A multi center real world observation to evaluate the efficacy of cryotherapy versus local hyperthermia for the treatment of plane warts.

Most plane warts are recalcitrant to treatment. Both cryotherapy and local hyperthermia have been applied to treat plane warts. However, no direct comparative study on their respective efficacy and safety has ever been performed. To assess the efficacy and safety of local hyperthermia at 43 ± 1°C versus liquid nitrogen cryotherapy for plane warts. Sequential patients with plane warts entered the study, either receiving cryotherapy or local hyperthermia therapy at the discretion of the patients and the recommendations of consultants. Cryotherapy with liquid nitrogen was delivered in two sessions 2 weeks apart, while local hyperthermia was delivered on three consecutive days, plus two similar treatments 10 ± 3 days later. The temperature over the treated skin surface was set at 43 ± 1°C for 30 min in each session. The primary outcome was the clearance rates of the lesions 6 months after treatment. Among the 194 participants enrolled, 183 were included in the analysis at 6 months. Local hyperthermia and cryotherapy achieved clearance rates of 35.56% (48/135) and 31.25% (15/48), respectively (p = 0.724); recurrence rates of 16.67% (8/48) and 53.33% (8/15) (p = 0.01); and adverse events rates of 20.74% (28/135) and 83.33% (40/48), respectively (p < 0.001). Cryotherapy had a higher pain score (p < 0.001) and a longer healing time (p < 0.001). Local hyperthermia at 43°C and cryotherapy had similar efficacy for plane warts. Local hyperthermia had a safer profile than cryotherapy but it required more treatment visits during a treatment course. More patients preferred local hyperthermia due to its treatment friendly nature.

Chinese Herbal Medicine Xingnaojing Injection for Acute Ischemic Stroke: An Overview of Systematic Reviews and Meta-Analyses.

Background: Xingnaojing injection (XNJ) is the only Chinese herbal injection approved for both intracerebral hemorrhage and ischemic stroke (IS) first-aid on ambulances in China; many systematic reviews (SRs) and meta-analyses (MAs) of XNJ on stroke have been published. The purpose of this research was to evaluate and summarize the current evidence on XNJ for IS. Methods: A comprehensive search was conducted for SRs and MAs of XNJ on IS in seven databases up to January 1, 2021. Two authors independently identified SRs and MAs, extracted data, assessed the quality of the included SRs and MAs using the Assessment of Multiple Systematic Reviews 2 (AMSTAR 2), and assessed quality of evidence using the Grading of Recommendations, Assessment, Development, and Evaluation (GRADE). Results: A total of 10 SRs met the inclusion criteria. The quality of included SRs using AMSTAR 2 was critically low as the critical items were poorly reported. Only 10% of SRs reported 50% of the 16 items, while the remaining 90% SRs reported just less than half of the items on AMSTAR 2. For GRADE, 7 (35%) of outcomes had low-quality evidence, 10 (50%) with very low, and 3 (15%) with moderate quality evidence. Very low to low quality of evidence indicated XNJ plus conventional therapy (CT) alleviated the neurological deficits of acute IS. Moderate-quality evidence showed XNJ plus CT reduced mortality when compared to Danshen injection plus CT, and very low-quality evidence showed XNJ plus CT could not improve the degree of coma, while low-quality evidence indicated the opposite. Mild adverse events in the CT group were less than those in the XNJ plus CT group, and there were no serious adverse events, but there was no statistical difference between the two groups. The included 10 SRs indicated that XNJ was used for acute IS, but only four SRs (40%) reported the course of disease. Conclusion: XNJ appears to be effective and safe for acute IS in improving the neurological deficits, but the evidence is not robust enough. However, whether administering XNJ immediately after or within 24 h of IS is best remains unknown due to the lack of data. Well-designed large-scale randomized controlled trials with measurable outcomes are required in future studies.

A global profiling strategy using comprehensive two-dimensional liquid chromatography coupled with dual-mass spectrometry platforms: Chemical analysis of a multi-herb Chinese medicine formula as a case study.

