Standardized Herbal Extract Research Articles

Phytosomes:An Overview

Phytosome is a patented technology that incorporates standardized plant extracts into phospholipids to create lipid-soluble molecular complexes with improved bioavailability and absorption. These phyto-constituents are increasingly important due to their nutritional and medicinal properties, but their bioavailability remains poor. Phytosome drug delivery is a method developed to enhance their bioavailability and is compatible in-vivo. Preparation methods are easy and can be characterized using techniques like FTIR, PXRD, DSC, SEM, TEM, and HNMR. Phytosomes can be used to augment the bioavailability of plant constituents and treat incurable diseases with less side effects. Phytosomes are formed by reacting a stoichiometric amount of phospholipid with standardized herbal extract or polyphenolic constituents in an aprotic solvent. Phosphatidylcholine molecules in phytosomes have hepatoprotective activity and nutritional value. In this article, we are going to keep an eye on Phytosomes Overview.

Molecular Mechanism of DLBS3233 Bioactive Fraction in Type-2 Diabetes Mellitus: Network Pharmacology and Docking Study

Although several antidiabetic agents are currently available, they commonly have undesirable effects and are not fully effective in reducing blood glucose. Therefore, since a long time ago, some Indonesians have preferred herbal medicine to cure and prevent diseases such as Lagerstroemia speciosa (L.) Pers. and Cinnamomum burmanni. (Nees & T.Nees) Blume, plants from Indonesia, are believed to be able to treat type 2 diabetes mellitus (T2DM). Both herbs are present in DLBS3233 bioactive fraction, a standardized herbal extract that acts as an insulin sensitizer like thiazolidinediones (TZDs). However, the molecular mechanisms, the bioactive compounds, and the target proteins involved remain unclear. To understand more about the potential molecular mechanism of DLBS3233 in treating T2DM, this network pharmacology study is conducted for the first time. Quercetin, kaempferol, and ellagic acid were discovered to have antidiabetic effects in this study as selected compounds of DLBS3233, primarily on eight core target proteins, including AKT1, EGFR, GSK3B, IL6, PTK2, RELA, SRC, and VEGFA. We also found that they exhibited ligand-receptor binding activity comparable to pioglitazone in the molecular docking study. Concisely, as a reference for furthering the development of this bioactive fraction, this study provides novel information on DLBS3233 in T2DM treatment that was not shown in prior studies.

Multi-wavelength fusion spectral extraction-assisted HPLC for simultaneous quantification of multiple secondary metabolites in herbal matrices

AbstractThe existing HPLC methods for the assaying of multiple markers in standardized herbal extracts use a single wavelength for quantification, which usually leads to lower assay than actual claims. It was because screening multiple phytochemical standards irrespective to their absorption maxima which drive decrease in peak are response which ultimately impact the assay. To overcome this issue, we have applied a methodology, called Mixed Standard Multi-Signal (MSMS) simultaneous detection, where multiple reference standards get extracted each with their respective λmax and quantification will be done at the same λmax in a single sequence data setup. This method was standardized using Single Signal Multi-Standards, Single Signal Single Standard, Multi-Signal Single Standard, for all individual reference standards, mixed reference standards, plant extracts, and Ayurvedic formulations. The results of our study demonstrate that higher assay reported total actives 5.04% by conventional detection and for current proposed method 13.81% with shorter span of analysis time and lesser solvent consumption. It helps to decide the actual standardization label claim on product which drives better commercial costings, and dosage regimen claims. Graphical Abstract

Evaluating the Aphrodisiac Potential of Mirabilis jalapa L. Root Extract: Phytochemical Profiling and In Silico, In Vitro, and In Vivo Assessments in Normal Male Rats.

