Magnolol is one of main active constituents from Magnolia officinalis, a widely used traditional Chinese medicine. Previous studies have proved its multiple pharmacological effects, such as anti-oxidation, anti-microbial and anti-tumor. In recent years, more and more studies have focused on magnolol both at home and abroad. This essay summarizes the advance in the latest studies on the pharmacological effects of magnolol, and briefs main problems in current studies and future development orientation.
Animals ; Biphenyl Compounds ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Lignans ; pharmacology ; Magnolia ; chemistry

Honokiol is the dominant biphenolic compound isolated from the Magnolia tree, and has long been considered as the active constituent of the traditional Chinese herb, 'Houpo', which is widely used to treat symptoms due to 'stagnation of qi'. Pharmacological studies have shown that honokiol possesses a wide range of bioactivities without obvious toxicity. Honokiol protects the liver, kidneys, nervous system, and cardiovascular system through reducing oxidative stress and relieving inflammation. Moreover, honokiol shows anti-diabetic property through enhancing insulin sensitivity, and anti-obese property through promoting browning of adipocytes. In vivo and in vitro studies indicated that honokiol functions as an anti-cancer agent through multiple mechanisms: inhibiting angiogenesis, promoting cell apoptosis, and regulating cell cycle. A variety of therapeutic effects of honokiol may be associated with its physiochemical properties, which make honokiol readily cross the blood brain barrier and the blood-cerebrospinal fluid barrier, with high bioavailability. In the future, more clinical researches on honokiol are needed to fully authenticate its therapeutic values.
Apoptosis ; Biphenyl Compounds/pharmacology* ; Drugs, Chinese Herbal/pharmacology* ; Humans ; Lignans/pharmacology* ; Magnolia

OBJECTIVETo investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius (A. ilicifolius).

METHODSAntioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil (DPPH) method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test.

RESULTSA. ilicifolius flower contained terpenoid, phenolic compounds, and alkaloid. The methanol extract of A. ilicifolius flower showed the highest antiradical efficiency (AE=1.41×10(-3)) against DPPH radicals and the highest cytotoxicity (LC50=22 µg/mL) against brine shrimp nauplii.

CONCLUSIONSIt is suggested that active compounds of A. ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii. The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.

Acanthaceae ; chemistry ; Animals ; Antioxidants ; pharmacology ; Artemia ; drug effects ; Biphenyl Compounds ; chemistry ; pharmacology ; Cytotoxins ; toxicity ; Flowers ; chemistry ; Lethal Dose 50 ; Picrates ; chemistry ; pharmacology ; Plant Extracts ; chemistry ; pharmacology

AIMTo investigate whether the selective AT1 receptor antagonist irbesartan exerts neuroprotective effect on focal cerebral ischemia in normotensive rats.

METHODSCerebral ischemia was induced by middle cerebral artery occlusion (MCAO) for 90 min followed by reperfusion, with the monitoring of laser Doppler flowmetry. To avoid the interaction with peripheral AT1 receptors, irbesartan was infused intracerebroventricularly (ICV) at a dose which effectively inhibited brain- but not vascular AT1 receptors. Neurological status was evaluated daily after MCAO. Rats were killed and brain samples were collected for the measurement of infarct size and immunohistochemical evaluation of apoptosis by deoxynucleotidyltransferase-mediated biotinylated UTP nick end labeling (TUNEL) and expression of activated Caspase-3 and the cleavage fragment of poly (ADP-ribose) polymerase (PARP).

RESULTSTreatment with irbesartan improved significantly the neurobehavioral functions after cerebral ischemia. The infarct size was reduced about 42% on day 7 after MCAO (P < 0.05). Meanwhile,irbesartan treatment significantly decreased the number of TUNEL-positive cells in the penumbra. The expression of activated Caspase-3 and the downstream cleavage fragment of poly (ADP-ribose) polymerase in the penumbra were also inhibited by irbesartan therapy on day 3 after transient cerebral ischemia.

CONCLUSIONAngiotensin AT1 receptor antagonist exhibits neuroprotection against transient cerebral ischemia in the brain. The neuroprotective effects in ischemic tissue may be associated with its inhibition of apoptotic cell death in the penumbra.

