Combining ability analysis in bitter gourd (Momordica charantia L.) for potential quality improvement

Abstract Combining ability analysis provides useful information for the selection of parents, also information regarding the nature and magnitude of involved gene actions. Crops improvement involves strategies for enhancing yield potentiality and quality components. Targeting the improvement of respective characters in bitter gourd, combining ability and genetic parameters for 19 characters were estimated from a 6×6 full diallel analysis technique. The results revealed that the variances due to general combining ability (GCA) and specific combining ability (SCA) were highly significant for most of the important characters. It indicated the importance of both additive and non-additive gene actions. GCA variances were higher in magnitude than SCA variances for all the characters studied indicating the predominance of the additive gene effects in their inheritance. The parent P2 (BG 009) appeared as the best general combiner for earliness; P1 (BG 006) for number of fruits, average single fruit weight and fruit yield; P4 (BG 027) for node number of first female flower and days to seed fruit maturity; P3 (BG 011) for fruit length and thickness of the fruit flesh; P5 (BG 033) for 100-seed weight; and P6 for number of nodes per main vine. The SCA effect as well as reciprocal effect was also significant for most of the important characters in different crosses.

Resumo A análise da capacidade de combinação fornece informações úteis para a seleção dos pais, também informações sobre a natureza e a magnitude das ações dos genes envolvidos. A melhoria das safras envolve estratégias para aumentar a potencialidade da produção e os componentes de qualidade. Visando ao aprimoramento dos respectivos caracteres em cabaça-amarga, capacidade de combinação e parâmetros genéticos para 19 caracteres, foram estimados a partir de uma técnica de análise dialélica completa 6 × 6. Os resultados revelaram que as variâncias, devido à capacidade geral de combinação (GCA) e capacidade específica de combinação (SCA), foram altamente significativas para a maioria dos caracteres importantes. Indicou a importância das ações gênicas aditivas e não aditivas. As variâncias GCA foram maiores em magnitude do que as variâncias SCA para todos os caracteres estudados, indicando a predominância dos efeitos do gene aditivo em sua herança. O pai P2 (BG 009) apareceu como o melhor combinador geral para o início; P1 (BG 006) para número de frutos, peso médio de um único fruto e produção de frutos; P4 (BG 027) para número de nó da primeira flor fêmea e dias para a maturidade do fruto da semente; P3 (BG 011) para comprimento do fruto e espessura da polpa do fruto; P5 (BG 033) para peso de 100 sementes; e P6 para o número de nós por videira principal. O efeito SCA, bem como o efeito recíproco, também foi significativo para a maioria dos personagens importantes em cruzamentos diferentes.

Combining ability analysis in bitter gourd (Momordica charantia L. ) for potential quality improvement / Análise de capacidade de combinação em cabaça-amarga (Momordica charantia L. ) para melhoria potencial da qualidade

Abstract Combining ability analysis provides useful information for the selection of parents, also information regarding the nature and magnitude of involved gene actions. Crops improvement involves strategies for enhancing yield potentiality and quality components. Targeting the improvement of respective characters in bitter gourd, combining ability and genetic parameters for 19 characters were estimated from a 6×6 full diallel analysis technique. The results revealed that the variances due to general combining ability (GCA) and specific combining ability (SCA) were highly significant for most of the important characters. It indicated the importance of both additive and non-additive gene actions. GCA variances were higher in magnitude than SCA variances for all the characters studied indicating the predominance of the additive gene effects in their inheritance. The parent P2 (BG 009) appeared as the best general combiner for earliness; P1 (BG 006) for number of fruits, average single fruit weight and fruit yield; P4 (BG 027) for node number of first female flower and days to seed fruit maturity; P3 (BG 011) for fruit length and thickness of the fruit flesh; P5 (BG 033) for 100-seed weight; and P6 for number of nodes per main vine. The SCA effect as well as reciprocal effect was also significant for most of the important characters in different crosses.