Although ultraviolet detector or mass spectrometer could be coupled with two-dimensional liquid chromatography (2DLC) to analyze complex constituents, full detection and identification of the compounds are difficult. Suffering from biased UV detection and insufficient MS data interpretation, a number of minor compounds are neglected though they are separated. In this study, we report a global chemical profiling strategy using comprehensive 2DLC coupled with dual-MS platforms, including Orbitrap-MS and QqQ-MS. It was exemplified by an 11-herb Chinese medicine formula Xiaoer-Feire-Kechuan (XFK). Firstly, constituents in XFK were separated on a CSH C18 × Phenyl-Hexyl 2DLC system with a practical peak capacity of 990.5 and an orthogonality of 90.3%. Secondly, untargeted mass spectral data was collected using dd-MS2 scan on an Orbitrap-MS. In total 542 peaks were detected, which was 4 times of that detected by 2DLC/UV (131 peaks). A total of 108 compounds were tentatively identified. Thirdly, targeted mass spectral data was collected for 8 characteristic substructures using neutral loss and precursor ion (NL/PRE) scan on a QqQ-MS. Extracted ion chromatogram was used to recognize minor constituents. An additional of 151 compounds were detected. Our study indicated that comprehensive 2DLC coupled with dd-MS2 and NL/PRE-MS is a powerful technique for the global profiling of multi-component systems.

[Acupuncture of intraorbital and extraorbital acupoints reduces apoptosis of retinal ganglion by down-regulating expression of Caspase-3 and ratio of Bax/Bcl-2 in rabbits with nonarteritis anterior ischemic optic neuropathy].

OBJECTIVE: To observe the effect of acupuncture of intraorbital and extraorbital acupoints on apoptosis and expression of Bax, Bcl-2 and Caspase-3 proteins of retinal ganglion tissue in rabbits with nonarteritis anterior ischemic optic neuropathy (NAION), so as to reveal its mechanism underlying improvement of NAION. METHODS: Female New Zealand rabbits were randomly divided into four groups: model, intraocular needling (ION), extraocular needling (EON), ION＋EON groups (n＝5 per group), and the 5 healthy eyes of those rabbits in the model group were selected to be used as the control group. The NAION model of the right eye was established by photodynamic stroke method. For ION group, acupoints "Jingming" (BL1), "Chengqi" (ST1) and "Qiuhou" (EX-HN7) were needled, and for EON group, "Cuanzhu" (BL2), "Yuyao" (EX-HN4) and "Qiaoming" (EX) were needled with filiform needles, followed by retaining the needles for 30 min. For ION＋EON group, the 6 acupoints were needled simutaneously. The treatment was conducted once daily for 3 days. The apoptosis of retinal ganglion tissue was detected by using TUNEL fluorescence labeling, and the expression of Bax, Bcl-2 and active Caspase-3 in the retinal ganglion were detected by immunohistochemistry. RESULTS: Following modeling and compared with the control group, the number of the apoptotic cells, and the expression levels of Bax and Caspase-3 proteins, as well as the ratio of Bax/Bcl-2 were significantly increased in the model group (P<0.01), while the expression of Bcl-2 was significantly decreased (P<0.01). After intervention, the number of the apoptotic cells in the ION, EON and ION＋EON groups, and the ratio of Bax/Bcl-2 in EON and ION＋EON groups, and the expression of Caspase-3 proteins in the ION and ION＋EON groups were significantly down-regulated (P<0.01, P<0.05), and the expression levels of Bcl-2 in both EON and ION＋EON groups were significantly up-regulated in comparison with the model group (P<0.01). No significant changes were found in the expression levels of Bax in the 3 needling groups relevant to the model group (P>0.05). CONCLUSION: Acupuncture of intraorbital and extraorbital acupoints can reduce apoptosis of retinal ganglion in NAION rabbits via inhibiting the activation of Caspase-3 protein and ratio of Bax/Bcl-2, and up-regulating the expression of Bcl-2 protein.

Fastigial nucleus electrostimulation promotes axonal regeneration after experimental stroke via cAMP/PKA pathway.