Angiotensin Receptor Antagonists ; pharmacology ; Animals ; Biphenyl Compounds ; pharmacology ; Cerebral Infarction ; pathology ; Ischemic Attack, Transient ; drug therapy ; pathology ; Lateral Ventricles ; Male ; Neuroprotective Agents ; pharmacology ; Rats ; Rats, Wistar ; Tetrazoles ; pharmacology

OBJECTIVETo study the phytochemical screening of different extracts from Citrullus colocynthis (C. colocynthis ) seeds extracts and to assess their antioxidant activity on the DPPH free radical scavenging.

METHODSPhytochemical screening, total content of polyphenols and flavonoids of C. colocynthis seeds extracts, including a crude aqueous extract (E1), a defatted aqueous extract (E2), a hydromethanolic extract (HM), an ethyl acetate extract (EA) and a n-butanol extract (n-B) was carried out according to the standard methods and to assess their corresponding effect on the antioxidant activity of this plant.

RESULTSNone of these extracts contained detectable amount of alkaloid, quinone, antraquinone, or reducing sugar. Catechic tannins and flavonoids were abundant in E1, HM and EA, whilst terpenoids were abundantly present in E1 and n-B but only weekly in HM. Coumarins were found in E2, EA and n-B. Polyphenols, expressed as gallic acid equivalent, amounted, per 100 g plant matter, to 329, 1002 and 150 mg in EA, HM an E1 respectively. Flavonoids, expressed as catechin equivalent, amounted, per 100 g plant matter to 620, 241 and 94 mg in EA, HM and E1 respectively. Comparable values were found in n-B and E1, with lower values in E2. Quercetin, myricetin and gallic acid were found in the EA and HM extracts by thin layer chromatography, The antioxidative effect of these extracts yielded, when tested at a concentration of 2 000 µg/mL in a 1,1-diphenyl-2-picrylhydrazyl assay, a reducing percentage of 88.8% with EA, 74.5% with HM and 66.2% with E1, and corresponding IC50 of 350, 580 and 500 µg/mL as compared to 1.1 µg/mL for ascorbic acid.

CONCLUSIONSThese qualitative and quantitative analytical data document the presence in C. colocynthis extracts of such chemical compounds as flavonoids responsible for the antioxidant activity, as well as other biological activities of this plant.

Antioxidants ; chemistry ; pharmacology ; Biphenyl Compounds ; chemistry ; Citrullus colocynthis ; chemistry ; Free Radical Scavengers ; chemistry ; pharmacology ; Oxidation-Reduction ; drug effects ; Picrates ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Seeds ; chemistry

OBJECTIVETo study the rubrofusarin glucosides from whole plants of Berchemia polyphylla var. leioclada, and their scavenging activities for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical.

METHODThe chemical constituents were isolated and purified via repeated silica gel and Sephadex LH-20 column chromatography. Their structures were elucidated by spectral analysis and the compounds were tested for their scavenging activities on DPPH radical.

RESULTThree rubrofusarin glucosides compounds were isolated and identified as rubrofusarin-6-O-beta-D-glucopyranoside (1), rubrofusarin-6-O-beta-D-(6'-O-acetyl) glucopyranoside (2), rubrofusarin-6-O-alpha-L-rhamnosyl-(1-6) -O-beta-D-glucopyranside (3). Three isolated compounds showed strong scavenging activities on DPPH radical, the concentration of half elimination ratio( micromol x L(-1)) of VitC and Compounds 1-3 were 18.2, 40.5, 23.3 and 13.6, respectively.

CONCLUSIONCompounds 1-3 were isolated from this plant for the first time and compound 2 was a new compound. They showed significant antioxidant activity, and the scavenging activity of compound 3 was a little stronger than that of VitC.

Biphenyl Compounds ; metabolism ; Free Radical Scavengers ; chemistry ; pharmacology ; Glucosides ; chemistry ; pharmacology ; Nuclear Magnetic Resonance, Biomolecular ; Picrates ; metabolism ; Pyrones ; chemistry ; pharmacology ; Rhamnaceae ; chemistry

