Elucidating the anti-obesity potential of bioactive fractions of kalanchoe pinnata (lam.) leaves extract using a combination of in vitro, in vivo and in silico methods along with characterisation of lead compounds through an HPTLC ms-MSn analytical study.

Fractions were isolated from the leaves extract of Kalanchoe pinnata and subjected to scrutiny for their prospective anti-obesity properties. An array of preliminary phytochemical, invitro antioxidant, and enzyme inhibition assays were executed, which discerned fractions F1 and F2 as the most effective fractions. These fractions were subsequently studied through invivo experiments, affirming that F2 as the most potent fraction. Further characterisation of F2 was conducted via HPTLC-Mass spectrometry (MS-MSn) techniques. The outcomes demonstrated that F2 produced a notable anti-obesity effect in obese mice, reducing their body weight and lipid metrics, and leading to advantageous changes in their organs. An analytical examination of F2 revealed the existence of four principal compounds, which were subsequently subjected to insilico molecular docking and dynamic analysis, confirming their aptitude for binding to selected proteins. These findings imply that the utilisation of Kalanchoe pinnata leaves could provide a promising therapeutic strategy for the treatment of obesity.

Active fractions from Jingfang Baidu Powder alleviate Klebsiella-induced Pneumonia by inhibiting TLR4/Myd88-ERK signaling pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: Jingfang Baidu Powder (JFBDP) is a classic traditional Chinese medicine prescription. Although Jingfang Baidu powder obtained a general consensus on clinical efficacy in treating pneumonia, there were many Chinese herbal drugs in formula, complex components, and large oral dosage, which brings certain obstacles to clinical application. AIM OF THE STUDY: Therefore, screening of the active fraction that exerts anti-pneumonia helps improve the pharmaceutical preparation, improve the treatment compliance of patients, and further contribute to the clinical application, and the screening of the new active ingredients with anti-pneumonia. The histopathological observation, real-time quantitative PCR, western blotting, and immunofluorescence were applied to evaluate the anti-pneumonia efficacy of active fractions from JFBDP. RESULTS: Three fractions from JFBDP inhibit the gene expression of IL-1ß, IL-10, CCL3, CCL5, and CCL22 in lung tissue infected by Klebsiella at various degrees, and presented a good dose-response relationship. JF50 showed stronger anti-inflammatory effects among three fractions including JF30, JF50, and JF75. Besides, JF50 significantly reduced the protein expression of TLR4 and Myd88 in lung tissue infected with Klebsiella, and it also significantly inhibited p-ERK and p-NF-κB p65. JF50 significantly inhibits the protein expression of Caspase 3, Caspase 8, and Caspase 9 in lung tissue infected with Klebsiella at the dose of 25 mg/kg and 50 mg/kg. CONCLUSION: JF50 improves lung pathological damage in Klebsiella pneumonia mice by inhibiting the TLR4/Myd88/NF-κB-ERK signaling pathway, and inhibiting apoptosis of lung tissue cells. These findings provide a reference for further exploring the active substance basis of Jingfang Baidu Powder in treating bacterial pneumonia.

Leaf Extract and Active Fractions of Dillenia pentagyna Roxb. Reduce In Vitro Human Cancer Cell Migration Via NF-κB Pathway.

BACKGROUND: Different parts of Dillenia pentagyna have long been used in traditional medicines to cure several diseases including cancer. However, the mechanism(s) of anti-cancer effects are still unknown. We aimed to elucidate the anti-metastatic potential of ethanolic extracts of leaves of D. pentagyna (EELDP) and active fractions of it in highly metastatic human cancer cells. METHODS: We screened different HPLC fractions of EELDP based on their anti-metastatic effect. We used TLC and ESI-MS for determining the presence of various phytochemicals in EELDP and fractions. We monitored in vitro anti-metastasis effect of EELDP (0-0.6 mg/ml) and active fractions (0-0.050 mg/ml) on various human cancer cells like A549, HeLa, and U2OS. RESULTS: EELDP significantly reduced cell viability and cell migration in A549, HeLa, and U2OS cells. However, higher sensitivity was observed in A549 cells. We screened 2 active HPLC fractions F6 and F8 having anti-MMPs activity. EELDP and active fractions reduced metastasis via the NF-κB pathway, decreased the expression of Vimentin, N-cadherin, and increased the expression of Claudin-1. CONCLUSION: Significant reduction of metastasis by EELDP at a dose of 0.1 mg/ml or by active fractions at 0.050 mg/ml implicates that the active compound(s) present in crude or fractions are extremely potent to control highly metastatic cancer.