Axon regeneration after cerebral ischemia in mammals is inadequate to restore function, illustrating the need to design better strategies for improving outcomes. Improvement of axon regeneration has been achieved through fastigial nucleus electrostimulation (FNS) in animal researches. However, the mechanisms underlying this neuroprotection remain poorly understood. Increasing the levels of the second messenger cyclic AMP (cAMP) enhances axon regeneration, making it an excellent candidate molecule that has therapeutic potential. In the present study, we examined the expression of cAMP signaling in ischemic brain tissues following focal cerebral ischemia. Adult rats were subjected to ischemia induced by middle cerebral artery occlusion (MCAO). A dipolar electrode was placed into the cerebellum to stimulate the cerebellar fastigial nucleus for 1 h after ischemia. Neurological deficits and the expressions of cAMP, PKA (protein kinase A) and ROCK (Rho-kinase) were determined. Axonal regeneration was measured by upregulation of growth-associated protein 43 (GAP43). The data indicated that FNS significantly enhanced axonal regeneration and motor function recovery after cerebral ischemia. FNS also significantly increased cAMP and PKA levels after ischemic brain injury. All the beneficial effects of FNS were blocked by Rp-cAMP, an antagonist of PKA. Our research suggested that the axonal regeneration conferred by FNS was likely achieved via the regulation of cAMP/PKA pathway.

Simvastatin decreases hyperbaric oxygen-induced acute lung injury by upregulating eNOS.

Statins, which are 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase competitive inhibitors, not only lower blood cholesterol but also exert pleiotropic and beneficial effects in various diseases. However, the effects of statins on acute lung injury (ALI) induced by hyperbaric oxygen (HBO) have not been investigated. The present study is the first to investigate the effects of simvastatin in ALI induced by HBO in 8- to 9-wk-old C57BL/6 mice exposed to 0.23 MPa [=2.3 atmosphere absolute (ATA)] hyperoxia (≥95% O2) for 6 h. Mice were either given simvastatin (20 mg·kg·-1·day-1) in saline or a saline vehicle for 3 days before oxygen exposure. Lung tissue, serum, and bronchoalveolar lavage fluid (BALF) were collected for analysis of proapoptotic proteins, low-density lipoprotein cholesterol (LDL-C) levels, and lung inflammation. Simvastatin treatment significantly reduced lung permeability, serum LDL-C levels, tissue apoptosis, and inflammation. However, simvastatin treatment had no effect on antioxidant enzyme activity, nicotinamide adenine dinucleotide phosphate oxidase 4 (NADPH4) expression, and Akt phosphorylation levels. Furthermore, we investigated the role of endothelial nitric oxide synthase (eNOS) in simvastatin protection through inhibiting eNOS activity with NG-nitro-l-arginine methyl ester (l-NAME; 20 mg/kg). Results showed that the beneficial effects of simvastatin on ALI induced by HBO (antiinflammatory, antiapoptotic, lipid lowering, and reduction in lung permeability) were reversed. These results showed that simvastatin curbs HBO-induced lung edema, permeability, inflammation, and apoptosis via upregulating eNOS expression and that simvastatin could be an effective therapy to treat prolonged HBO exposure.

Differentially expressed genes in heads and tails of Angelica sinensis diels: Focusing on ferulic acid metabolism.

OBJECTIVE: To explore the scientific connotation of the discrepant pharmaceutical activities between the head and tail of Angelica sinensis diels (AS), an important herb extensively utilized in Chinese medicine, by the approach of transcriptome sequencing. METHODS: Ten samples of AS were randomly collected in Min County, Gansu Province of China. Transcriptome sequencing of AS was accomplished in a commercial ILLumina HiSeq-2000 platform. The transcriptome of each head and tail of AS were fixed in a gene chip, and detected under the procedure of Illumina HiSeq-2000. Differentially expressed unigenes between the heads and tails of AS were selected by Shanghai Biotechnology Corporation (SBC) online analysis system, based on Gene Ontology, Kyoto Encyclopedia of Genes and Genomes and relevant bioinformatic database. RESULTS: Totally 63,585 unigenes were obtained from AS by high-throughput sequencing platform. Among which 3359 unigenes were identified as differentially expressed unigenes between the heads and tails of AS by SBC analysis system scanning. Of which 15 differentially expressed unigenes participate in the metabolic regulation of phenylpropanoid biosynthesis (PB) pathway and ferulic acid metabolites, in response to the distinguished pharmaceutical actions of the heads and tails of AS. CONCLUSION: Different content of ferulic acid in the heads and tails of AS is related to the differentially expressed genes, particularly involved in the PB pathway.

A chemical profiling solution for Chinese medicine formulas using comprehensive and loop-based multiple heart-cutting two-dimensional liquid chromatography coupled with quadrupole time-of-flight mass spectrometry.

