Assessment of Antioxidative and Alpha-Amylase Potential of Polyherbal Extract.

The present study aims to prepare a polyherbal formulation (PHF) of Azadirachta indica (Neem), Aloe barbadensis (Aloe vera), Allium sativum (garlic), Acacia arabica (Babul), and Aegle marmelos (Bel) and evaluation of antidiabetic and antioxidant activity utilizing the in vitro model. Air-dried powder of 5 medicinal plants, which are divided into equal portions, and PHF, is prepared by the soxhlet technique using polar and nonpolar solvents. The PHF is screened for the phytochemical screening, and then the antidiabetic activity is determined by alpha-amylase inhibition. The extracts thus obtained are also subjected to the inhibition assay by the use of (DNS) dinitro salicylic acid. The antioxidant activity was determined by the DPPH radical scavenging assay, H2O2 scavenging assay, and TBARS assay. In in vitro study, the result revealed polyherbal formulation in which hot water extract has the topmost inhibitory effect on alpha-amylase activity, ranging from 20.4% to 79.5% with an IC50 value of 48.98 ± 0.31 µg/ml. This extract clearly showed the effective lowering of postprandial hypertriglyceridemia (PPHG). In the antioxidant activity carried out by using the (DPPH) radical scavenging assay, the highest result was obtained by the concentration of 250 µg/ml, which was around 77.2 ± 0.05 with statistical significance compared with control (a: p < 0.01; b: p < 0.001), while in the GTA method, the highest result was obtained by the concentration of 250 µg/ml, which was around 78.2 ± 0.05, and in the case of the TBARS assay, the concentration of 250 µg/ml gave around 76.2 ± 0.03 anti-oxidant value. In conclusion, the study shows that polyherbal formulation has superior antidiabetic activity and antioxidant properties.

Design and evaluation of dental pastes Containing anti-inflammatory drugs

Abstract Periodontitis is an oral disease associated with inflammation and pain with swollen and bleeding gums. In the present study, dental pastes containing NSAIDs, namely, diclofenac sodium and nimesulide (1 % w/w) were prepared to treat periodontitis. Dental pastes of diclofenac sodium and nimesulide (1 % w/w) were prepared with/without mucoadhesive hydrocolloid polymers such as sodium carboxy methyl cellulose (NaCMC), hydroxyl ethyl cellulose (HEC) and methyl cellulose (MC) by conventional trituration method. The pH, drug content, viscosity, tube spreadability and tube extrudability of these prepared dental pastes were measured. These dental pastes of diclofenac sodium and nimesulide (1 % w/w) were characterized by FTIR analyses for drug-excipient compatibility. The in vitro drug releases from these dental pastes in 6.4 pH phosphate buffer solution displayed sustained release over longer period and the drug release rate was found to be decreased when the concentration of mucoadhesive polymer was increased. These dental pastes displayed good adhesion to the oral mucosa revealing more retention time in mouth when tested for ex vivo mucoadhesion using bovine cheek pouch. The stability study results reveal that the DC3 and NC3 dental paste formulations were found stable enough over a longer period in different storage conditions. The present study revealed that the prepared mucoadhesive dental pastes of diclofenac sodium and nimesulide (1 % w/w) had good adhesion with the oral mucosa to maintain consistent release of drugs over prolonged time.

Neuroprotective effects of polyhydroxy pregnane glycoside isolated from Wattakaka volubilis (L.f.) Stapf. after middle cerebral artery occlusion and reperfusion in rats.

Wattakaka volubilis (L.f) (Stapf.) is well known for its rich steroid pregnane contents and this plant is known for its potential use as alternative biological activities. However, little is known about its neuroprotective effect in ischemia-reperfusion (I/R)-induced cerebral injury. Hence, the present study was carried out to investigate the effect of W. volubilis(L.f) (Stapf.) sapogenin glycosides mixture (WVSM) and polyhydroxy pregnane glycoside (PPG) isolated from it on neuroprotection and the potential mechanisms in the rat I/R model induced by middle cerebral artery occlusion (MCAO). The rats were pretreated with WVSM (50 mg/kg) and PPG (5 mg/kg and 10 mg/kg) (p.o.) once a day for 5 days before MCAO. Neurological deficit score (NDS), rotarod performance, brain water content, 2,3,5-triphenyltetrazolium chloride (TTC) staining and indices of oxidative stress [superoxide dismutase (SOD), malondialdehyde (MDA), nitric oxide (NO) and nitric oxide synthase (NOS)] were measured at 24 h after ischemia. The results indicated that pretreatment with WVSM and PPG (10 mg/kg) significantly diminished the volume of infarction and brain water content, and improved NDS. Moreover, WVSM and PPG (10 mg/kg) markedly reversed the level of MDA, NO, NOS and SOD to their normal state in serum or cerebral ischemic section. These findings demonstrate that WVSM and PPG (10 mg/kg) exhibit neuroprotective effect through its anti-oxidative action in MCAO rats.

In vivo and in vitro anti-inflammatory potential of pentahydroxy-pregn-14-ol, 20-one-ß-D-thevetopyranoside in rats.

Polyhydroxy pregnane glycoside (PPG), a steroidal glycoside was isolated from Wattakaka volubilis Linn. (Stap.f.). PPG was evaluated for in vivo and in vitro anti-inflammatory activity using acute inflammation and chronic model of inflammation in rats and LPS-induced RAW 264.7 macrophage cells. PPG seemed to be responsible for the anti-inflammatory activity in the studied models. PPG at dose level of both 5 and 10 mg/kg significantly reduced the edema induced by the carrageenan in acute model of inflammation. It also showed significant anti-proliferative effect (dry pellet weight basis) in chronic model of inflammation. Cellular content of granuloma was measured by assaying activity of N-acetyl glucosaminidase (NAG) and total nucleic acid content. PPG at 5 and 10 mg/kg significantly suppressed the cellular infiltration measured by total nucleic acid content. In contrast, NAG activity decreased over a period of 10 days resulting in inhibition of granuloma weight gain. PPG had a more effective response than the reference drug diclofenac sodium in both the models of inflammation. Wattakaka volubilis steroidal glycoside mixture (WVSM) and PPG (1-50 µM) significantly inhibited the COX-2 and iNOS enzymes resulting in low levels of PGE2 and NO in LPS-induced RAW 264.7 macrophage cells. Hence the study supports the traditional use of Wattakaka volubilis and its constituent PPG in treatment of inflammatory disorders.