Immunological regulation of the active fraction from Polygonatum sibiricum F. Delaroche based on improvement of intestinal microflora and activation of RAW264.7 cells.

ETHNOPHARMACOLOGICAL RELEVANCE: Polygonatum sibiricum, known as "Huangjing" in Chinese traditional medicine, of which functions include invigorating Qi and nourishing Yin, tonifying spleen and kidney, which are considered to replenish energy, and strengthen immunity. However, both the active components and mechanism of the immune-enhancing effect of Polygonatum sibiricum have not been clarified. AIM OF THE STUDY: To evaluate the immunoregulation effects of PSE30 (Polygonatum sibiricum ethanol 30) and PSE75 (Polygonatum sibiricum ethanol 75). The gut microbial and activation of RAW264.7 cells were also evaluated for exploring the mechanism of PSE75. MATERIALS AND METHODS: Female ICR mice were randomly divided into different groups, which were pretreated with 0.9% saline, Yupingfeng granules, different dosage of PSE30 or PSE75. And the immunosuppressed mice model was constructed using cyclophosphamide. And the total duration of the experiment was 15 d. After that, the serum Immunoglobulins G (IgG) and Immunoglobulins M (IgM) antibody, regular blood testing, assessment of natural killer cell activity, and histological observation of spleen in immunosuppressed mice were measured to evaluate the immunoregulation effects of PSE30 and PSE75. Besides, effects of PSE75 on gut microbial were evaluated using 16s rRNA sequence. And the mRNA expression and cytokine secretion of RAW264.7 cell were evaluated to analyze the immunoregulation mechanism of PSE75. RESULTS: The content of serum IgG, IgM was significantly elevated by PSE75 (P＜0.05, P＜0.001). The NK cells killing activity in splenocytes against K562 cells induced by PSE30, and PSE75 was pronounced higher than that of the model group (P < 0.05). Both mRNA expression of Th1 molecular markers including interleukin (IL)-2, interferon (IFN)-γ, and signal transducers and activators of transcription (STAT) 4, and Th2 molecular markers including IL-4 in splenocytes were markedly enhanced by PSE30, and PSE75 (P < 0.05, P < 0.01, or P < 0.001). Besides, the result of 16s rRNA sequence indicated that PSE75 could recover the gut microbial community disturbed by cyclophosphamide. PSE75 could markedly promote the secretion of IL-6, IL-10, and IL-12 p40 from RAW264.7 cell (P＜0.01, or P＜0.001). CONCLUSIONS: PSE75 was proved to be a more promising immunomodulation agent, of which may enhance the immunity of immunosuppressed mice by improving gut microbial and activating macrophages. And PSE75 could be developed as a good immune booster in the future.

Optimization for ultrasonic-microwave synergetic extraction of total iridoid glycosides and screening of analgesic and anti-inflammatory active fractions from patrinia scabra Bunge (Valerianaceae).

BACKGROUND: Patrinia scabra Bunge is a well-known herbal medicine for its favorable treatment on inflammatory diseases owing to its effective ingredients, in which iridoid glycoside plays an extremely significant role. This article aimed to improve the content of total iridoid glycosides in crude extract through a series optimization of extraction procedure. Moreover, considering that both pain and inflammation are two correlated responses triggered in response to injury, irritants or pathogen, the article investigated the anti-inflammatory and analgesic activities of P. scabra to screen out the active fraction. METHOD: P. scabra was extracted by ultrasonic-microwave synergistic extraction (UMSE) to obtain total iridoid glycosides (PSI), during which a series of conditions were investigated based on single-factor experiments. The extraction process was further optimized by a reliable statistical method of response surface methodology (RSM). The elution fractions of P. scabra extract were prepared by macroporous resin column chromatography. Through the various animal experiment including acetic acid-induced writhing test, formalin induced licking and flinching, carrageenan-induced mice paw oedema test and xylene-induced ear edema in mice, the active fractions with favorable analgesic and anti-inflammatory effect were reasonably screen out. RESULTS: The content of PSI could reach up to 81.42 ± 0.31 mg/g under the optimum conditions as follows: ethanol concentration of 52%, material-to-liquid ratio of 1:18 g/mL, microwave power at 610 W and extraction time of 45 min. After gradient elution by the macroporous resin, the content of PSI increased significantly. Compared with other concentrations of elution liquid, the content of PSI in 30 and 50% ethanol eluate was increased to reach 497.65 and 506.90 mg/g, respectively. Owing to the pharmacology experiment, it was reasonably revealed that 30 and 50% ethanol elution fractions of P. scabra could relieve pain centrally and peripherally, exhibiting good analgesic and anti-inflammatory activities. CONCLUSION: Patrinia scabra possessed rich iridoids and exhibited significant analgesic and anti-inflammatory activities.

