Antifungal Effect and Protective Role of Ursolic Acid and Three Phenolic Derivatives in the Management of Sorghum Grain Mold Under Field Conditions.

In this study, investigation was carried out under in vitro as well as field conditions to explore inhibitors of sorghum grain mold. Phytochemicals, viz., methyl trans-p-coumarate (AIC-1), methyl caffeate (AIC-2), syringic acid (AIC-3), and ursolic acid (UA), at different concentrations (500, 750, and 1000 ppm) were tested on spore germination of Alternaria alternata, Curvularia lunata, Fusarium moniliforme, F. pallidoroseum, and Helminthosporium sp. Significant growth inhibition (P < 0.001) was observed against all fungi except A. alternata which was found to be resistant to AIC-3. Further, two separate sets of field experiments involving spraying of water and F. moniliforme suspension over chemicals treated (1000 ppm) sorghum panicles were done. The levels of protection varied with different treatments which were graded using a standard 1 - 9 rating scale. The Fusarium-challenged panicles (FCP) showed lesser susceptibility and decreased the rate of infection of grain mold (grade 7.0), compared to simple UA, AIC-2, and AIC-1 treatments (7.4, 7.6, and 8.0 grade, resp.). The HPLC quantification of differentially induced phenolic acids in treated sorghum grains substantiated this effect disclosing the higher accumulation of chlorogenic, vanillic, and salicylic acids in FCP. This might be due to defensive induction of these acids by the plants. Although mold control by examined chemicals were lesser than the standard Tilt (grade 5.9), they were found to be nontoxic to mammalian cells under cytotoxicity assay.

Dermal wound healing potency of single alkaloid (betaine) versus standardized crude alkaloid enriched-ointment of Evolvulus alsinoides.

CONTEXT: Evolvulus alsinoides Linn. (Convolvulaceae), well known as shankhpushpi in Ayurvedic text, is traditionally used for several healing purposes. OBJECTIVE: A comparative evaluation of dermal wound healing potential of acidic and basic alkaloid enriched-ointment (AAO and BAO) of aerial parts of E. alsinoides versus pure alkaloid, betaine (BEO), was undertaken. MATERIAL AND METHODS: The effect of topical application (50 mg/animal/day) of AAO-1%, AAO-2%, BAO-1%, BAO-2%, BEO-0.5% and BEO-1% was assessed through excision (14 days) and incision (10 days) models on rats. The percentage wound contraction, total protein content, and breaking strengths were determined followed by histopathological studies. RESULTS AND DISCUSSION: The total alkaloid in acidic and basic alkaloid enriched fractions was found to be 0.1114 and 0.1134 µg/mL, respectively. Thus, 0.1528, 0.3056, 0.1380 and 0.2459 µg of total alkaloid were estimated to be present in AAO-1%, AAO-2%, BAO-1% and BAO-2%, respectively. AAO and BAO promoted wound healing activity significantly in both the models. Higher rate of wound contraction (p < 0.001) with significant increase in protein content in the treatment groups (from 2.32 to 2.55) demonstrated stimulation of cellular proliferation and epithelization, which was further supported by histopathological reports. High skin breaking strength (mean value 393 in control was increased to the range of 535-572 in treated groups) proved a significant (p < 0.001) wound healing potential of E. alsinoides. Early dermal and epidermal regeneration in drug-treated groups also confirmed the positive effect. CONCLUSION: Observation of higher healing power of alkaloid enriched-ointment compared with single alkaloid ointment corroborated the synergy mechanism.

Attenuation of TNF-α secretion by L-proline-based cyclic dipeptides produced by culture broth of Pseudomonas aeruginosa.

To identify small molecule inhibitors of TNF-α, bioassay- and LC-MS-guided chemical investigation on EtOAc extract of Pseudomonas aeruginosa ABS-36 culture broth (EEPA) was performed, which yielded four proline-based cyclic dipeptides, cyclo(Gly-l-Pro) (1), cyclo(l-Pro-l-Phe) (2), cyclo(trans-4-hydroxy-l-Pro-l-Phe) (3) and cyclo(trans-4-hydroxy-l-Pro-l-Leu) (4). Compounds 1 and 3 exhibited potent inhibition of TNF-α release with IC50 values of 4.5 and 14.2µg/mL, respectively, while EEPA showed IC50 of 38.8µg/mL under lipopolysaccharide treated RAW 264.7 cell ELISA assay. Also, marked attenuation of mRNA-expression of TNF-α was shown by all compounds. In vivo testing in rats of EEPA and chemically synthesized 4 validated significant TNF-α reduction with 51% (500mg/kg) and 79% (50mg/kg), respectively. In addition, all compounds exhibited significant diminution of IL-1ß and IL-6 mRNA-expression levels and NO production. All samples displayed only weak toxicity to lipopolysaccharide-induced RAW 264.7 cells.

Cytotoxic constituents of Abutilon indicum leaves against U87MG human glioblastoma cells.

The study was aimed to identify cytotoxic leads from Abutilon indicum leaves for treating glioblastoma. The petroleum ether extract, methanol extract (AIM), chloroform and ethyl acetate sub-fractions (AIM-C and AIM-E, respectively) prepared from AIM were tested for cytotoxicity on U87MG human glioblastoma cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. These extracts exhibited considerable activity (IC50 values of 42.6-64.5 µg/mL). The most active AIM-C fraction was repeatedly chromatographed to yield four known compounds, methyl trans-p-coumarate (1), methyl caffeate (2), syringic acid (3) and pinellic acid (4). Cell viability assay of 1-4 against U87MG cells indicated 2 as most active (IC50 value of 8.2 µg/mL), whereas the other three compounds were much less active. Interestingly, compounds 1-4 were non-toxic towards normal human cells (HEK-293). The content of 2 in AIM-C was estimated as 3% by HPLC. Hence, presence of some more active substances besides methyl caffeate (2) in AIM-C is anticipated.

Antiproliferative activity and standardization of Tecomella undulata bark extract on K562 cells.

ETHNOPHARMACOLOGICAL RELEVANCE: The bark of Tecomella undulata is primarily used in the treatment of syphilis, painful swellings and cancer by traditional healers. Also, it is claimed to be useful in treating urinary discharges, enlargement of spleen, leucorrhoea, leukoderma, tumors, liver disorders, gonorrhea, gout and promotes wound healing in Indian traditional system of medicine. AIM: To establish a scientific validation for the antitumor effects of Tecomella undulata bark and explore the mechanistic pathway in chronic myeloid leukemia cell line, K562. The study was further extended to standardize the extract using quercetin as biomarker. METHODS: Induction of apoptosis by chloroform extract of Tecomella undulata bark (CTUB) was determined by MTT, Annexin V and caspase activation assays. The cell cycle analysis was done by flow cytometer and nuclear staining by DAPI. The standardization of the extract was performed through reverse phase-HPLC method under PDA detection. RESULT: Results clearly showed the induction of apoptosis by CTUB in K562 cells. The effect was found to be dose dependent, having IC(50) of 30 µg/ml with activation of FAS, FADD, caspase 8, caspase 3/7 and fragmentation of DNA. The bioactive CTUB was determined to possess 0.03% (w/w) of quercetin. CONCLUSION: The investigation clearly demonstrated the potential antitumor effect of CTUB, thereby validating the traditional claim. Quercetin, known to have anticancer activity is being reported and quantified for the first time from the bark of Tecomella undulata.