Sub chronic toxicity potential of the alcoholic extract of Biophytum reinwardtii whole plant

Biophytum reinwardtii Edgew is an important and highly valued sensitive medicinal small herb and whole plant is ethnobotanically used in the treatment of insomnia, convulsion, inflammation, lithiasis, fevers and gonorrhea. The present study was carried out to evaluate acute and sub-chronic toxicity of alcoholic extract of Biophytum reinwardtii Edgew (B. reinwardtii) whole herb extract in albino mice and rats. The median acute toxicity value ( LD50 ) of the extract of B. reinwardtii was determined to be 588.88 mg/kg b.w. (i.p.) in mice. In sub-chronic toxicity studies 50, 75 and 100 mg/kg b.w. of the alcoholic extracts of B. reinwardtii (AEBR) whole plant were administered orally to the test groups while distilled water was given to the control group. The parameters measured include food and fluid intake, body weight, absolute and relative weight of various organs, haematological parameters [total white blood cell (WBC) and packed cell volume (PCV)], and tests for liver function: Serum glutamic oxaloacetic transaminase (SGOT), Serum glutamic pyruvic transaminase (SGPT), alkaline phosphatase and total bilirubin. Rats treated with AEBR in the therapeutic dose level had no progressive increase in body weight or fluid intake. There were no significant changes in both the absolute and relative organ weights between the control and the test groups after 30 days. The liver enzymes and haematological parameters were statistically equal in all the groups. The results of the present study therefore indicated that B. reinwardtii whole herb is safe in adult male albino mice demonstrating no noticeable toxicity. Keywords: Biophytum reinwardtii, sub-chronic toxicity, liver function, packed cell volume, absolute weight, relative weight

Flavonoids and Phenolic Compounds from Litsea polyantha Juss. bark

The 18th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic, Medicinal and Natural Products ChemistryFlavonoids and phenolic compounds from plants have been reported to have multiple biological effects. In the present communication, bioactive compounds from Litsea polyantha Juss. bark were studied. The total phenolic content was determined by using the Folin-Ciocalteu reagent and aluminum chloride colorimetric method was used for determination of total flavonoids. The content of phenolics in 100 gm (dry weight) extract of Litsea polyantha Juss. was 511.472 ± 22.304 mg gallic acid equivalent (GAE), while total flavonoid content was 230.785 ± 5.439 mg/g quercetin equivalent in MELP. Results obtained showed that the plant materials studied are a good source of phenolic and flavonoids compound

Optimization Process for Increasing the Yield of Crude Alkaloid from Litsea polyantha Juss. bark

The 18th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic, Medicinal and Natural Products ChemistryLitsea polyantha Juss. (Lauraceae) also known as Litsea monopetala Roxb. is a small to medium sized evergreen tree distributed chiefly in tropical and subtropical Asia, Australia and the Pacific Islands. The bark of Litsea polyantha Juss. has a long history of medicinal use among the traditional healers of Oraon and Munda community of Jharkhand (India). In this work, optimization process for increasing the yield of crude alkaloid from Litsea polyantha Juss. bark was performed by taking pH and temperature as the factors influencing the yield. With the help of yield optimization by 22 factorial design the percentage yield of crude alkaloid was increased from 3.8% w/w to 17.3% w/

A novel druggable interprotomer pocket in the capsid of rhino- and enteroviruses

Rhino- and enteroviruses are important human pathogens, against which no antivirals are available. The best-studied inhibitors are capsid binders that fit in a hydrophobic pocket of the viral capsid. Employing a new class of entero-/rhinovirus inhibitors and by means of cryo-electron microscopy (EM), followed by resistance selection and reverse genetics, we discovered a hitherto unknown druggable pocket that is formed by viral proteins VP1 and VP3 and that is conserved across entero-/rhinovirus species. We propose that these inhibitors stabilize a key region of the virion, thereby preventing the conformational expansion needed for viral RNA release. A medicinal chemistry effort resulted in the identification of analogues targeting this pocket with broad-spectrum activity against Coxsackieviruses B (CVBs) and compounds with activity against enteroviruses (EV) of groups C and D, and even rhinoviruses (RV). Our findings provide novel insights in the biology of the entry of entero-/rhinoviruses and open new avenues for the design of broad-spectrum antivirals against these pathogens.Peer reviewe