An Active Fraction of Trillium tschonoskii Promotes the Regeneration of Intestinal Epithelial Cells After Irradiation.

Despite significant scientific advances toward the development of safe and effective radiation countermeasures, no drug has been approved for use in the clinic for prevention or treatment of radiation-induced acute gastrointestinal syndrome (AGS). Thus, there is an urgent need to develop potential drugs to accelerate the repair of injured intestinal tissue. In this study, we investigated that whether some fractions of Traditional Chinese Medicine (TCM) have the ability to regulate intestinal crypt cell proliferation and promotes crypt regeneration after radiation. By screening the different supplements from a TCM library, we found that an active fraction of the rhizomes of Trillium tschonoskii Maxim (TT), TT-2, strongly increased the colony-forming ability of irradiated rat intestinal epithelial cell line 6 (IEC-6) cells. TT-2 significantly promoted the proliferation and inhibited the apoptosis of irradiated IEC-6 cells. Furthermore, in a small intestinal organoid radiation model, TT-2 promoted irradiated intestinal organoid growth and increased Lgr5+ intestinal stem cell (ICS) numbers. More importantly, the oral administration of TT-2 remarkably enhanced intestinal crypt cell proliferation and promoted the repair of the intestinal epithelium of mice after abdominal irradiation (ABI). Mechanistically, TT-2 remarkably activated the expression of ICS-associated and proliferation-promoting genes and inhibited apoptosis-related gene expression. Our data indicate that active fraction of TT can be developed into a potential oral drug for improving the regeneration and repair of intestinal epithelia that have intestinal radiation damage.

Advances in next-generation lipid-polymer hybrid nanocarriers with emphasis on polymer-modified functional liposomes and cell-based-biomimetic nanocarriers for active ingredients and fractions from Chinese medicine delivery.

Recently, functional liposomes modified with versatile polymer and cell-based- biomimetic nanoparticles have emerged as the most advanced lipid-polymer hybrid nanocarriers (LPNs) for drug delivery. This review highlights the advances of these two LPNs in the delivery of active ingredients and fractions from Chinese medicine with promising therapeutic, chemopreventive, or chemosensitive effects. To understand their complete potency, the relationship between the nanoparticle characteristics and their in vitro and in vivo performance characteristics has been discussed. Polymer-modified liposomes and cell-based biomimetic nanoparticles are beneficial for improving absorption, modulating release, targeting and overcoming multidrug resistance, and reducing side effects. The associated challenges, current limitations, and opportunities in this field are also discussed.

Study on the anti-inflammatory and analgesic effects of active fractions of Tongfeng granule on arthritis rats / 药学实践杂志

Objective To investigate the anti-inflammatory and analgesic effects of the active fractions of Tongfeng granules on rats with arthritis induced by complete Freund's adjuvant. Methods 56 SD rats were randomly divided into seven groups, blank group, model group, total flavonoids group, total organic acid group, total alkaloid group, Tongfeng granule group and positive control group. Except for the blank group, the remaining 6 groups established joints pathological model of inflammation. 15 days after the successful modeling, intragastric drug administration was continued for 30 days. The swelling of ankle joint, WBC, N%, IL-6, IL-10, TNF-α and the histopathology of joint were measured. Results Comparing with the model group, each effective fraction group of Tongfeng granules, Gout granules and positive control group decreased the ankle joint swelling rate significantly (P<0.01) and reduced fibrous tissue proliferation. There was no significant difference in WBC and N% of neutrophils. They significantly reduce the level of serum IL-6 and TNF-α, and increase the level of IL-10 (P<0.05, P<0.01). Conclusion This study clarifies the anti-inflammatory and analgesic effects of active fractions of Tongfeng granules and provides a basis for further clinical medication and preparation development.

