polymer matrix. The objective of the present study was to design and formulate TDDS of topiramate (TPM) and to evaluate their extended release in vitro and ex vivo.Materials and Methods:In the present study, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising TPM with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent casting technique.Results:The physicochemical compatibility of the drug and the polymers was studied by Fourier transform infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the ex vivo permeation studies using pig ear skin.Conclusions:On the basis of results obtained from the physical evaluation and ex vivo studies the patches containing the polymers, that is, Eudragit L 100 and polyvinylpyrrolidone, with oleic acid as the penetration enhancer were considered as the best formulations for the transdermal delivery of TPM.
Nowadays the prevalence of hyperuricemia has significantly increased in which serum uric acid levels are exceeding the normal range. Gout is the predominant clinical implication of the hyperuricemia, but many clinical investigations have confirmed that hyperuricemia is an independent risk factor for cardiovascular disease (CVD), hypertension, diabetes, and many other diseases. The xanthine oxidase (XO) converts hypoxanthine to xanthine and ultimately to uric acid, and the irreversibly accumulated uric acid causes hyperuricemia associated with gout. Hence specific and selective xanthine oxidase inhibitors (XOI) are potentially powerful tools for inactivating target XO in the pathogenic process of hyperuricemia (Gout). The objective of the current study was to overview the various XOI isolated from the microorganisms. Microorganisms have been employed for several decades for the large-scale production of a variety of bio-chemicals ranging from alcohol to antibiotics and as well as enzyme inhibitors. Currently available XOI (allopurinol and febuxostat) for the treatment of gout have been exhibiting serious side effects. Thus, there is a need to search for new molecules to treat hyperuricemia and its associated disorders. At present, microbes have been unexplored in the development of successful products for the management of XO-related diseases. Hence, the present review focused on novel XOI produced from various microbial species such as Actinobacteria, lichens, bacteria, endophytic fungi and mushrooms, which can be expected to play an important role in the ongoing transition from the empirical screening to the real rational drug design.
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