Monoamine Oxidase Inhibitory Activity Of Novel Pyrazoline Analogues: Curcumin Based Design And Synthesis

A series of new 2-methoxy-4-(5-pheny1-4,5dihydro-1H-pyrazol-3-yl)phenolderivatives, 4-13, were synthesized and tested for their human MAO inhibitory activity. All the compounds were found to be selective and reversible toward hMAO-A except 4, a selective inhibitor of hMAO-B and 12, a nonselective inhibitor. Compound 7 was found to be a potent inhibitor of hMAO-A with K-i = 0.06 +/- 0.003 mu M and was having selectivity index of (SI = 1.02 X 10(-5)). It was found to be better than standard drug, Moclobemide (hMAO-A with K = 0.11 +/- 0.01 mu M) with selectivity index of SI = 0.049. Molecular docking simulation was carried out to understand the crucial interactions responsible for selectivity and potency.Wo

Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1

Phytoestrogens are class of natural compounds that shares structural similarity with estrogen and has the capacity to alter the fertilization in mammals. Till early 1990s, the natural phytoestrogens as well as their synthetic analogues were explored for their fertility modulating activity. During late 1990s, two findings renewed the interest on phytoestrogens as means to control hormone induced cancer: (i) revelation of overexpression of CYP1B1 in breast &amp; ovarian cancer and (ii) protection offered by alphanapthoflavone (ANF) against hormone induced cancer. The objective of the review is to summarize the CYP1B1 inhibitory activity of phytoestrogens and their synthetic analogues reported till date. This review is an attempt to classify phytoestrogens and their synthetic analogues on their chemical architecture rather than simply by their chemical class (flavones, stilbenes etc.). This provides a broader sense to cluster many chemical classes under a particular chemical architecture/framework. Accordingly, we divided the phytoestrogen into three different classes based on two aryl groups (Ar) separated by linker (X), which may be either cyclic (c) or linear (l). The number in subscript to X denotes number of atoms: (i) Ar-cX4-Ar, (ii) Ar-lX3-Ar and (iii) Ar-lX2-Ar. This provides an opportunity to cluster flavones, quinolines and quinazolinones under Ar-cX4-Ar class, while biphenyl ureas and chalcones under Ar-lX3-Ar class. We believe in coming years many chemical scaffolds may be clustered under this framework.</p

New chemical constituents from the <i>Piper betle</i> Linn. (Piperaceae)

<p>The phytochemical investigation of chloroform extract from <i>Piper betle</i> var. <i>haldia</i>, Piperaceae, leaves has resulted in the isolation of two new chemical constituents which were identified as 1-<i>n</i>-dodecanyloxy resorcinol (<b>H1</b>) and desmethylenesqualenyl deoxy-cepharadione-A (<b>H4</b>), on the basis of spectroscopic data 1D NMR (¹H and ¹³C) and 2D NMR (¹H-¹H COSY and HMBC) as well as ESI-MS, FT-IR and HR-ESI-MS analyses. Compounds <b>H1</b> and <b>H4</b> showed excellent antioxidant DPPH free radical scavenging activity with IC₅₀ values of 7.14 μg/mL and 8.08 μg/mL compared to ascorbic acid as a standard antioxidant drug with IC₅₀ value of 2.52 μg/mL, respectively. Evaluation of cytotoxic activity against human hepatoma cell line (PLC-PRF-5) showed moderate effect with the GI₅₀ values of 35.12 μg/mL for <b>H1</b>, 31.01 μg/mL for <b>H4</b>, compared to Doxorubicin^® as a standard cytotoxic drug with GI₅₀ value of 18.80 μg/mL.</p