Active fraction combination from Liuwei Dihuang decoction (LW-AFC) ameliorates corticosterone-induced long-term potentiation (LTP) impairment in mice in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: Liuwei Dihuang decoction (LW), a classic formula in Traditional Chinese medicine (TCM), has been used for nearly one thousand years for various diseases with characteristic features of kidney yin deficiency. LW consists of 6 herbs including Dihuang (prepared root of Rehmannia glutinosa (Gaertn.) DC.), Shanyao (rhizome of Dioscorea polystachya Turcz.), Shanzhuyu (fruit of Cornus officinalis Siebold & Zucc.), Mudanpi (root bark of Paeonia × suffruticosa Andrews), Zexie (rhizome of Alisma plantago-aquatica L.) and Fuling (scleorotia of Wolfiporia extensa (Peck) Ginns). LW-active fraction combination (LW-AFC) is extracted from LW, it is effective for the treatment of kidney yin deficiency in many animal models. Recent researches indicate that the "kidney deficiency" is related to a disturbance in the neuroendocrine immunomodulation (NIM) network, and glucocorticoids play an important role in kidney deficiency. AIM OF THE STUDY: This study evaluated the effects of LW-AFC and the active fractions (polysaccharide, LWB-B; glycoside, LWD-b; oligosaccharide, CA-30) on corticosterone (Cort)-induced long-term potentiation (LTP) impairment in vivo. MATERIALS AND METHODS: In this study, LTP was used to evaluate the synaptic plasticity. LW-AFC was orally administered for seven days. The active fractions were given by either chronic administration (i.g., i.p., 7 days) or single administration (i.c.v., i.g., i.p.). Cort was injected subcutaneously 1 h before the high-frequency stimulation (HFS) to induce LTP impairment. Moreover, in order to research on the possible effective pathways, an antibiotic cocktail and an immunosuppressant were also used. RESULTS: Chronic administration (i.g.) of LW-AFC and its three active fractions could ameliorate Cort-induced LTP impairment. Single administration (i.c.v., i.g., i.p.) of any of the active fractions had no effect on Cort-induced LTP impairment, while chronic administration (i.g., i.p.) of LWB-B or LWD-b showed positive effects against Cort. Interestingly, CA-30 only showed protective effects via i.g. administration, and there was little effect when CA-30 was administered i.p. In addition, when the intestinal microbiota was disrupted by application of the antibiotic cocktail, CA-30 showed little protective effects against Cort. The effects of LW-AFC were also abolished when the immune function was inhibited. In the hippocampal tissue, Cort treatment increased corticosterone and glutamate, and LW-AFC could inhibit the Cort-induced elevation of corticosterone and glutamate; there was little change in D-serine in Cort-treated animals, but LW-AFC could increase the D-serine levels. CONCLUSION: LW-AFC and its three active fractions could ameliorate Cort-induced LTP impairment. Their protective effects are unlikely by a direct way, and immune modulation might be the common pathway. CA-30 could protect LTP from impairment via modulating the intestinal microbiota. Decreasing corticosterone and glutamate and increasing D-serine in the Cort-treated animals' hippocampal tissue might be one of the mechanisms for the neural protective effects of LW-AFC. Further study is needed to understand the underlying mechanisms.

Study Approach of Antioxidant Properties in Foods: Update and Considerations.

The assessment of interactions between natural antioxidants and other food matrix components represents the main step in the investigation of total antioxidant properties, in terms of potential health benefits. The diversity of chemical structures of natural compounds, besides their possible interactions, as well as the biological role and different modes of action makes it difficult to assess a single and reliable procedure for the evaluation of antioxidant activity. Today, much attention is given to the distinction between extractable and non-extractable antioxidants as a key tool in the description of the nutritional and healthy properties of food matrices. The starting point for the investigation of antioxidant effects of food extracts is the analysis of antioxidant properties of pure compounds and their interactions. Another complementary approach could be represented by the study of how different biologically active compound-rich extracts contribute to the total antioxidant capacity.

