ABSTRACT
Millettia ovalifolia is traditionally used in variety of diseases including inflammation. In our investigation in to the phytochemical constituents of Millettia ovalifolia an effort was made to find out bioactive constituent from medicinal Plant M. ovalifolia to scientifically validate its use in inflammatory disorders. The compound 7-hydroxy-6-methoxy-2H-chromen-2-one was isolated from the bark of M. ovalifolia and was found to exhibited significant lipoxygenase [LOX] inhibitory activity with [IC50 value: 116.83+/-0.02?M]. The Standard compounds Baicalein and Tenidap sodium revealed IC50 value being 22.1+/-0.03?M and 41.6+/-0.02?M. Molecular docking study further displayed significant molecular interactions between 7-hydroxy-6-methoxy-2H-chromen-2-one and LOX showed potential for further optimization as a possible anti-inflammatory lead compound
ABSTRACT
A dimeric naphthoquinone namely dihydrodyspyrole R [1] was purified once more from Diospyros lotus. Dihydrodyspyrole R and chloroform fractions were evaluated for their effects on the reversion of multidrug resistance [MDR]. The compounds [1] and extract exhibited promising MDR reversing effect in a dose-dependent manner against mouse T-lymphoma cell line. Molecular docking of compound 1 revealed the correlation between in-silico with in-vitro results. The molecular docking results showed that compound 1 is bind closely where co-crystal ligand of P-gp is present. But usually, computational investigation predicts that, if a compound gives lesser score then compound will exhibit good activity. Hence, the docking scores of compound 1 are the near to the Rhodamine. It is conclude that there are certain important structural features of compound 1which are responsible for the inhibiting potency of P-gp from mice. The computational Petra/Osiris/Molinspiration [POM] analysis confirms the possibility of use of compound 1 without side effect or less toxicity risks
ABSTRACT
Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 µmol·L, respectively, using thiourea (IC = 21 ± 0.11 µmol·L) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.
Subject(s)
Biological Assay , Diospyros , Chemistry , Enzyme Inhibitors , Chemistry , Pharmacology , Molecular Structure , Naphthoquinones , Chemistry , Pharmacology , Plant Extracts , Chemistry , Pharmacology , Plant Roots , UreaseABSTRACT
The aim of the current study was to evaluate the antinociceptive activity of the selected Pakistani medicinal plants [Chenopodium botrys, Micromeria biflora and Teucrium stocksianum] in-vivo followed by their antioxidant potential against 1,1-diphenyl-2-picrylhidrazyl [DPPH] in-vitro. The results demonstrated profound antinociceptive effect of both the crude methanolic extract of Chenopodium botrys [CBM] and subsequent aqueous fraction [CBW] of C. botrys with 80.76% and 84% pain relief in acetic acid induced writhing test at 100 mg/kg i.p respectively. Similarly the crude methanolic extract of Micromeria biflora [MBM] and its subsequent aqueous fraction [MBW] with 66.46% 78.08% pain reversal in acetic acid induced writhing test respectively at 100mg/kg i.p. However, the crude methanolic extract and isolated water fraction of Teucrium stocksianum [TS] did not show any significant effect at test doses. Both the crude extracts and aqueous fractions of selected medicinal plants exhibited marked scavenging effects on DPPH and therefore strongly support the antinociceptive activity. Phytochemical analysis indicated the presence of various classes of natural products [alkaloids, terpenoids, flavonoids etc.] and thus the current finding can be attributed to the presence of these compounds. In short, our findings provide a strong scientific background to the folk uses C. botrys and M. biflora in the management of various painful conditions
ABSTRACT
OBJECTIVE: To evaluate the sedative effect of Diospyros lotus L (D. lotus) extract in mice using the open field and Rota rod tests. METHODS: For the sedative and muscle relaxants activities of extract/fractions of the plant, in-vivo open field and phenobarbitone-induced sleeping time were used, while the Roda rod test was employed in animals for the assessment of muscle relaxant activity. RESULTS: Results from this investigation revealed that the extracts of D. lotus have exhibited significant sedative effect in mice (45.98%) at 100 mg/kg i.p. When the extract was partitioned with different solvents, the n-hexane fraction was inactive whereas the chloroform fraction was the most active with 82.67% sedative effect at 50 and 100 mg/kg i.p. On the other hand, the ethyl acetate and n-butanol fractions displayed significant sedative effects (55.65% and 40.87%, respectively) at 100 mg/kg i.p. Among the tested extract/fractions, only chloroform and ethyl acetate fractions showed significant (P < 0.05) muscle relaxant activity in the Rota rod test. CONCLUSIONS: In short, our study provided scientific background to the traditional uses of D. lotus as sedative.
ABSTRACT
<p><b>OBJECTIVE</b>To evaluate pharmacologically the traditional use of Diospyros lotus as antipyretic and antinociceptive in various animal models.</p><p><b>METHODS</b>In vivo experimental models were used in this study. Antipyretic activity of extract/fractions was evaluated in brewer's yeast induced hyperthermic mice while antinociceptive activity was studied in acetic acid induced writhing test at 50 and 100 mg/kg i.p.</p><p><b>RESULTS</b>The crude extract strongly ameliorated the induced pyrexia during various assessment times. Upon fractionation, the antipyretic effects were strongly augmented by the chloroform and ethyl acetate fractions of the plant. However, hexane and butanol fractions were insignificant in their effect as antipyretic. The extract showed marked inhibition on the noxious simulation induced by post acetic acid injection. The effect was strongly supported by other fraction expect hexane.</p><p><b>CONCLUSIONS</b>In short, our study scientifically validated the traditional use of the plant as antipyretic.</p>
ABSTRACT
To explore the free radical scavenging properties of crude ethanolic extract of galls, bark, leaves, roots of Pistacia integerrima and its subsequent solvent fractions viz., n-hexane, chloroform, ethyl acetate and methanol against 1, 1-diphenyl-2-picrylhydrazyl [DPPH] stable. In vitro DPPH based free radical was employed using querceitin as standard antioxidant while methanol as negative control. Different parts of P. integerrima showed marked scavenging on DPPH in a concentration dependent manner. The ethanolic extract exhibited 60.51 88.51% scavenging effect on DPPH which differentiated upon fractionation. Of the part used, leaves of the plant were the least effective while n-hexane was the least dominant fraction. However, the rest of the parts and fractions demonstrated profound scavenging potential. This in-vitro study revealed an outstanding free radical scavenging potential of various solvent fractions of different parts of whole plant P. integerrima
ABSTRACT
Euphorbia milii is a Pakistani herb used for various infectious diseases. In this study we have carried out phytochemical, antibacterial and antioxidant investigation of different extracts/fractions. Phytochemical studies showed the presence of cardiac glycosides, steroids/phytosterols, anthocyanin, proteins, terpenoids, flavonoids and tannins. Susceptibility testing by well diffusion assay of its chloroform and methanol fractions revealed good antimicrobial activity against Klebsiella pneumonia and Staph epidermis. Ethyl acetate fraction of roots also exhibited considerable antimicrobial activity against most of tested pathogens. Various fractions [Hexane, chloroform, methanol and water] of E. milii were screen for their antioxidant potential using DPPH radical scavenging assay at different concentrations among these, chloroform fraction exhibited good scavenging activity. The IR spectroscopy of the various extracts/fractions indicated the presence of OH, saturated CH stretching, C=C, C=O, NO[2], C-N, Ar-O, C-O- and R-O-Stretching respectively. The findings provide helpful evidence for the use of E. milii in traditional medicines