AIM: To study the chemical constituents and their bioactivity of Polygonum amplexicaule. METHODS: The isolation of compounds was achieved by chromatographic techniques and structure of the isolates was established by UV, IR, HRESI-MS and NMR including 1D and 2D experiments. RESULTS: Bioassay-guided fractionation of an ethanolic extract of Polygonum amplexicaule led to the isolation of a hitherto unidentified compound, 5, 6-dihydropyranobenzopyrone (1) along with nine previously known compounds (2-10). Compounds 2-10 were identified as amplexicine (2), catechin (3), rutin (4), quercetin-3-O-β-D-galactopyranoside (5), chlorogenic acid (6), galloyl glucose (7), caffeic acid (8), gallic acid (9) and scopletin (10). CONCLUSION Compound 1 is new. Compounds 1-10 exhibited considerable antioxidant activity in a 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging assay.
Antioxidants ; chemistry ; isolation & purification ; pharmacology ; Biphenyl Compounds ; metabolism ; Coumarins ; chemistry ; isolation & purification ; pharmacology ; Molecular Structure ; Picrates ; metabolism ; Plant Extracts ; chemistry ; pharmacology ; Polygonum ; chemistry

A549 Cells ; Apoptosis ; Biphenyl Compounds/pharmacology* ; Carcinoma, Non-Small-Cell Lung/pathology* ; Cell Line, Tumor ; Cell Proliferation ; Gefitinib/pharmacology* ; Humans ; Lignans/pharmacology* ; Lung Neoplasms/pathology*

OBJECTIVETo find a research method suitable to multi-component multi-index composition-activity relationship of traditional Chinese medicines (TCMs) with the antioxidant activity of four compatible active constituents of TCMs as the subject.

METHODLARS-based regression algorithm and comprehensive weight coefficient method were adopted to study in vitro clearance of DPPH and polyaromatic hydrocarbon with different doses of four compatible active constituents--total flavonoids of Glycyrrhizae Radix et Rhizoma (TFG), Ginkgo Folium extract (GBE), total flavonoids of Epimedii Folium (TFE) and astragaloside (AST) according to the comprehensive efficacy assessment procedures, that is test design, efficacy test and mathematical modeling (model verification).

RESULTLARS and comprehensive weight coefficient method was adopted to assess the optimal comprehensive efficacy of clearing DPPH and polyaromatic hydrocarbon. The results showed that the optimal dose combination of compatible constituents is TFG-GBE-TFE-AST 1: 0.2545: 0.007 6:0.011 5.

CONCLUSIONThe above compatibility of TCMs constituents can effectively clear polyaromatic hydrocarbon and DPPH with a good antioxidation. The uniform design adopted in this experiment, in combination of synthetic weight method, is suitable to the data analysis of "non-linear and small-sample" biotic experiment and the study on screening and assessment of compatibility of TCMs constituents.

Antioxidants ; chemistry ; pharmacology ; Biphenyl Compounds ; chemistry ; Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Medicine, Chinese Traditional ; methods ; Picrates ; chemistry ; Polycyclic Aromatic Hydrocarbons ; chemistry ; Regression Analysis

OBJECTIVETo explore the effect of irbesartan on angiotensin-converting enzyme 2 (ACE2) mRNA expression in diabetic rat myocardium.

METHODSThirty 8-week-old male Wistar rats were randomly divided into control group (n=7), diabetic model group (n=14) and irbesartan group (n=9). Diabetes was induced by a single intraperitoneal injection of STZ (55 mg/kg), a blood glucose>16.7 mmol/L 72 h after the injection indicated successful establishment of diabetes. Four weeks after the modeling, the rats in irbesartan group were given 50 mg/kg irbesartan. ELISA was used to measure myocardial AngII content in the rats, and myocardial ACE2 mRNA expression was determined by real-time PCR.

RESULTSMyocardial AngII level in the diabetic model group was significantly higher than that in the control group (P<0.001). Irbesartan administration significantly lowered cardiac AngII levels in the diabetic rats (P<0.001). The rats in irbesartan group showed significantly increased myocardial ACE2 mRNA expression compared with those in the control and diabetic rat groups (P<0.05).

CONCLUSIONIrbesartan can increase ACE2 mRNA expression in the myocardium, which might be one of the mechanisms underlying its effect in improving the cardiac function in diabetic rats.

Animals ; Biphenyl Compounds ; pharmacology ; Diabetes Mellitus, Experimental ; enzymology ; Male ; Myocardium ; enzymology ; Peptidyl-Dipeptidase A ; genetics ; metabolism ; RNA, Messenger ; genetics ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Tetrazoles ; pharmacology