Effects of the combined Herba Epimedii and Fructus Ligustri Lucidi on bone turnover and TGF-ß1/Smads pathway in GIOP rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Kidney deficiency is the main pathogenesis of osteoporosis based on the theory of "kidney governing bones" in traditional Chinese medicine (TCM). Combined Herba Epimedii and Fructus Ligustri Lucidi, based on traditional Chinese formula Er-Zhi pills, were frequently used in TCM formulas that were prescribed for kidney tonifying and bone strengthening. However, it is unclear whether the combination of the two herbs may have a protective influence on glucocorticoid-induced osteoporosis (GIOP). The objective of this study was to evaluate the therapeutic effects and the underlying molecular mechanism of the decoction and the active fractions of the combined herbs in GIOP rats. MATERIALS AND METHODS: Male Sprague-Dawley rats were divided into seven groups, including the normal control (NC), GIOP model (MO), active fractions low (100mg/kg, LAF), active fractions high (200mg/kg, HAF), decoction low (3.5g/kg, LD), decoction high (7g/kg, HD) and Calcium with Vitamin D3 (0.2773g/kg, CaD)-treated group. The GIOP model was established by intramuscular injection of dexamethasone (1mg/kg) twice a week for 8 weeks. Different kinds of indicators were measured, including bone mineral density (BMD), bone biomechanical properties, serum bone alkaline phosphatase (b-ALP), serum bone γ-carboxyglutamic acid-containing protein (BGP), serum bone morphogenetic protein-2 (BMP-2), serum tartrate-resistant acid phosphatase (TRACP) and serum carboxy terminal cross linked telopeptide of typeⅠcollagen (ICTP), bone mineral content (BMC) and bone structured histomorphometry. The protein and mRNA expression of TGF-ß1, Smad2, Smad3, Smad4 and Smad7 were detected by Western blotting (WB) and quantitative real time polymerase chain reaction (qRT-PCR), respectively. RESULTS: Administration of combined Herba Epimedii and Fructus Ligustri Lucidi decoction and combined active fractions could significantly prevent GC-induced bone loss by increasing the contents of serum b-ALP, BGP and BMP-2 as the markers of bone formation, reducing the serum TRACP and ICTP contents to inhibit bone resorption and enhancing BMC. They could also attenuate biomechanical properties and BMD reduction, deterioration of trabecular architecture in MO rats. The mRNA and protein expressions of TGF-ß1, smad2, smad3 and smad4 were up-regulated, and the mRNA and protein expression of Smad7 was down-regulated following combined Herba Epimedii and Fructus Ligustri Lucidi treatment. CONCLUSION: Combination of Herba Epimedii and Fructus Ligustri Lucidi exhibited protective effects on promoting bone formation and precluding bone resorption. The underlying mechanism may be attributed to its regulations on TGF-ß1/Smads pathway. The substance bases of the combined herbs on anti-osteoporosis were total flavonoids of Herba Epimedii, total iridoids and flavonoids of Fructus Ligustri Lucidi.

Evaluation of hepatoprotective effects of different extracts in root of Gardenia jasminoides based on partial least squares method and multi-attribute comprehensive index method / 中草药

Objective To compare the hepatoprotective effects of different extracts in root of Gardenia jasminoides including ethanol extract, petroleum ether fraction, ethyl acetate, chloroform extract, n-butanol extract, and surplus water extract on the jaundice hepatitis mice by the partial least squares (PLS) method and multi index comprehensive evaluation method. Methods Setting up two groups of high and low doses (9 and 3 g/kg) in different extraction sites in root of G. jasminoides respectively, and administered to the stomach for 7 d. Copying a icteric hepatitis model of mice by alpha naphthylisothiocyanate (ANIT) in 5th d. Then, the alanine aminotransferase (ALT), aspartic transaminase (AST), alkaline phosphatase (AKP), γ-glutamyl transpeptidase (γ-GT), total bile acid (TBA), total bilirubin (TBIL), superoxide dismutase (SOD), malonic dialdehyde (MDA), glutathione (GSH) activity were determinated in serum and liver, and pathological changes were observed in mouse liver by HE stain, total hepatoprotective effect of the different extracts in root of G. jasminoides was compared by PLS and multi index comprehensive evaluation method. Results In addition to the high dose group of petroleum ether and low dose group of chloroform, the different extracts in root of G. jasminoides were improved on some indexes or multiple indicators to an extent and compared with the model group, the pathological damage of liver tissue was alleviated obviously, multi index comprehensive evaluation showed that the high dose group of ethyl acetatein root of G. jasminoides had the best hepatoprotective effect. Conclusion The ethyl acetate extract and n-butanol extract in root of G. jasminoides have better inhibitory effect on icteric hepatitis, and the high dose group of ethyl acetate has the best effect, which may be the active site of liver protection, and mechanism may be related to improving the ability of eliminating oxygen free radical, inhibiting lipid peroxidation and enhancing bile bilirubin metabolism and secretion.