The traditional use of Mirabilis jalapa L. roots to enhance male sexual performance prompted us to assess the in silico, in vitro, and in vivo aphrodisiac activities of its hydroethanolic extract using normal male rats. Spectroscopic characterization indicated the presence of ß-D-glucopyranoside, methyl-1,9-benzyl-2,6-dichloro-9H-purine, and Bis-(2-ethylhexyl)-phthalate; these compounds have a significant inhibitory effect on the phosphodiesterase-5 (PDE-5) enzyme in silico evaluation and minerals (including zinc, cadmium, and magnesium). Other phytochemical analyses revealed the presence of phenolic compounds and flavonoids. These phytochemicals and minerals may contribute to the aphrodisiac activities of the extract. Additionally, the in vivo study revealed that the administration of M. jalapa root extract (300 mg/kg) significantly enhanced (p < 0.01, p < 0.03) mount, intromission, and ejaculation frequencies while significantly (p < 0.05) decreasing the mount and intromission latencies, as well as the post-ejaculatory interval time, in comparison with the standard drugs sildenafil and ginseng, resulting in enhanced erection and sexual performance in the rats. Furthermore, the extract significantly (p < 0.05) increased penile reflexes and also elevated the levels of testosterone and luteinizing hormones. Extract (300 mg/kg) significantly (p < 0.05) inhibited the PDE-5 enzyme in an in vitro study. Concludingly, the comprehensive findings of this study suggest that a standardized herbal extract derived from M. jalapa roots alleviates erectile dysfunction and premature ejaculation in male rats. M. jalapa root extract proved to be an alternative treatment for erectile dysfunction and premature ejaculation.

Saw Palmetto may fight prostate cancer.

Saw Palmetto may fight prostate cancer.

Ocular Formulation Development of a Standardized Herbal Extract for the Prevention and Treatment of Diabetic Cataract

Diabetes-induced Cataract is a major concern regarding the cause of blindness in developed and developing countries. Recent basic research studies have emphasized the role of the polyol pathway in the initiation of the disease process. Diabetes induced cataract is also referred to as “Diabetic cataract”. Demographic studies have certainly enhanced our knowledge concerning an association between diabetes and cataract formation and have defined the risk factors for the development of cataracts. Diabetic patients also have a higher risk of complications after phacoemulsification cataract surgery as compared to non-diabetic people. Aldose-reductase inhibitors and antioxidants have been proven beneficial in the prevention or treatment of this sight-threatening condition in in vitro experimental studies. Aldose reductase inhibitors have a vital importance in the treatment and prevention of diabetic complications. Nowadays, use of natural, herbal, and naturopathic medications has increased, as they have more therapeutic potential and lesser side effects as compared to the allopathic and ayurvedic medications. This research work provides an insight into herbal standardized extract and its ocular formulation development, Eyedrop, as an easy, sterile, safe, and alternative to phacoemulsification. Development of eyedrop as an ocular formulation and its standardization with an in vitro evaluation of the herbal extract for the prevention as well as treatment of Diabetic cataract.

Hypericum oblongifolium Choisy: A Pharmacognostic Review

Many herbal remedies have been employed in various medical system for treatment and management of different diseases. Medicinal plants and their investigation towards the phytoconstituents is much interested in today’s research. Herbal medicine is the use of medicinal plants for prevention and treatment of diseases: it ranges from traditional and popular medicines of every country to the use of standardized and tritated herbal extracts. Generally cultural rootedness enduring and widespread use in a Traditional Medical System may indicate safety, but not efficacy of treatments, especially in herbal medicine where tradition is almost completely based on remedies containing active principles at very low and ultra low concentrations, or relying on magical-energetic principles. Here, the aim of this study is to evaluate the Pharmacognostic parameters and identify the Phytoconstituents. Hypericum oblongifolium (family:- Guttiferae) is a well known in India and is one of the most versatile medicinal plants having a wide spectrum of biological activity.It is a highly useful and traditionally used medicinal herbaceous plant which is found in tropical and subtropical areas of the world. The genus Hypericum consists of about 400 species with widespread medicinal applications in a variety of health disorders.