Resumo A análise da capacidade de combinação fornece informações úteis para a seleção dos pais, também informações sobre a natureza e a magnitude das ações dos genes envolvidos. A melhoria das safras envolve estratégias para aumentar a potencialidade da produção e os componentes de qualidade. Visando ao aprimoramento dos respectivos caracteres em cabaça-amarga, capacidade de combinação e parâmetros genéticos para 19 caracteres, foram estimados a partir de uma técnica de análise dialélica completa 6 × 6. Os resultados revelaram que as variâncias, devido à capacidade geral de combinação (GCA) e capacidade específica de combinação (SCA), foram altamente significativas para a maioria dos caracteres importantes. Indicou a importância das ações gênicas aditivas e não aditivas. As variâncias GCA foram maiores em magnitude do que as variâncias SCA para todos os caracteres estudados, indicando a predominância dos efeitos do gene aditivo em sua herança. O pai P2 (BG 009) apareceu como o melhor combinador geral para o início; P1 (BG 006) para número de frutos, peso médio de um único fruto e produção de frutos; P4 (BG 027) para número de nó da primeira flor fêmea e dias para a maturidade do fruto da semente; P3 (BG 011) para comprimento do fruto e espessura da polpa do fruto; P5 (BG 033) para peso de 100 sementes; e P6 para o número de nós por videira principal. O efeito SCA, bem como o efeito recíproco, também foi significativo para a maioria dos personagens importantes em cruzamentos diferentes.

Research progress of taste masking and evaluation technology of medicine / 中国药科大学学报

@#Most drugs taste bitter and irritating, resulting in poor compliance of patients, and the bad odor affects the therapeutic effect. The successful research and development of a drug should not only conform to the five quality characteristics of effectiveness, stability, safety, uniformity and economy, but also the compliance of patients to drugs with bad odor. The development of taste masking techniques is critical for bitter drugs.This review describes the principles, advantages and drawbacks of traditional taste masking techniques, and introduces the mechanism and application of novel taste masking techniques, such as melt granulation, hot melt extrusion, 3D printing, drug complex preparation, and bitter taste inhibitors. The in vitro evaluation methods of drug taste masking effect, such as functional magnetic resonance imaging, in vitro dissolution, and electronic tongue technology, are described. And introduce in vivo evaluation methods, such as animal and human taste, in the field of taste masking effect. A new strategy of BP neural network prediction model for drug taste evaluation is proposed, with a view to providing theoretical reference for the future research on drug taste masking.

Properties of new exotic traditional Chinese medicinal Vernonia amygdalina leaves:a literature research / 中国中药杂志

The leaves of Vernonia amygdalina Delile of the family Asteraceae(also known as "bitter leaf"), rich in biological activities, are used as both medicine and food for a long time in West tropical Africa. They have been introduced into Southeast Asia and Fujian and Guangdong provinces of China in recent years. However, little is known about the properties of the plant in traditional Chinese medicine(TCM), which limits its combination with other Chinese medicinal herbs. In this study, 473 articles on V. amygdalina leaves were selected from PubMed, Web of Science, CNKI, Wanfang Data and VIP to summarize their components, pharmacological effects and clinical research. V. amygdalina leaves presented anti-microbial, hypoglycemic, anti-hypertensive, lipid-lowering, anti-tumor, anti-inflammatory, antioxidant, and other pharmacological effects. On the basis of the theory of TCM properties, the leaves were inferred to be cold in property and bitter and sweet in flavor, acting on spleen, liver, stomach and large intestine and with the functions of clearing heat, drying dampness, purging fire, removing toxin, killing insects and preventing attack of malaria. They can be used to treat dampness-heat diarrhea, interior heat and diabetes, malaria, insect accumulation and eczema(5-10 g dry leaves by decoction per day and an appropriate amount of crushed fresh leaves applying to the affected area for external use). Due to the lack of TCM properties, V. amygdalina leaves are rarely used medicinally in China. The determination of medicinal properties of the leaves is conducive to the introduction of new exotic medicinal herbs and the development of new TCM resources, which facilitated further clinical application and research and development of Chinese medicinal herbs.

Alternativas fitoterápicas no controle da obesidade / Phytotherapy alternatives in obesity control / Alternativas herbales en el control de la obesidad

Nos últimos anos, a obesidade vem aumentando consideravelmente entre adultos e crianças e, segundo a OMS, estima-se que em 2025 o número de obesos ultrapasse a 2,3 milhões em todo o mundo. O indivíduo obeso apresenta maiores riscos de desenvolver doenças crônicas não transmissíveis, como diabetes, doenças cardiovasculares, dislipidemias e ainda alguns tipos de cânceres. O tratamento para a obesidade é variado e inclui mudanças no estilo de vida como: hábitos alimentares e prática de atividade física, tratamento medicamentoso, cirurgia bariátrica e fitoterápicos com o potencial de auxiliar no tratamento. O objetivo deste trabalho foi realizar uma revisão bibliográfica a fim de avaliar os benefícios da utilização de medicamentos fitoterápicos como auxiliar no tratamento da obesidade, seus principais ativos, mecanismos de ação e sua utilização popular. Dentre as plantas pesquisadas e que demonstraram potencial para atuar no tratamento da obesidade encontram-se Camelia sinensis, Citrus aurantium, Hibiscus sabdariffa, Coffea arabica, Ephedra sinica, Zingiber oficinale e Senna alexandrina. Os principais mecanismos de ação envolvidos no potencial anti-obesidade das plantas medicinais são a capacidade de controle do apetite e ingestão de energia, estímulo da termogênese, inibição da lipase pancreática e redução da absorção de gordura, diminuição da lipogênese e aumento da lipólise. Desta forma, conclui-se que as plantas selecionadas neste estudo apresentaram efeitos positivos nos parâmetros bioquímicos e físicos, podendo ser incluídas nos protocolos como coadjuvantes nos tratamentos de emagrecimento.