Active chemical fractions of stem bark extract of Khaya grandifoliola C.DC and Entada africana Guill. et Perr. synergistically protect primary rat hepatocytes against paracetamol-induced damage.

BACKGROUND: Khaya grandifoliola (Meliaceae) and Entada africana (Fabaceae) are traditionally used in Bamun (a western tribe of Cameroon) traditional medicine for the treatment of liver related diseases. In this study, the synergistic hepatoprotective effect of respective active fractions of the plants were investigated against paracetamol-induced toxicity in primary cultures of rat hepatocytes. METHODS: Paracetamol conferred hepatocyte toxicity, as determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay, alanine aminotransferase (ALT), superoxide dismutase (SOD), catalase (CAT) activities, malondialdehyde (MDA) and glutathione (GSH) content assays. The crude extracts were fractionated by flash chromatography and fractions were tested for hepato-(protective and curative) activities. The most active fractions of both plants were tested individually, and in combination based on their respective half effective concentration (EC50). RESULTS: The methylene chloride/methanol fractions of K. grandifoliola (75:25 v/v) (KgF25) and E. africana (90:10 v/v) (EaF10) were found to be the most hepato-protective with EC50 values of 10.30 ± 1.66 µg/ml and 13.47 ± 2.06 µg/ml respectively, comparable with that of silymarin (13.71 ± 3.87 µg/ml). These fractions and their combination significantly (P <0.05) improved cell viability, inhibited ALT leakage and MDA formation, and restored cellular CAT, SOD activities and GSH content. The combination was more effective in restoring biochemical parameters with coefficients of drugs interaction (CDI) less than 1. CONCLUSION: These findings demonstrate that the active fractions have synergistic action in the protection of rat hepatocytes against paracetamol-induced damage and suggest that their hepatoprotective properties may be maximized by using them in combination.

Study on anti-inflammatory efficacy and correlative ingredients with pharmacodynamics detected in acute inflammation rat model serum from Caulis Lonicerae japonicae.

BACKGROUND: Caulis Lonicerae japonicae (CLJ) is often used for the treatment of inflammation such as acute fever, headache, respiratory infection and epidemic diseases. Nevertheless, domestic and foreign researches simply fail to focus on reports of CLJ, especially its anti-inflammatory effects and correlative components. PURPOSE: In this study, we investigated anti-inflammatory effects and serum components of Caulis Lonicerae japonicae (CLJ) in models of acute inflammation and correlative analysis between anti-inflammatory effects and serum components of CLJ in rat serum to analyze the changes in the relative contents of components in serum with time and in the corresponding values to characterize active fractions of CLJ and identify the major active components of CLJ in rats. STUDY DESIGN: Active fractions of CLJ were screened using xylene-induced ear oedema mice model. Anti-inflammatory effects were evaluated using carrageenan-induced paw oedema rat model, and then correlative components in rat serum were demonstrated with HPLC-QTOF/MS/MS method explored. METHODS: HPLC-QTOF/MS/MS was developed to analyze the components absorbed in rat serum after oral administration of CLJ. RESULTS: Ethyl acetate extracts (ECLJ) and n-butanol extracts (BCLJ) of CLJ were preliminarily screened as active fractions of CLJ (EBCLJ) using xylene-induced ear oedema mice model, and effectively inhibited edema and values of interleukin-1 (IL-l), nuclear factor-kappaB (NF-kB), tumor necrosis factor-α (TNF-α) activities and prostaglandinE2 (PGE2) productions using carrageenan-induced paw oedema rat model. 33 peaks were found in total ion current chromatograms of EBCLJ, and 27 components were observed in EBCLJ-treated rat serum, only 11 of which were correlated with anti-inflammatory effects. CONCLUSIONS: The present study contributes to the study on the pharmacodynamic basis of CLJ and provides potent evidence for developing CLJ as a safe and promising natural drug in inflammation treatment.

Wound healing properties of ethyl acetate fraction of Moringa oleifera in normal human dermal fibroblasts.