Redox Behavior and Radical Scavenging Capacity of Hepatoprotective Nutraceutical Preparations

Background: Over-the-counter hepatoprotective nutraceuticals are highly commercialized preparations worldwide. However, their alleged antioxidant capacity and health benefits are still not fully understood. Objective: This work showcased the first investigation of the redox behavior of hepatoprotective nutraceuticals by spectrophotometric and electrochemical approaches. Methods: The samples were segregated into two groups, namely: A, B, and C based on isolated compounds (IC); and D, E and F based on standardized herbal extracts (SHE). Results: Results evidenced that IC showcase similar response and distinctions could be attributed to varying concentrations of choline. In SHE, the slopes showcased superimposition due to the presence of Peumus boldus. The electrochemical assays showcased that samples A and C exhibited a single anodic peak at Ep1a ≈ +0.7 V, which could be attributed to the oxidation of methionine; while samples D, E and F, showcased two anodic peaks at Ep1a ≈ +0.35V and Ep2a ≈ +0.7 V, suggesting the oxidation of phenolic and amine moieties respectively. Furthermore, the first two principal components explained 84.8% of all variance in the model, thereby suggesting statistical reproducibility. Conclusion: This work showcased the first investigation of the redox behavior of hepatoprotective nutraceuticals, thereby shedding light on their antioxidant capacity and physical-chemistry.

Antioxidant and reduced skin-ageing effects of a polyphenol-enriched dietary supplement in response to air pollution: a randomized, double-blind, placebo-controlled study.

BackgroundAir pollution exposure is one of the major threats to skin health and accelerates skin ageing mainly through oxidative stress mechanisms. Since it is difficult to minimize skin exposure to air pollutants, especially in urban areas, strategies to protect the skin are needed. Plant phenolic compounds have been found to be effective in attenuating cellular oxidative stress and inflammation induced by different air pollutants and a dietary approach based on these compounds could provide an efficient protection measure.ObjectiveHere we investigated the efficacy of a commercially available polyphenol-enriched dietary supplement (Zeropollution®) in reducing pollution-induced oxidative stress and in improving different skin parameters related to skin ageing of Caucasian and Asian subjects exposed to air pollution. Zeropollution is composed of four standardized herbal extracts: Olea europaea leaf, Lippia citriodora, Rosmarinus officinalis, and Sophora japonica.DesignA double-blind randomized, parallel group study was carried out on 100 outdoor workers living in a polluted urban European area (Milan) to assess the efficacy of the dietary supplement. The total antioxidant capacity on saliva (FRAP), the oxidative damage on skin (lipoperoxides content), skin moisturization (corneometer), transepidermal water loss (tewameter), skin radiance and colour (spectrophotometer), skin elasticity (cutometer), skin sebum content (sebumeter), and the skin roughness (image analysis) were measured.ResultsBoth inter-group and intra-group analysis proved that the dietary supplement improved all clinical and biochemical-monitored parameters, in both Caucasian and Asian individuals. Some of the positive effects such as decreased wrinkle depth, increased elasticity and firmness, improved skin moisturization and transepidermal water loss, and reduced dark spots pigmentation were statistically significant as early as 2 weeks of product consumption.ConclusionsThe results of the study indicate reduced oxidative stress-induced skin damage in both Asian and Caucasian women living in a polluted urban area. Therefore, the oral intake of this four-plant based supplement could be considered a complementary nutrition strategy to avoid the negative effects of environmental pollution exposure.