In recent years, obesity has increased considerably among adults and children and according to the WHO, it is estimated that in 2025 the number of obese people will exceed 2.3 million worldwide. The obese individual is at greater risk of developing non-communicable chronic diseases, such as diabetes, cardiovascular disease, dyslipidemia and even some types of cancer. The treatment for obesity is varied, including changes in lifestyle such as eating habits and physical activity, drug treatment, bariatric surgery and phytotherapy with the potential to aid in the treatment. The objective of this work was to carry out a literature review, evaluating the benefits of using herbal medicines as an aid in the treatment of obesity, their main assets, mechanisms of action and their popular use. Among the plants researched and that have shown potential to act in the treatment of obesity are Camelia sinensis, Citrus aurantium, Hibiscus sabdariffa, Coffea arabica, Ephedra sinica, Zingiber officiale and Senna alexandrina. The main mechanisms of action involved in the antiobesity potential of medicinal plants are the ability to control appetite and energy intake, thermogenesis stimulation, pancreatic lipase inhibition and reduction of fat absorption, lipogenesis decrease and lipolysis increase. Thus, it is concluded that the plants selected in this study showed positive effects on biochemical and physical parameters, and can be included in the protocols as adjuvants in weight loss treatments.

En los últimos años, la obesidad ha aumentado considerablemente entre adultos y niños y, según la OMS, se estima que en 2025 el número de obesos superará los 2,3 millones en todo el mundo. Los individuos obesos tienen un mayor riesgo de desarrollar enfermedades crónicas no transmisibles, como la diabetes, las enfermedades cardiovasculares, las dislipidemias e incluso algunos tipos de cáncer. El tratamiento de la obesidad es variado e incluye cambios en el estilo de vida como: hábitos alimenticios y práctica de actividad física, tratamiento farmacológico, cirugía bariátrica y medicamentos a base de hierbas con potencial para ayudar en el tratamiento. El objetivo de este trabajo fue realizar una revisión bibliográfica para evaluar los beneficios del uso de las hierbas medicinales como ayuda en el tratamiento de la obesidad, sus principales activos, mecanismos de acción y su uso popular. Entre las plantas investigadas y que mostraron potencial para actuar en el tratamiento de la obesidad están Camelia sinensis, Citrus aurantium, Hibiscus sabdariffa, Coffea arabica, Ephedra sinica, Zingiber oficinale y Senna alexandrina. Los principales mecanismos de acción implicados en el potencial antiobesidad de las plantas medicinales son la capacidad de controlar el apetito y la ingesta de energía, estimular la termogénesis, inhibir la lipasa pancreática y reducir la absorción de grasas, disminuir la lipogénesis y aumentar la lipólisis. Por lo tanto, se concluye que las plantas seleccionadas en este estudio mostraron efectos positivos sobre los parámetros bioquímicos y físicos, y pueden ser incluidas en los protocolos como coadyuvantes en los tratamientos de pérdida de peso.

A study on physiological taste threshold in hyperthyroidism

Background: Taste is the perception produced when a substance in the mouth reacts chemically with taste receptors located on taste buds in the oral cavity. The five basic taste modalities are sweet, salt, sour, bitter, and umami. Disorders of taste can result from various diseases and use of various drugs. Hyperthyroidism is one among them which affects the taste sensation and threshold. Aim and Objectives: The study was conducted to assess the physiological taste threshold for the five primary taste modalities in hyperthyroid patients and to compare their taste thresholds with that of the normal healthy controls. Materials and Methods: Investigations were carried out in 30 hyperthyroid patients aged between 20 and 50 years and in age, sex, and anthropometrically matched control groups of 30, who were apparently healthy. The statistical analysis was done by student’s t-test. Results: There is no difference in the physiological threshold of the all the basic tastes but salt. A significant (P < 0.05) increase in the taste threshold for salt taste can be seen in hyperthyroid patients compared to that of controls. Conclusion: The threshold for salt taste was altered in hyperthyroidism, which can be detected by proper screening. Taste dysfunction leads to reduced food intake and poor nutrition. Proper treatment and counseling can help them to get back their normal taste threshold along with normal thyroid status.

