玛咖对维甲酸诱导的骨质疏松症的抑制作用

目的:探讨云南首次引种植物玛咖对维甲酸诱导的骨质疏松症的缓解作用。方法:维甲酸(70mg/kg)给药诱导15d建立SD大鼠骨质疏松模型,以云南种植玛咖块根的95%乙醇提取物(0.48 g/kg,0.24 g/kg,0.12 g/kg)给药至第30d,取腰椎骨切片做HE染色,测右股骨骨密度,测定血清中碱性磷酸酶(AKP)、抗酒石酸酸性磷酸酶(TRAP)、及雌二醇(E2)活性。结果:云南种植玛咖的95%乙醇提取物3个剂量组(0.48 g/kg,0.24 g/kg,0.12 g/kg)均能够有效改善维甲酸引起的骨小梁稀疏、断裂及骨小梁间距变宽等现象,升高骨密度,降低碱性磷酸酶及抗酒石酸酸性磷酸酶活性并能显著升高雌二醇水平。结论:云南引种玛咖的95%乙醇提取物对维甲酸诱导的骨质疏松症有较好的抑制作用。     

玛咖对虚寒及虚热证大鼠环核苷酸水平及神经-内分泌-免疫网络的影响

研究玛咖对虚寒及虚热证大鼠环核苷酸、神经递质水平、下丘脑-垂体-肾上腺轴及免疫功能的影响,探讨玛咖的寒热药性。SD大鼠分为空白组、虚寒模型组、虚寒肉桂组(30 g·kg-1)、虚寒玛咖高剂量组(2.4 g·kg-1)、虚寒玛咖低剂量组(1.2 g·kg-1)、虚热模型组、虚热黄柏组(5 g·kg-1)、虚热玛咖高剂量组(2.4 g·kg-1)、虚热玛咖低剂量组(1.2 g·kg-1);采用每日肌肉注射氢化可的松琥珀酸钠、地塞米松磷酸钠注射液1次,连续21 d的方法制备虚寒、虚热证动物模型;通过放免法检测环磷酸腺苷(cAMP)、环磷酸鸟苷(cGMP)、去甲肾上腺素(NE)、多巴胺(DA)、5-羟色胺(5-HT)、促肾上腺皮质激素释放激素(CRH)、促肾上腺激素释放激素(ACTH)、皮质酮(CORT)、免疫球蛋白M(IgM)、免疫球蛋白G(IgG)、补体3(C3)、补体4(C4)含量变化。玛咖高剂量组和玛咖低剂量组均能使虚寒证大鼠整体状态及体质量得到明显改善(P<0.01,P<0.05),使cAMP,cAMP/cGMP,NE,DA,ACTH均明显升高(P<0.01,P<0.001),而5-HT明显降低(P<0.01,P<0.001);虚热玛咖高剂量组、低剂量组的体质量,cAMP,cAMP/cGMP,NE,DA,5-HT,ACTH无统计学意义;玛咖对虚寒、虚热证大鼠的CORT,IgM,IgG,C3含量均有显著调节作用(P<0.01,P<0.05,P<0.001)。玛咖对大鼠体质量、环核苷酸、神经递质水平及HPA轴的调整与肉桂一致,与黄柏相反;对机体免疫功能有双向调节作用;用药理学实验方法通过同类比较、异类反证,从对环核苷酸水平和神经-内分泌-免疫网络的影响证实玛咖药性微温。     

Dose-response effects of Lepidium meyenii (Maca) aqueous extract on testicular function and weight of different organs in adult rats

Lepidium meyenii (Brassicaceae) known as Maca grows exclusively between 4000 and 4500 m over the sea level in the Peruvian central Andes. The dried hypocotyls of Maca are traditionally used as food and for its supposed fertility-enhancing properties. A dose-response study was performed to determine the effect of 7 days oral administration of an aqueous lyophilized extract of Maca at 0.01-5 g/kg (corresponding to 0.022-11 g dry hypocotyls of Maca/kg) on body and different organ weights, stages of the seminiferous tubules, epididymal sperm count and motility, and serum testosterone and estradiol levels in rats. In doses up to 5 g extract/kg, no toxicity was observed. Almost all organ weights were similar in controls and in the Maca extract-treated groups. Seminal vesicles weight was significantly reduced at 0.01 and 0.10 g extract/kg. Maca increased in length of stages VII-VIII of the seminiferous tubules in a dose-response fashion, with highest response at 1.0 g/kg, while caput/corpus epididymal sperm count increased at the 1.0 g dose. Cauda epididymal sperm count, sperm motility, and serum estradiol level were not affected at any of the doses studied. Serum testosterone was lower at 0.10 g extract/kg. Low-seminal vesicle weights correlated with low-serum testosterone levels (R2=0.33; P<0.0001) and low-testosterone/estradiol ratio (R2=0.35; P<0.0001). Increase in epididymal sperm count was related to lengths of stages VII-VIII. Highest effect on stages VII-VIII of the seminiferous tubules was observed at 1.0 g Maca aqueous extract/kg. The present study demonstrated that Maca extract in doses up to 5 g/kg (equivalent to the intake of 770 g hypocotyls in a man of 70 kg) was safe and that higher effect on reproductive parameters was elicited with a dose of 1 g extract/kg corresponding to 2.2 g dry Maca hypocotyls/kg.     