In Vitro Anti Tubercular Activity and Physicochemical Standardization of Selected Medicinal Plant Extracts

Globally tuberculosis is a major health problem. The main question with the current tuberculosis treatment is adverse effects and drug resistance. The present study aimed to identify safe and effective alternative herbal drugs for the treatment of tuberculosis. This study involves the standardization of selected medicinal plant extracts and in vitro antitubercular activity. Based on the literature survey, four medicinal plant extracts were selected i.e. Glycyrrhiza glabra (Yastimadhu), Piper longum (Pippali), Curcuma longa (Haridra) and Adhatoda vasica (Vasaka). To evaluate the authenticity and quality control aspect, chromatographic fingerprinting and physicochemical analysis were carried out. Quantification of phytomarkers was analyzed by High performance liquid chromatography and in vitro anti-mycobacterial activity was performed by agar well diffusion method on Mycobacterium smegmatis. All necessary physicochemical parameters were performed and found to comply with specified limits. Extracts were authenticated by qualitative High-performance thin layer chromatography fingerprinting in comparison with suitable raw herbs and phytomarkers. Quantification by High performance liquid chromatography showed that Glycyrrhiza glabra contains 10 % Glycyrrhizin, Piper longum contains 7 % Piperine, Curcuma longa contains 82.41 % Curcumin and Adhatoda vasica contains 2.3 % Vasicine. In vitro activity of Glycyrrhiza glabra, Piper longum and Curcuma longa showed 20 mm, 16 mm and 14 mm of maximum Zone of inhibition respectively. Adhatoda vasica did not show any activity against Mycobacterium smegmatis. The present study demonstrates that the selected plant extracts have the potential to inhibit mycobacterial growth. Thus, these standardized herbal extracts could be used in the design and development of a polyherbal formulation for the treatment of primary stage tuberculosis.

Evaluation of Antioxidant Interactions in Combined Standardized Extracts of Tinospora Cordifolia (Willd), Terminalia Arjuna (Roxb) and Ocimum Sanctum (LINN)

Generation of reactive oxygen species ROS occurs in the normal cell during metabolism in animals. Over production of ROS in the animals causes oxidative stress that leads to oxidative DNA damage which is implicated in the pathogenesis of numerous diseases. Since antioxidant mechanism plays vital role in the pharmacotherapy of different disorders the present investigation aims to check the synergisticantagonistic antioxidant effects of standardised extracts of Tinospora cordifolia Willd TCE Terminalia arjuna Roxb TAE Ocimum sanctum Linn OSE in combinations by DPPH Scavenging Activity hydroxyl radical scavenging activity reducing power assay. In all the methods the extract combinations exhibited good scavenging activity. Reaction of combination of standardized extracts with 22 Diphenyl -1-picryl hydrazyl DPPH radicals showed better scavenging activity compared to individual extracts. The IC50 values for TCETAE TCEOSE TAEOSE were found to be 74.12 microg ml 78.62 microg ml and 71.70 microg ml respectively. The IC50 values for hydroxyl radical scavenging activity of different herb combinations viz. TCETAE TCEOSE TAEOSE were found to be 320.28 microgml 340 microgml and 261 microgml respectively. Further the standardized herb combinations showed more effective reductive ability when compared to that of individual standardized herbal extract. Hence it may be concluded that standardized extracts containing potent antioxidant constituents like phenolics flavonoids triterpenoids alkaloids steroids tannins showed synergistic antioxidant activity.nbsp

PM014 attenuates radiation-induced pulmonary fibrosis via regulating NF-kB and TGF-b1/NOX4 pathways

Radiation therapy is the mainstay in the treatment of lung cancer, and lung fibrosis is a radiotherapy-related major side effect that can seriously reduce patient’s quality of life. Nevertheless, effective strategies for protecting against radiation therapy-induced fibrosis have not been developed. Hence, we investigated the radioprotective effects and the underlying mechanism of the standardized herbal extract PM014 on radiation-induced lung fibrosis. Ablative radiation dose of 75 Gy was focally delivered to the left lung of mice. We evaluated the effects of PM014 on radiation-induced lung fibrosis in vivo and in an in vitro model. Lung volume and functional changes were evaluated using the micro-CT and flexiVent system. Fibrosis-related molecules were evaluated by immunohistochemistry, western blot, and real-time PCR. A orthotopic lung tumour mouse model was established using LLC1 cells. Irradiated mice treated with PM014 showed a significant improvement in collagen deposition, normal lung volume, and functional lung parameters, and these therapeutic effects were better than those of amifostine. PM104 attenuated radiation-induced increases in NF-κB activity and inhibited radiation-induced p65 translocation, ROS production, DNA damage, and epithelial-mesenchymal transition. PM104 effectively alleviated fibrosis in an irradiated orthotopic mouse lung tumour model while not attenuating the efficacy of the radiation therapy by reduction of the tumour. Standardized herbal extract PM014 may be a potential therapeutic agent that is able to increase the efficacy of radiotherapy by alleviating radiation-induced lung fibrosis.