Evaluation of Phytochemical and Antibacterial Potential of Vernonia amygdalina and Elaeis guineensis on Some Bacteria Associated with Diarrhea

Background: Bitter leaf and palm oil combination in treating diarrhoea is common in Africa. The aim of this study is to determine the synergistic and antimicrobial potential of Vernonia amygdalina and Elaeis guineensis on bacteria isolates from diarrheic stool.Methodology: One hundred and fifty (150) diarrheic stool samples from the Diagnostic Laboratory in Rivers State University Teaching Hospital (RSUTH), Port Harcourt, were inoculated in Selenite F broth, MacConkey, Nutrient and Salmonella-Shigella agar plates using standard methods. Fresh and dry bitter leaf extracts were prepared by mashing, weighing and dissolving 100 grams(g) and 150 g concentrations of each in 100 milliliters(mls) of ethanol and sterile distilled water respectively. Undiluted mixture of bitter leaf and palm oil were prepared by mixing 2 mls of each in a sterile beaker. Zero-point one milliliter (0.1ml) of each undiluted extract, their mixture, ethanol and palm oil were separately dispensed into appropriately labeled wells using sterile pipette for sensitivity test on the isolated bacteria. The pH, temperatures and the phytochemical contents of the bitter extracts and palm oil were determined using pH meter, thermometer and spectrophotometric method.Results: Escherichia coli, Staphylococcus aureus and Salmonella sp. were isolated. The pH and temperature of bitter leaf extract and palm oil were 7.2 and 26?C and 6.7 and 26?C respectively while the pH and temperature for bitter leaf and the palm oil mixture was 6.9 and 26?C. The bitter leaf and palm oil extracts, their combination, ethanol and distilled water used on the isolates as antibiotics did not show any sensitivity. The phytochemicals identified in the bitter leaf were saponins, alkaloids and tannins while carotene was detected in the palm oil.Conclusion: It can be concluded that the bitter leaf extract, palm oil and their combination did not inhibit the growth of bacteria as a result of lack of bioactive components from the bitter leaf. The nature of the diluents used for the extraction may not have been the right one as it would have caused the low concentration, dilution and disfiguring of the molecules of the bioactive compounds that prevented the proper reaction between the bacteria and the extracts used.

Product Optimization, Storage Quality and Sensory Acceptance of Low Calorie Beverage Developed from Bitter Gourd and Kiwifruit

Abstract Bitter gourd (Momordica charantia L.) fruit is good source of many nutraceutical compounds and possess antioxidant, anti-diabetic and hypoglycaemic activities. However, its utilization in the preparation of beverages is limited due to its bitter after taste. Therefore, to realize the functional and therapeutic benefits of bitter gourd, an attempt was made to optimize nutritious and low caloriebitter gourd based beverage by blending with kiwifruit (Actinidia deliciosa), a store house of bioactive compounds and substituting sugar with stevioside (steviol glycoside). The standard (sugar sweetened) bitter gourd (BG)-kiwifruit (K) blended beverage was developed by utilizing 30% fruit part of BG:K blended juice (80: 20) with 40oB TSS and 1.3% acidity. Further, to develop the low calorie beverage, sucrose (table sugar) was replaced with 25, 50, 75 and 100% equi-sweetness level of stevioside (steviol glycoside). Results revealed that 75% substitution of sucrose with stevioside resulted in shelf stable beverage with identical taste, good antioxidant potential (68.80%) and strong antimicrobial activity (26 mm ZOI) with reduced calorie values (28.5 Kcal/100g) compared to the sugar sweetened control sample (150.60 Kcal/100g). Hence, the developed beverage can be commercialized as low calorie beverage with additional health benefits of natural compounds of bitter gourd and kiwifruit with highest bioactivity.