Chinese medicine formulas represent an excellent illustration for "complex matrix". The complexity lies in a big array of small molecules with high chemical diversity. The present paper describes a novel chemical profiling solution for complex matrix by combining comprehensive and multiple heart-cutting two-dimensional liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (2DLC/qTOF-MS). This solution includes method optimization, combinational separation, and structural characterization. It was exemplified by fully profiling the chemical constituents of a four-herb traditional Chinese medicine formula, Gegen-Qinlian Decoction (GQD). GQD was separated by a RP × RP (C18 × Phenyl-Hexyl) 2DLC system, and eluted with acidic × alkaline mobile phases with an optimized shift gradient elution program. In the comprehensive 2DLC mode, 280 peaks were detected, and 125 compounds were characterized within 42 minutes. The multiple heart-cutting (MHC) mode extended the (2)D modulation time to 3.0 min to effectively separate the minor compounds. The (1)D eluate within 4.4 min was loaded into eleven 40-µL loops. These fractions were successively separated by (2)D to resolve 13 additional compounds. The combination of comprehensive and MHC 2DLC/qTOF-MS provides a powerful technique for global chemical profiling of Chinese medicine formulas and other complex systems.

Novel daidzein analogs and their in vitro anti-influenza activities.

A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti-influenza activity, in vitro, against H1N1 Tamiflu-resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4-oxo-4H-1-benzopyran-8-carbaldehydes 11a-11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3-(4-Bromophenyl)-7-hydroxy-4-oxo-4H-1-benzopyran-8-carboxaldehyde (11c) displayed the best inhibitory activity (EC50 , 29.0 µM) and selectivity index (SI>10.3). Analysis of the structureactivity relationships (SAR) indicated that both the non-naturally-occurring Br-substituted B-ring and appropriate CHO and OH groups on the A-ring might be critical for the activity and selectivity against H1N1 TR influenza viruses.

Separation and detection of minor constituents in herbal medicines using a combination of heart-cutting and comprehensive two-dimensional liquid chromatography.

Herbal medicines contain a large number of minor constituents, which could contribute to their therapeutic effects and provide valuable lead compounds for drug discovery. However, to explore minor constituents from complicated herbal extracts is usually laborious and time-consuming. In order to discover minor novel herbal constituents efficiently, we combined heart-cutting and comprehensive two-dimensional liquid chromatography (HC-2DLC) to remove major components from herbal extracts, and then characterized the minor ones by mass spectrometry. This strategy was employed to analyze Pueraria lobata and Pueraria thomsonii, the roots of which are used as the Chinese herbal medicine Ge-Gen. Five major compounds in Ge-Gen extract were removed by on-line heart-cutting, and the minor compounds were separated on an RP×RP 2DLC system (1D, Acquity CSH C18, 2.1×100mm, 1.7µm; 2D, Poroshell Phenyl-Hexyl, 3.0×50mm, 2.7µm). A synchronized gradient elution program was used to improve chromatographic resolution of the second dimension. By using this 2DLC system, a total of 271 and 254 peaks were separated in P. lobata and P. thomsonii within 35min, respectively. The practical and effective peak capacity was 1593 and 677, respectively, and the orthogonality was around 70%. Structures of 12 selected compounds were tentatively characterized by mass spectrometry, and 9 of them were discovered from Ge-Gen for the first time. Contents of these minor compounds in Ge-Gen were preliminarily determined to be 0.01-0.1% (w/w). The HC-2DLC/MS system is a powerful and convenient tool to explore minor novel chemical constituents from complex herbal extracts.

Synthesis and anti-influenza activities of novel baicalein analogs.

A series of novel flavones derivatives were synthesized based on modification of the active ingredients of a traditional Chinese medicine Scutellaria baicalensis GEORGI and screened for anti-influenza activity. The synthetic baicalein (flavone) analogs, especially with the B-rings substituted with bromine atoms, were much more potent than oseltamivir or ribavirin against H1N1 Tamiflu-resistant (H1N1 TR) virus and usually with more favorable selectivity. The most promising were 5b, 5c, 6b and 6c, all displaying an 50% effective concentration (EC50) at around 4.0-4.5 µM, and a selective index (SI=50% cytotoxic concentration (CC50)/EC50)>70. For seasonal H3N2-infected influenza virus, both 5a and 5b with SI >17.3 indicated superior to ribavirin. The flavonoids having both not-naturally-occurring bromo-substituted B-rings and appropriate hydroxyls positioning on the A-rings might be critical in determining the activity and selectivity against H1N1-Tamiflu-resistant infected influenza viruses.