Discovery of bioactive drug candidates from some Turkish medicinal plants-neuroprotective potential of Iris pseudacorus L.

Abstract Medicinal plants have an enormous potential for producing bioactive compounds of great benefit to mankind. There is a great scope for new drug candidates based on traditional medicinal plants throughout the world. The number of drugs derived from medicinal plants that are recently introduced into clinical use is increasing. Besides, numerous of standardized herbal extracts were also approved as phytomedicines by the health authorities to be used in phytotherapy. The drug discovery program from nature in our laboratory involves several steps from plant collection, extraction, HTS of the extracts by using in vitro enzyme inhibitory tests, bioassay-guided fractionation through the isolation and structure elucidation of bioactive compounds. Continuing our researches in the field of anticholinesterase activity, neuroprotective potential of Iris pseudacorus L. have presented in this article.

A REVIEW ON FORMULATION AND CHARACTERIZATION OF HERBOSOME COMPLEX

The major amount of active constituents comprises in herbal drugs with excellent bioactivity in vitro but less in vivo because of their poor lipid solubility and improper size of the molecules. This results in poor absorption and bioavailability of active constituents from the herbal extract. Herbosome technology enhances the bioavailability of herbal extracts. Herbosome act as the bridge between the novel delivery system and conventional delivery system. It is a complex of natural active ingredients and phospholipids (phosphatidylcholine, phosphatidylserine etc.) which increases absorption of herbal extract. Herbosome is the novel emerging technique applied to phytopharmaceuticals for the enhancement of bioavailability of herbal extract for medicinal applications. This article overviews about herbosome technology, recent advance, their application for various standardized herbal extracts and aims to provide complete scientific information, characterization about herbosomes as a promising drug delivery system.

A standardized herbal extract PM014 ameliorates pulmonary fibrosis by suppressing the TGF-\u03b21 pathway

Idiopathic pulmonary fibrosis (IPF) is a devastating and common chronic lung disease pathologically characterized by loss of epithelial cells and activation of fibroblasts and myofibroblasts. The etiology of IPF remains unclear and the disease pathology is poorly understood with no known efficacious therapy. PM014 is an herbal extract that has been shown to have beneficial effects in pulmonary diseases, which are likely to exert anti-inflammatory bioactions. In the present study, we observed that bleomycin (BLM) caused increased inflammatory infiltration as well as collagen deposition in lungs of mice on day 14 after treatment. Administration of PM014 suppressed BLM-induced inflammatory responses and fibrotic changes in dose-dependent manner in mice. Additionally, we provided in vitro evidence suggesting that PM014 inhibited TGF-β1-induced epithelial-mesenchymal transition (EMT) and fibroblast activation in alveolar epithelial cells and human lung fibroblasts from healthy donor and IPF patients. PM014 appeared to target TGF-β1 signaling via Smad-dependent pathways and p38 mitogen-activated protein kinases (MAPKs) pathways. Taken together, our data suggest that PM014 administration exerts a protective effect against lung fibrosis and highlight PM014 as a viable treatment option that may bring benefits to patient with IPF.

Evaluation of Herb-Drug Interaction of Synacinn™ and Individual Biomarker through Cytochrome 450 Inhibition Assay.