Mechanism of Combination of Pungent Dispersing Bitter Evacuant in Treatment of Asthma Based on Theory of Five Flavor Compatibility / 中国实验方剂学杂志

Bronchial asthma， a chronic inflammatory airway disease， belongs to the category of wheezing disease in the system of traditional Chinese medicine （TCM）. The wheezing symptom of this disease is mainly caused by the imbalance of lung Qi. According to the theory of five flavor compatibility， the Chinese medicinal materials with five different flavors （pungent， bitter， sour， sweet， and salty） can be combined to produce new functions. The pungent medicinal materials have dispersing effect and the bitter medicinal materials have discharging effect， which are important components in the theory of five flavor compatibility. Pungent herbs and bitter herbs can relieve the adverse lung Qi， occupying an important position in the current medication for the treatment of asthma. However， there is still a lack of in-depth analysis of the TCM theory and mechanism of the compatibility of pungent herbs and bitter herbs in the treatment of asthma. The molecular mechanisms of action of pungent herbs and bitter herbs are closely related to transient receptor potential （TRP） channels and bitter taste receptors （TAS2Rs）， respectively. Ca2+ signaling has been recognized in the process of asthma and is involved in the development of multiple symptoms of asthma. The TRP channels and TAS2Rs located on the cell membrane have been proved to directly regulate the intracellular Ca2+ signal and play a role in the treatment of asthma. Therefore， the dispersing effect of pungent herbs and the discharging effect of bitter herbs may be realized through the Ca2+ signaling pathway mediated by TRPs/TAS2Rs. We summarized the theoretical understanding and modern studies of pungent herbs dispersing lung Qi and bitter herbs discharging lung Qi， aiming to explain the internal relationship and mechanism of the compatibility of pungent herbs and bitter herbs in the treatment of asthma from the perspective of TCM theory and modern medicine. The compatibility of pungent herbs and bitter herbs based on the theory of five flavor compatibility for the treatment of asthma has a solid theoretical basis of TCM， and its mechanism can be verified by modern research. Therefore， it may be a main research direction in the treatment of asthma by Chinese medicinal herbs in the future.

Herbal Textual Research on Polygonati Rhizoma in Famous Classical Formulas / 中国实验方剂学杂志

By consulting ancient Chinese herbal medicines and medical books， combined with modern documents， the textual research of Polygonati Rhizoma has been conducted to verify the name， origin， bitter-flavored Polygonatum species， Latin name evolution， origin， quality evaluation， harvesting and processing changes， so as to provide reference and basis for the development and utilization of the famous classical formulas. Through textual research， it can be seen that there are many other names for Polygonati Rhizoma， and Huangjing is the correct name since Mingyi Bielu. Based on the original research， it is concluded that P. sibiricum and P. cyrtonema were the mainstream of Polygonati Rhizoma before the Tang dynasty， and P. kingianum was added in the Qing dynasty. According to the shape of medicinal materials， these Polygonatum species were called Jitou Huangjing， Jiangxing Huangjing and Dahuangjing. The harvest time of Polygonati Rhizoma is spring and autumn. After harvest， it is steamed and dried in the sun， and its processing method is mainly "nine steaming and nine storms". Bitter-flavored Polygonatum is mainly P. cirrhifolium， P. zanlanscianense， P. curvistylum and P. verticillatum， which are not suitable for medicine. Based on textual research， it is recommended that when developing famous classical formulas and health products with Polygonati Rhizoma as the main raw material， the origin and producing area should be clear and fixed， and P. sibiricum or P. cyrtonema with clear origin should be used. It is necessary to conduct germplasm survey and sampling in the producing area， establish a planting base and a traceability system for Polygonati Rhizoma， in order to control the quality and stabilize the efficacy of the products. The processing method of Polygonati Rhizoma can be determined according to the product function positioning.

Bitter kola and kola nut use and their effect on treatment outcome on People Living with HIV at a Military Hospital in Benue state Nigeria: Bitter kola (Garcinia) and Cola nut (Cola nitida among PLWHIV

Introduction Bitter Kola (Garcinia Kola) and kola nut, contains substances attributed to numerous effects on humans including anti-inflammatory, anti-allergic properties, anti-infective and caffeinism. This study explores Bitter kola and kola nut use and its impact on treatment outcome on People Living with HIV (PLWHIV). Methods: The study was conducted at a Military Hospital in Nigeria. An analytical cross-sectional study was done using questionnaire among 700 HIV-positive clients selected using simple random sampling. Data were collected by researcher and three trained assistants. Chi-square test and binary logistic regression were used for identifying associations and predictors, respectively. The level of significance was set at p < 0.05. Results: Findings show that 260 (63.6%) and 179 (25.6%) have ever and currently used Bitter kola/Kola nut, respectively. Also, 14 (7.8%) used Bitter kola/Kola nut alone while 165 (92.2%) used it in addition to other substances, especially with alcohol 123 (68.7%). Bitter kola use was associated with age (p = 0.037), gender (p < 0.001), occupation (p = 0.001), and number of children (p < 0.011). Identified predictors were being a female (AOR 0.79; 95% CI 0.08-0.92) and earning <18,000 Naira (AOR 2.91; 95% CI 2.03-21.54). There was no association of Bitter kola/kola nut use with CD4 count and viral load suppression. Conclusion: Though Kola nut and Bitter kola use was high as in the general population we have not found any effect on treatment outcome among PLWHIV. This calls for more research to ascertain if there are other possible beneficial effects on PLWHIV.