BACKGROUND/AIM: Wounds are the outcome of injuries to the skin that interrupt the soft tissue. Healing of a wound is a complex and long-drawn-out process of tissue repair and remodeling in response to injury. A large number of plants are used by folklore traditions for the treatment of cuts, wounds and burns. Moringa oleifera (MO) is an herb used as a traditional folk medicine for the treatment of various skin wounds and associated diseases. The underlying mechanisms of wound healing activity of ethyl acetate fraction of MO leaves extract are completely unknown. MATERIALS AND METHODS: In the current study, ethyl acetate fraction of MO leaves was investigated for its efficacy on cell viability, proliferation and migration (wound closure rate) in human normal dermal fibroblast cells. RESULTS: Results revealed that lower concentration (12.5 µg/ml, 25 µg/ml, and 50 µg/ml) of ethyl acetate fraction of MO leaves showed remarkable proliferative and migratory effect on normal human dermal fibroblasts. CONCLUSION: This study suggested that ethyl acetate fraction of MO leaves might be a potential therapeutic agent for skin wound healing by promoting fibroblast proliferation and migration through increasing the wound closure rate corroborating its traditional use.

Evaluation of the effects of active fractions of chinese medicine formulas on IL-1ß, IL-6, and TNF-α release from ANA-1 murine macrophages.

ETHNOPHARMACOLOGICAL RELEVANCE: Yaotongning (YTN) is a traditional Chinese Medicine (TCM) that contains ten component medicinal materials (CMMs) and uses Chinese rice wine as a vehicle to enhance its efficacy. YTN has been used for rheumatoid arthritis (RA) treatment in China for decades and has been reported to have anti-inflammatory and analgesic effects, as well as to strengthen the immune system. AIM OF THE STUDY: The present work quantitatively evaluated the in vitro effects of active fractions from the ten CMMs that make up YTN and eight additional herbs commonly used in TCM formulas for RA treatment, as well as different combinations of these active fractions, on cellular immune response; the findings were used to determine which active fractions are responsible for promoting an immune response, and to assess whether YTN is superior to other similar formulas and whether YTN can be improved by simplifying its formula from the point of its cellular immunomodulatory activity. MATERIALS AND METHODS: Using the YTN formulation principles and some concepts in combinatorial chemistry, 27 TCM samples were designed by combining some or all of the active fractions of YTN and other eight herbs used for RA treatment. Release of interleukin-1ß (IL-1ß), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α) from ANA-1 murine macrophages was measured using an enzyme-linked immunosorbent assay (ELISA). The immunoregulatory effects of the TCM samples were evaluated by comparing their half-effective concentrations (EC50) for stimulating the release of these cytokines. RESULTS: Among the investigated active fractions, the flavonoids from Carthamus tinctorius (Fct), Davallia mariesii (Fdm), and Cinnamomum cassia Twig volatile oils (Vca) from the eight selected herbs effectively promoted IL-1ß and IL-6 release from ANA-1 cells. Saponins from the YTN CMM Glycyrrhiza uralensis (Sgu) were the most potent promoters of IL-1ß and TNF-α release. The aqueous extract of YTN CMM Eupolyphaga sinensis (Ves) strongly enhanced the release of IL-1ß, IL-6, and TNF-α from ANA-1 cells. The EC50 values for stimulating the secretion of IL-1ß, IL-6, and TNF-α could be determined for only six samples. The full YTN formula and the sample containing 50% Glycyrrhiza uralensis saponins, 25% of the mixture of alkaloids, and 25% of the mixture of all flavonoids exhibited good comprehensive cellular immunomodulatory activity. The immunomodulatory activity of the complete YTN formula was better than that of the sample containing all active fractions of YTN without Chinese rice wine (the YTN vehicle). CONCLUSIONS: Sgu and Ves are the primary active fractions of YTN involved in stimulating immune responses. The YTN prescription was reasonably effective at promoting cellular immune responses. Chinese rice wine, the YTN vehicle, strengthened the immunoregulatory activity of YTN. The results of this study demonstrate that the YTN recipe could be improved by reducing the number of CMMs and altering some active fractions without reducing its activity to promote cellular immune responses.