Discovery of non-glucoside SGLT2 inhibitors.

A series of benzothiazinone and benzooxazinone derivatives were discovered as SGLT2 inhibitors. The optimization led to the discovery of compounds 31 and 32, which exhibited similar potency and better SGLT1 selectivity compared to dapagliflozin. These compounds may provide novel promising scaffolds, which are different from phlorizin-based SGLT2 inhibitors.

[Soil respiration variations in winter wheat field in different previous crops and its influencing factors].

This study was to define the Variations of soil respiration, the response of influence factors to soil respiration and carbon sink in the total growing season, in winter wheat field of different previous crops. The results showed that: (1) as soil depth increases, the response of temperature to soil respiration rate also increased with a lag; (2) the soil respiration rate was quadric to soil moisture, phosphorus, potassium, soil urease activity, soil temperature, soil moisture as the main factors had an effect on soil respiration rate; soil temperature had the stronger effect on soil respiration rate when potassium had the weaker effect on soil respiration rate; (3) the average carbon emission rate in wheat filed of different previous crops showed as follow: Pepper of previous crops > celery of previous crops > corn of previous crops > eggplant of previous crops. The intensity of carbon "sink" displayed as follow: eggplant of previous crops > celery of previous crops > corn of previous crops > pepper of previous crops. As for the trials of this study, although the soil respiration rate is highest in the winter wheat filed of previous pepper, the amount of carbon fixed is the most. Its ratio of net primary productivity (NPP) and soil carbon release quantity was highest, so carbon sink was the strongest. If rotation planting was arranged according to the purpose of increasing carbon sink and reducing carbon emissions, pepper was relatively appropriate stubbles crop, followed by corn crop, celery and eggplant.

[Chemical constituents from bark of Caragana opulens].

OBJECTIVE: To investigate the chemical constituents of the bark of Caragana opulens. METHODS: The constituents of the CH3Cl-soluble portion in the 95% ethanol extract were isolated and purified by means of chromatography. The compounds were identified by their physical characteristics and spectral features. RESULTS: Eight compounds were isolated and identified as encelin(1), (+)-13-Hydroxyspathulenol(2), (+) -3alpha,9beta-aromaden dranediol(3), quercetin(4), penduletin(5), lupenol(6), Lup-20(29) -en-3-one (7), beta-sitosterol(8). CONCLUSION: Compounds 1, 2, 5, 7 are isolated for the first time from Caragana genus.

[ESR study and protection of water extract of Carthamus tinctorius on ox-LDL induced injury in rat cardiac microvascular endothelial cell].

OBJECTIVE: To observe the antioxidant effects of water extract of Carthamus tinctorius on ox-LDL induced injury in rat cardiac microvascular endothelial cell and detecting oxygen derived free radicals (OFR) to explore the antioxidant mechanisms. METHOD: By using the third generation of rat cardiac microvascular endothelial cells (rCMEC), the protection of water extract of C. tinctorius was investigated after ox-LDL (100 mg x L(-1) induced damage. The supernatant was collected for detecting lactate dehydrogenase (LDH), malondialdehyde (MDA), superoxide dismutase (SOD), xanthine oxidase (XOD), glutathione peroxidase (GSH-Px), nitric oxide (NO), nitric oxide synthase (NOS) activity, and cell suspension was collected for detecting reactive oxygen species (ROS) by electron spin resonance (ESR). RESULT: Water extract of C. tinctorius increased the rCMEC survival rate, reduced LDH, MDA and XOD levels, and improved SOD, GSH-Px and NOS activity, while in the cell suspension ROS signal decreased significantly. CONCLUSION: Water extract of C. tinctorius has antioxidation. The mechanisms are likely related with scavenging of free radicals, enhancing its clearance, enhancing endogenous antioxidant activity.

High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections.