Review of taste masking techniques in Chinese patent medicine / 中国中药杂志

Single herbs and Chinese patent medicine preparations often have bad taste, such as bitterness and astringency, which is one of the key factors affecting patients' medication compliance, and would affect the therapeutic effect and restrict the extensive application in clinical practice. Therefore, how to make use of taste masking techniques to improve the bad taste of traditional Chinese medicines has become an important project. Through the collection and summarization of Chinese and foreign journals and papers in recent years, this paper discussed the generation mechanism of bitter taste, the new methods of masking bitter taste and the evaluation me-thods of bitter taste, in order to provide references for the taste masking of Chinese patent medicines preparations.

Bitter gourd extract improves glucose homeostasis and lipid profile via enhancing insulin signaling in the liver and skeletal muscles of diabetic rats

Objective: To investigate the modulatory effects of bitter gourd extract on the insulin signaling pathway in the liver and skeletal muscle tissues of diabetic rats. Methods: The ethanolic extract of bitter gourd was prepared and its contents of total polyphenols and flavonoids were assayed. A neonatal streptozotocin-induced diabetic rat model was established and the diabetic rats were assigned into different groups and were treated with different doses of bitter gourd extract (100, 200, 400, or 600 mg/kg) or with glibenclamide (0.1 mg/kg) for 30 d. Fasting blood glucose, insulin, and lipid profile were evaluated and the insulin signaling pathway in the liver and skeletal muscle of rats was investigated. The correlations between homeostasis model assessment (HOMA) and the components of insulin signaling pathway were also evaluated. Results: Different doses of bitter gourd extract significantly ameliorated fasting blood glucose level and HOMA index for insulin resistance. Moreover, bitter gourd extract increased serum insulin and improved disrupted serum lipid profile. The levels of insulin receptor substrate-1 (IRS-1), p-insulin receptor β (p-IR-β), protein kinase C (PKC), GLUT2, and GLUT4 were improved by treatment with bitter gourd extract. The best results were obtained with 400 mg/kg dose of the extract, the effect of which was equivalent to that of glibenclamide. HOMA in the bitter gourd treated rats was negatively correlated with p-IR-β, IRS-1 and PKC in hepatic and skeletal muscle. HOMA was also negatively correlated with skeletal muscle GLUT4. Conclusions: Bitter gourd extract improves glucose homeostasis and lipid profile in diabetic rats via enhancement of insulin secretion and sensitivity. Therefore, bitter gourd can be used as a potential pharmacological agent for the treatment of type 2 diabetes mellitus.

Studies of dietary phytoestrogen from momordica charantia Linn. Seeds / Estudios de fitoestrógeno en la dieta a partir de semillas de momordica charantia Linn

Phytoestrogens are secondary plant metabolites produced by plants that are similar in structure of estrogen. Human consumption of these compounds has been associated with many health benefits. In this study, we investigated the potential phytoestrogen content of dietary Momordica charantia Linn. (Bitter melon) seeds were collected from the Hyderabad-Karnataka regions of India. A phenolic dietary phytoestrogen has been isolated from the crude ethanol extract of Bitter melonseeds. After preparative HPLC whitish amorphous compound was yielded. The HPLC purified compound is subjected to spectral analysis using IR, NMR and MS. The spectral data revealed that the phenolphthalein a phytoestrogenic molecule is present in the ethanol extract of dietary Bitter melonseeds.

Los fitoestrógenos son metabolitos vegetales secundarios, producidos por plantas que tienen una estructura similar al estrógeno. El consumo humano de estos compuestos se ha asociado con muchos beneficios para la salud. En este estudio, investigamos el contenido potencial de fitoestrógenos de Momordica charantia Linn en la dieta. Se recolectaron semillas (melón amargo) de las regiones de Hyderabad-Karnataka de la India. Se ha aislado un fitoestrógeno dietético fenólico del extracto de etanol crudo de semillas de melón amargo. Después de HPLC preparativa, se obtuvo un compuesto amorfo blanquecino. El compuesto purificado por HPLC se somete a análisis espectral usando IR, NMR y MS. Los datos espectrales revelaron que la fenolftaleína, una molécula fitoestrogénica, está presente en el extracto etanólico de las semillas de melón amargo en la dieta.