SynacinnTM contains five standardized herbal extracts of Orthosiphon Stamineus (OS), Syzygium polyanthum (SZ), Curcuma xantorrizza (CX), Cinnamomum zeylanicum (CZ) and Andrographis paniculata (AP) and is standardized against phytochemical markers of rosmarinic acid, gallic acid, curcumin, catechin and andrographolide respectively. This herbal medicine has been used as health supplement for diabetes. SynacinnTM is recommended to be consumed as supplement to the diabetic drugs. However, herb-drug interaction of SynacinnTM polyherbal with present drugs is unknown. This study was designed to investigate the effect of SynacinnTM and its individual biomarkers on drug metabolizing enzymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam), CYP3A4 (Testosteron)), to assess its herb-drug interaction potential through cytochrome P450 inhibition assay. This study was conducted using liquid chromatography- tandem mass spectroscopy (LC-MS/MS) using probe substrates using human liver microsomes against CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam) and CYP3A4 (Testosteron). Result showed that SynacinnTM at maximum concentration (5000 µg/ml) 100% inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam) and CYP3A4 (Testosteron). IC50 values determined were 0.23, 0.60, 0.47, 0.78, 1.23, 0.99, 1.01, and 0.91 mg/ml for CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4 (midazolam) and 3A4 (testosterone), respectively. Meanwhile, all individual biomarkers showed no, less or moderate inhibitory effect towards all the tested CYP450 except for curcumin that showed inhibition of CYP2C8 (91%), CYP2C9 (81%) and CYP2C19 (72%) at 10µM. Curcumin was found to be an active constituent that might contribute to the inhibition of SynacinnTM against CYP2C8, CYP2C9 and CYP2C19. It can be suggested that SynacinnTM can be consumed separately from a drug known to be metabolized by all tested CYP450 enzymes.

A Chinese herbal decoction, Jian-Pi-Yi-Shen, regulates the expressions of erythropoietin and pro-inflammatory cytokines in cultured cells

BackgroundA Chinese herbal formula, namely Jian-Pi-Yi-Shen (JPYS), has been clinically prescribed for patients with chronic kidney disease associated-anemia, and which can improve the patient’s immunological system. However, the mechanisms of JPYS involved in anemia and immune response have not been investigated. To study the role of JPYS in regulating hematopoietic and immunological functions, we investigated its activities on the expressions of erythropoietin and pro-inflammatory cytokines in cultured cells.MethodsThe standardized herbal extracts of JPYS (0–30 μg/ml) were applied onto cultured cells for 24–48 h. Total RNA was collected from the treated cells and subjected to real-time quantitative PCR analysis. Cultured HEK293T cells, transfected with a construct composed of hypoxia response element tagged with a luciferase gene, i.e. pHRE-Luc, were treated with JPYS extracts (1–30 μg/ml) for 24 h. The cell lysates were subjected to luciferase assay.ResultsThe treatment with JPYS extract onto cultured HEK293T cells induced erythropoietin expression in a dose-dependent manner, having the highest response by ~ 50% of increase. In parallel, application of JPYS extract for 24 h stimulated expressions of interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α in cultured RAW 264.7 macrophages. In contrast, the pretreatment with JPYS extract suppressed expressions of IL-1β, IL-6, and TNF-α in lipopolysaccharide-induced macrophages.ConclusionsThese results confirmed the hematopoietic function of JPYS in regulating erythropoietin expression, as well as the bidirectional immune-modulatory roles of JPYS by regulating the expression of pro-inflammatory cytokines in cultures.

Prevention of Prostate Tumor Development by Stimulation of Antitumor Immunity Using a Standardized Herbal Extract (Deep Immune®) in TRAMP Mice.