The high mortality rate of immunocompromised patients with fungal infections and the limited availability of highly efficacious and safe agents demand the development of new antifungal therapeutics. To rapidly discover such agents, we developed a high-throughput synergy screening (HTSS) strategy for novel microbial natural products. Specifically, a microbial natural product library was screened for hits that synergize the effect of a low dosage of ketoconazole (KTC) that alone shows little detectable fungicidal activity. Through screening of approximately 20,000 microbial extracts, 12 hits were identified with broad-spectrum antifungal activity. Seven of them showed little cytotoxicity against human hepatoma cells. Fractionation of the active extracts revealed beauvericin (BEA) as the most potent component, because it dramatically synergized KTC activity against diverse fungal pathogens by a checkerboard assay. Significantly, in our immunocompromised mouse model, combinations of BEA (0.5 mg/kg) and KTC (0.5 mg/kg) prolonged survival of the host infected with Candida parapsilosis and reduced fungal colony counts in animal organs including kidneys, lungs, and brains. Such an effect was not achieved even with the high dose of 50 mg/kg KTC. These data support synergism between BEA and KTC and thereby a prospective strategy for antifungal therapy.

Antioxidative and anti-inflammatory activities of polyhydroxyflavonoids of Scutellaria baicalensis GEORGI.

The active ingredients of 'golden root' of Scutellaria baicalensis GEORGI (Huang-Qin), a valuable traditional Chinese medicine, are polyhydroxyflavonoids, namely baicalein, oroxylin A and wogonin. With the objective of overcoming their poor solubility and to investigate their structure and activity relationships, baicaleinyl 7-O-sulfate was prepared, and extensive comparative antioxidative and anti-inflammatory tests were conducted. All the polyhydroxyflavonoids exhibited significant antioxidative and free-radical scavenging activities. In respect of their nitric oxide (NO) inhibition, wogonin was superior to all the other flavonoids, while oroxylin A was most potent in the inhibition of lipid peroxidation. Wogonin proved to be the most potent (82.9% inhibition, p<0.05) in its anti-inflammatory activity against carrageenan-induced rat hind paw edema. There was a correlation between the in-vivo anti-inflammatory activity and the in-vitro antioxidative activities.

Synthesis of baicalein derivatives as potential anti-aggregatory and anti-inflammatory agents.

The direct acylation of trimethoxyphenol (1) with substituted cinnamoyl chlorides followed by Fries rearrangement and cyclization afforded a practical route for the synthesis of novel baicalein derivatives 4 functionalized on the B-ring in good overall yields. In the methylthiazoletetrazolium bromide (MTT) assay, none of the synthetic polyhydroxyflavonoids were cytotoxic at concentrations up to 200 microM on lipopolysaccharide (LPS)-activated murine RAW 264.7 macrophages over 24 h, while in the same cells they significantly inhibited NO production. Among the derivatives, 4d (IC50=46.1 +/- 0.3 microM) was found to exhibit the most potent activity compared with N-nitro-(L)-arginine methyl ester (L-NAME, IC50 >300 microM). Compounds 4b, 4e, 4f, 4h and 4i remarkably inhibited platelet aggregation induced by arachidonic acid and collagen in rabbit washed platelets compared with aspirin. Analysis of their structure-activity relationships indicated that, in the structural modification on the B-ring of baicalein (4a), introduction of appropriate electro-withdrawing substituents such as 2-Cl (4b), 4-Cl (4d), and 4-phenyl (4i) notably increased the potency on the inhibition of LPS-activated NO production and arachidonic acid- and collagen-induced aggregation. Baicalein itself was equally effective in the inhibition of LPS-activated NO production and collagen-induced aggregation but less active against arachidonic acid-induced aggregation. Our in-vitro results suggested that by appropriate structural modification of baicalein it may be possible to develop novel therapeutic agents against platelet-aggregation and inflammation.

Synthesis and radical scavenging of novel magnolol derivatives.

We have investigated the developdment of potential antioxidants based on magnolol, a naturally occurring biphenolic obtained from the bark of Magnolia officinalis. A series of aminomethylated derivatives of magnolol were synthesized under the aromatic Mannich reaction. In-vitro testing for diphenyl-p-picrylhydrazyl (DPPH) scavenging and chemiluminescence assays in whole cell models revealed that the pyrrolidyl-containing magnolols (2b (5,5'-diallyl-3-(pyrrolidin-1-ylmethyl)-biphenyl-2,2'-diol), 3a (5,5'-diallyl-3,3'-bis-(pyrrolidin-1-ylmethyl)-biphenyl-2,2'-diol) and 4c (5,5'-diallyl-3-(morphorin-4-ylmethyl)-3'-(pyrrolidin-1-ylmethyl)-biphenyl-2,2'-diol)) displayed promising free radical scavenging effects as compared with magnolol. The results from compound 4c indicated that the naturally occurring component was suitable to be a lead compound toward promising antioxidants.