Preparation and evaluation of azithromycin-loaded microspheres for oral administration / 中国药科大学学报

@#To mask the bitterness of azithromycin（AZI） and improve patient compliance, an AZI-loaded microsphere (AZI-EC MS) for oral administration was prepared by O/W emulsion solvent evaporation with ethylcellulose (EC) as carrier. The release profiles and taste-masking effect of AZI-EC MS were preliminarily assessed. Its physical properties and morphology were then investigated by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The results indicated that the polymer weight of EC could influence the drug release behavior. With a drug polymer ratio of 1∶1 and mixed EC (N22/T10, 7∶3) as carrier, the cumulative release of AZI-EC MS at 0.5 h was less than 40% and reached 90% at 8 h; the drug loading efficiency of microspheres was (48.95 ± 0.86)% with smooth spherical morphology. The AZI bitterness threshold is 9.93 μg/mL with a strong bitter taste, which indicated a better taste masking effect. Therefore, AZI-EC MS prepared in this study can mask AZI bitterness and improve patient compliance, setting the stage for the research of new AZI preparations.

Structure-activity relationship of coptis alkaloid bitterness inhibited by mPEG-PLLA / 中国中药杂志

Inhibition of bitterness is a significant measure to improve the compliance and clinical efficacy of traditional Chinese medicine(TCM) decoction. According to the characteristics of TCM decoction, such as high dispersion of bitterness components, multi-component bitterness superposition and strong instantaneous stimulation, the research group put forward a new strategy to inhibit bitterness in the early stage based on the self-assembly characteristics of amphiphilic substances in aqueous solution, in order to reduce the distribution of bitterness components in real solution and achieve the purpose of bitter-masking. It was found that the bitter-masking effect of amphiphilic substances was different on the bitter compounds of various structures. Therefore, it was speculated that there might be a certain relationship between the bitter inhibition effect and the substrate structure. In this paper, the interaction between mPEG-PLLA and five bitter alkaloids(bamatine, jatrorrhizine, berberine, epiberberine and coptisine) in Coptidis Rhizoma was studied to explore the effect of substrate structure on the inhibition of bitterness. The sensory test of volunteers was used to determine the bitter-masking effect of mPEG-PLLA on the decoction of Coptidis Rhizoma and its main bitter alkaloids. The molecular docking and molecular force field were applied to locate the bitter groups and the bitter-masking parts. The relationship between the bitter strength and the structure was analyzed by the surface electrostatic potential of the bitter alkaloids, and the correlation between the bitter-masking effect and the structural parameters of the bitter components was explored by factor analysis, so as to clarify the structure-activity relationship of mPEG-PLLA in masking the bitterness of coptis alkaloids. It was found that mPEG-PLLA had significant taste masking effect on the decoction of Coptidis Rhizoma and five alkaloids. The masking effect was obviously related to the structure of different alkaloids: the effect increased with the increase of the number of hydrogen donors, rotatable bonds, molecular weight, and hydrophobicity, and decreased with the increase of surface electrostatic potential, electrophilicity and binding energy with bitter receptors. In this study, the influence of alkaloid structure of Coptidis Rhizoma on the butter-masking effect of mPEG-PLLA was preliminarily elucidated, providing a scientific basis for better exerting the bitter-masking effect of amphiphilic block copolymers.

Chemical components and pharmacological action for Euodiae Fructus and predictive analysis on its Q-marker / 中草药

Euodiae Fructus is one of the most commonly used traditional Chinese medicinal materials with rich resource and wide distribution. It has broad prospects for development and utilization. The chemical constituents of Euodiae Fructus are abundant, including alkaloids, bitter principles, volatile oils, flavonoids and so on. Traditionally, the alkaloids and bitter principles are considered as its main pharmacodynamic components. Based on the review of its chemical composition and pharmacological action of herbal medicine, according to the theory of quality marker, the quality maker of Euodiae Fructus were predicted from the aspects of source, chemical composition and traditional efficacy, traditional medicinal properties, new clinical uses, and toxicity, measurable ingredients, blood-entering ingredients and different compatible environments, which provide a basis for defining quality markers and formulating scientific quality standards of Euodiae Fructus.