Low-risk prostate cancer (PCa) does not require immediate treatment, but PCa progression after years of active surveillance will need the treatment. This study was to test the efficacy of immunostimulant Deep Immune (DI) in controlling PCa progression. DI is an extract of eight different medicinal herbs. In vitro activity of DI was determined by phagocytosis activation using flow cytometric analysis of fluorescence-labeled latex bead uptake, expression of immune-modulating 84 genes using PCRarray, and tumor killing using coculturing with immune cells. Anti-PCa activity of DI in vivo was examined in male TRAMP mice. In vitro DI stimulated phagocytosis and expression of a panel of inflammatory mediators (C4b, CXCL3, lymphotoxin, NOS2, TLR1, TNF, and TNFSF14) in cultured macrophages and increased tumor killing of both macrophages and TRAMP mouse splenocytes. Daily intake of this herbal product significantly suppressed the tumor size (P = 0.0368) with lower histopathologic scores (P = 0.0364) in TRAMP mice, which were associated with an increase in both splenocyte cytotoxicity against tumor cells and numbers of CD8 T cells, macrophages, and dendritic cells in the spleens in vivo. In conclusion, daily intake of DI prevents PCa progression in TRAMP mice, suggesting the possible effectiveness of the immunostimulant herbal products on prevention of PCa progression after diagnosis of low-risk PCa.

A Chinese Herbal Preparation, Xiao-Er-An-Shen Decoction, Exerts Neuron Protection by Modulation of Differentiation and Antioxidant Activity in Cultured PC12 Cells.

Xiao-Er-An-Shen Decoction (XEASD), a Chinese herbal formula, has been used in clinic for treating insomnia and mental excitement in children and adolescents. However, less of scientific data supports its effectiveness in clinic. Here, we aim to study the role of XEASD in regulating neuron differentiation and antioxidant activity. An HPLC-MS was used to chemically standardize herbal extract of XEASD. The standardized herbal extracts of XEASD (0.3–3.0 mg/mL) were applied onto cultured PC12 cells for 48 hours. The treatment with XEASD extract induced neurite outgrowth of PC12 cells in a dose-dependent manner, having the highest response by ~50% of differentiated cells. Application of XEASD extract dose dependently stimulated expressions of NF68, NF160, and NF200 in cultured PC12 cells. Furthermore, XEASD activated the phosphorylation of cAMP responsive element binding protein on PC12 cells, the effect of which was blocked by H89, a protein kinase A inhibitor. Moreover, XEASD showed free radical scavenging activity and stimulated the transcriptional activity of ARE. These results supported the neurobeneficial effects of XEASD in the induction of neurite outgrowth and protection against oxidative stress and could be useful for neurological diseases, in which neurotrophin deficiency and oxidation insult are involved.

A standardized herbal extract mitigates tumor inflammation and augments chemotherapy effect of docetaxel in prostate cancer

Activation of the NFκB pathway is often associated with advanced cancer and has thus been regarded as a rational therapeutic target. Wedelia chinensis is rich in luteolin, apigenin, and wedelolactone that act synergistically to suppress androgen receptor activity in prostate cancer. Interestingly, our evaluation of a standardized Wedelia chinensis herbal extract (WCE) concluded its efficacy on hormone-refractory prostate cancer through systemic mechanisms. Oral administration of WCE significantly attenuated tumor growth and metastasis in orthotopic PC-3 and DU145 xenografts. Genome-wide transcriptome analysis of these tumors revealed that WCE suppressed the expression of IKKα/β phosphorylation and downstream cytokines/chemokines, e.g., IL6, CXCL1, and CXCL8. Through restraining the cytokines expression, WCE reduced tumor-elicited infiltration of myeloid-derived suppressor cells (MDSCs), tumor-associated macrophages (TAMs) and endothelial cells into the tumors, therefore inhibiting angiogenesis, tumor growth, and metastasis. In MDSCs, WCE also reduced STAT3 activation, downregulated S100A8 expression and prevented their expansion. Use of WCE in combination with docetaxel significantly suppressed docetaxel-induced NFκB activation, boosted the therapeutic effect and reduced the systemic toxicity caused by docetaxel monotherapy. These data suggest that a standardized preparation of Wedelia chinensis extract improved prostate cancer therapy through immunomodulation and has potential application as an adjuvant agent for castration-resistant prostate cancer.