Screening of anti-inflammatory and analgesic effective fractions from Cayratia japonica / 中草药

Objective: To investigate the anti-inflammatory and analgesic effective fractions from Cayratia japonica. Methods: The acute inflammatory models, such as xylene-induced ear edema, egg white-induced paw edema, and the chronic inflammatory model granuloma induced by cotton pellet implantation, were used in researching the inflammatory effects of the different fractions from C. japonica by ig administration. Meanwhile, the analgesic effects of the different fractions from C. japonica were observed by hot plate and acetic acid writhing test. Results: Compared with the model group, high-and low-dose water fraction and water extract could significantly inhibit ear edema in mice (P<0.05, 0.01) and paw edema in rats (P<0.05, 0.01). Also, water fraction and water extract decreased the granuloma of rats (P<0.01). Moreover, after the treatment with high-and low-dose petroleum ether fraction and water extract, the pain threshold with hot plate method was significantly prolonged (P<0.05, 0.01) compared with the model group and the data before the drugs administration. The writhing number was reduced after administration (P<0.01) compared to the model group. Conclusion: The anti-inflammatory effect of C. japonica mainly locates in the water fraction, and the analgesic effect is mainly the petroleum ether fraction.

Screening of Active Fractions for Purple Sweet Potato Flavonoids with Insulin Resistance Improving Ability of L6 Cells / 中国药师

Objective:To screen the active fractions from purple sweet potatoes containing flavonoids with insulin resistance impro -ving ability.Methods:L6 cell model with insulin resistance was established .The extracting solutions with different polarity of purple sweet potato flavonoids were used to affect the model .The residual glucose concentration in insulin resistant L 6 cells was observed and compared before and after the intervention .Results:The residual glucose concentration of total flavonoids extracting solution , butanol extracting solution at middle and high dose , and chloroform extracting solution at all doses of purple sweet potato were lower than that of IR group (P<0.05).Conclusion:The total flavonoids extract, chloroform extracting solution and butanol extracting solution of purple sweet potato can improve insulin resistance in L 6 cells.

Nanocarriers for the delivery of active ingredients and fractions extracted from natural products used in traditional Chinese medicine (TCM).

Traditional Chinese medicine (TCM) has been practiced for thousands of years with a recent increase in popularity. Despite promising biological activities of active ingredients and fractions from TCM, their poor solubility, poor stability, short biological half-life, ease of metabolism and rapid elimination hinder their clinical application. Therefore, overcoming these problems to improve the therapeutic efficacy of TCM preparations is a major focus of pharmaceutical sciences. Recently, nanocarriers have drawn increasing attention for their excellent and efficient delivery of active TCM ingredients or fractions. This review discusses problems in the delivery of active TCM ingredients or fractions; focuses on recent advances in nanocarriers that represent potential solutions to these problems, including lipid-based nanoparticles and polymeric, inorganic, and hybrid nanocarriers; and discusses unanswered questions in the field and criteria for the development of better nanocarriers for the delivery of active TCM ingredients or fractions to be focused on in future studies.

Antiproliferative and apoptotic activities of extracts of Asclepias subulata.

CONTEXT: Asclepias subulata Decne. (Apocynaceae) is a shrub used in the Mexican traditional medicine for the treatment of cancer. OBJECTIVE: The objective of this study was to evaluate the antiproliferative activity of methanol extract of aerial parts of A. subulata and its fractions against different cancer cell lines. Additionally, we analyzed the mechanism of action of the active fractions. MATERIALS AND METHODS: Methanol extract fractions were prepared by serial extraction with n-hexane, ethyl acetate, and ethanol. The antiproliferative activity of methanol extract and its fractions was evaluated, against several murine (M12.C3.F6, RAW 264.7, and L929) and human (HeLa, A549, PC-3, LS 180, and ARPE-19) cell lines by the MTT assay, using concentrations of 0.4-400 µg/mL for 48 h. Ethanol and residual fractions were separated using silica gel column. Apoptosis induction of cancer cells was evaluated by Annexin and JC-1 staining using flow cytometry. RESULTS: Methanol extract and its fractions showed antiproliferative activity against all human cancer cell lines tested. Methanol extract had the highest antiproliferative activity on A549 and HeLa cells (IC50 values < 0.4 and 8.7 µg/mL, respectively). Ethanol and residual fractions exerted significant antiproliferative effect on A549 (IC50 < 0.4 µg/mL) and PC3 cells (IC50 1.4 and 5.1 µg/mL). Apoptotic assays showed that CEF7, CEF9, CRF6, and CRF5 fractions induced mitochondrial depolarization in A549 cells, 70, 73, 77, and 80%, respectively. Those fractions triggered the apoptosis mitochondrial pathway. CONCLUSION: Our data show that A. subulata extracts have potent antiproliferative properties on human cancer cell lines. This plant should be considered an important source of potent anticancer compounds.