Intervening effects of lupulone and humulone in humulus lupulus l. On osteoblasts and osteoclasts of rats / 第二军医大学学报

Objective To explore the effects of lupulone (LUP) and humulone (HUM) in Humulus lupulus L. on osteoblasts and osteoclasts of rats. Methods Osteoblasts and osteoclasts isolated from 24-h-old Wistar rats were studied and divided into control group, LUP-treated low (10－15 mol/L)-, medium (10－14mol/L)-and high (10－13 mol/L)-dose groups, and HUM-treated low (10－15 mol/L)-, medium (10－14 mol/L)-and high (10－13mol/L)-dose groups. After drug treatment, the proliferation, differentiation and bone mineralization of osteoblasts were determined by MTT assay, alkaline phosphatase (ALP) activity assay and alizarin red staining, respectively. Osteoclasts were counted and tartrate-resistant acid phosphatase (TRAP) activity was measured to evaluate the effects of LUP and HUM on the activity of osteoclasts. Osteocalcin (OCN) levels were measured by kit assay, and the expression levels of bone formation related proteins osteopontin (OPN), bone sialoprotein (BSP), bone morphogenetic protein 2 (BMP-2), bone resorption related proteins cathepsin K (CK) and matrix metalloproteinase 9 (MMP-9) were measured by Western blotting analysis to evaluate the effects of LUP and HUM on bone metabolism. Results At the osteoblast level, LUP at dosages of 10－15 and 10－14 mol/L could significantly promote the cell proliferation (P0.05). LUP at dosages of 10－14 and 10－13 mol/L could significantly improve ALP activity and bone mineralization (P0.05, P0.01). LUP at dosage of 10－13 mol/L could significantly induce the expression of OCN (P0.01). Furthermore, LUP at dosages of 10－14 and 10－13 mol/L could significantly increase the expression of BSP and BMP-2 (P0.05). HUM at dosages of 10－15-10－13 mol/L could also significantly promote the osteoblastic proliferation, ALP activity and bone mineralization (P0.01), and could significantly increase the expression of OCN and OPN (P0.05, P0.01). Additionally, HUM at dosages of 10－14 and 10－13 mol/L could significantly increase the expression of BSP and BMP-2 (P0.05). At the osteoclast level, both LUP and HUM at dosages of 10－15-10－13 mol/L could significantly reduce the number of osteoclasts (P0.01) and could significantly inhibit the expression of CK (P0.05, P0.01). HUM at dosages of 10－15-10－13 mol/L could also significantly inhibit the expression of MMP-9 (P0.05, P0.01). Conclusion This study preliminarily clarifies that LUP and HUM can prevent bone loss by promoting bone formation and inhibiting bone resorption, which provides a new reference for the development of osteoporosis drugs.

Nature-effect relationship research of Salviae Miltiorrhizae Radix et Rhizoma and Carthami Flos based on nature combination / 中国中药杂志

Salviae Miltiorrhizae Radix et Rhizoma and Carthami Flos are commonly traditional Chinese medicines with invigorating blood circulation and eliminating blood stasis,but they are different in effects due to differences in five tastes and four properties. In this study,Salviae Miltiorrhizae Radix et Rhizoma and Carthami Flos are selected as research vectors to obtain the active ingredients and targets through TCMD,TCMSP database and Ch EMBL database. The protein interaction information of the target is used to obtain from STRING online database,then imported into Cytoscape software to plot the protein interaction network and perform GO enrichment analysis.The results show that the heart-liver protein interaction network,involving blood circulation and hepatic lipid metabolism,thereby exerting the effect of activating blood circulation. The cold-bitter protein interaction network involves the biological process of vasoconstriction,thereby exerting cooling blood and the efficacy of eliminating phlegm. The warm-pungent protein interaction network involves blood coagulation,lipid metabolism and other biological processes to play the role of phlegm pain. Through analysis,it is found that the relationship between pharmacological efficacy and medicinal properties has a certain degree of specificity,which facilitates the subsequent scientific and systematic study of medicinal properties on the basis of this study.

Correlation study on Tibetan medicine Pterocephalus hookeri of bitter taste receptors based on molecular docking technology / 中国中药杂志

In order to study the interaction between Pterocephalus hookeri and bitter taste receptors,three-dimensional structural models of bitter taste receptors TAS2 R16,TAS2 R14 and TAS2 R13 were established by homology modeling in this paper. Maestro software was used for docking the chemical constituents of P. hookeri with bitter taste receptors. The results showed that 25 chemical components of P. hookeri can regulate three bitter taste receptors. And these components were mainly iridoid glycosides and phenolic acids.This research focused on the comprehensive application of homology modeling and molecular docking technology to explore the interaction between bitter chemical constituents of P. hookeri and bitter taste receptors. This study provided assistance in revealing pharmacodynamic basis of bitter Tibetan medicine at molecular level. It also provided new ideas and methods for the study of Tibetan medicine.