Protective Effects of Lepidium meyenii (Maca) Aqueous Extract and Lycopene on Testosterone Propionate‐Induced Prostatic Hyperplasia in Mice

The inhibitory effect of maca extractant, lycopene, and their combination was evaluated in benign prostatic hyperplasia (BPH) mice induced by testosterone propionate. Mice were divided into a saline group, solvent control group and testosterone propionate‐induced BPH mice [BPH model group, solvent BPH model group, benzyl glucosinolate group (1.44 mg/kg), maca group (60 mg/kg), lycopene treated (15, 5, and 2.5 mg/kg), maca (30 mg/kg) combine lycopene treated (7.5, 2.5, and 1.25 mg/kg), and finasteride treated]. Benzyl glucosinolate was used in order to evaluate its pharmacological activity on BPH to find out whether it is the major active component of maca aqueous extract. Finasteride was used as positive control. The compounds were administered once for 30 successive days. Compared with solvent BPH model group, BPH mice fed with maca (30 mg/kg) and lycopene (7.5 mg/kg) combination exhibited significant reductions in the prostatic index, prostatic acid phospatase, estradiol, testosterone, and dihydrotestosterone levels in serum. They also had similar histological compared with those aspects observed in the mice in the solvent control group. The results indicated that combination of maca and lycopene synergistically inhibits BPH in mice. Copyright © 2017 John Wiley & Sons, Ltd.     

秘鲁特产药用植物玛卡研究的新进展

对近5年来秘鲁特产药用植物玛卡的研究进展作了简要综述，内容包括玛卡的生物学及生态学研究、化学成分研究、药理作用研究以及临床应用研究。玛卡的药理作用及保健功能日益受到瞩目和关注。     

玛咖提取物的激素样活性实验研究

目的初步研究玛咖提取物的激素样活性作用。方法采用雄性去势小鼠，经灌胃玛咖不同提取物22d后，观察各组小鼠前列腺和精囊腺的重量并测定血清中睾丸酮的含量。用幼龄雌性小鼠，灌胃玛咖醇提物10d后，观察各组小鼠子宫、卵巢重量以及阴道上皮角化细胞。结果玛咖提取物可以显著提高雄性去势小鼠前列腺和精囊腺重量，但并不升高血清睾丸酮水平。玛咖醇提取物对雌性幼年小鼠子宫、卵巢重量以及阴道上皮角化细胞没有显著影响。结论玛咖具有弱的雄激素样作用，但对幼年雌性小鼠未显示雌激素样活性。     

Effect of short-term and long-term treatments with three ecotypes of Lepidium meyenii (MACA) on spermatogenesis in rats

Lepidium meyenii (Brassicaceae), known as Maca, is a Peruvian hypocotyl that grows exclusively between 4000 and 4500 m above sea level in the central Andes. Maca is traditionally employed in the Andean region for its supposed fertility-enhancing properties. The study aimed to test the hypothesis that different ecotypes of Maca (Red, Yellow and Black) after short-term (7 days) and long-term (42 days) treatment affects differentially spermatogenesis adult rats. After 7 days of treatment with Yellow and Red Maca, the length of stage VIII was increased (P<0.05), whereas with Black Maca stages II-VI and VIII were increased (P<0.05). Daily sperm production (DSP) was increased in the group treated with Black Maca compared with control values (P<0.05). Red or Yellow Maca did not alter DSP and epididymal sperm motility was not affected by treatment with any ecotype of Maca. After 42 days of treatment, Black Maca was the only ecotype that enhanced DSP (P<0.05). Moreover, Black Maca was the only that increased epididymal sperm motility (P<0.05). In relation to the control group, Red Maca did not affect testicular and epididymal weight nor epididymal sperm motility and sperm count; however, prostate weight was reduced (P<0.05). Black or Yellow Maca did not affect prostate weight. In conclusion, there were differences in the biological response of the three ecotypes of Maca (Yellow, Red and Black). Black Maca appeared to have more beneficial effect on sperm counts and epididymal sperm motility.     

玛咖质量标准研究

为了建立玛咖定性、定量标准,参照2010年版药典附录相关方法,分别对玛咖的水分、浸出物、总灰分、酸不溶成分、重金属含量进行了测定;以玛咖中特征性酰胺类成分亚油酰胺为指标性成分,分别采用TLC和HPLC进行定性鉴别和含量测定研究。结果显示,玛咖中亚油酰胺的薄层色谱鉴别特征明显,专属性强;含量测定线性范围为0.01~2.00 μg(r=0.999 8),平均回收率(n=9)为99.27%(RSD 2.0%) 。所建立的玛咖定性鉴别和定量测定方法简单准确,能够为玛咖的质量控制提供有效数据。     

药用植物玛咖研究新进展

玛咖作为国际保健品市场的明星产品之一,具广泛应用价值,且可向全球推广种植,但目前玛咖的基础研究尚不深入,缺乏系统化学成分及明确药效活性研究,市场产品多围绕其壮阳功效予以夸大宣传,极大影响了对该植物进行更为系统深入的研究探索。该文对近几年药用植物玛咖的资源现状、生长栽培、植物化学成分、药理药效等方面进行了阐述,旨在为合理开发利用玛咖提供参考。     

Screening for in vivo (anti)estrogenic and (anti)androgenic activities of Tropaeolum majus L. and its effect on uterine contractility

Ethnopharmacological relevance

Tropaeolum majus L. (Tropaeolaceae) is a medicinal herb popularly used in Brazil for treatment of inflammatory and cardiovascular diseases. Despite some published data on its efficacy, there are still few toxicological data describing the safety of this plant. The aim of this study was to evaluate the (anti)estrogenic and (anti)androgenic activity of the hydroethanolic extract obtained from Tropaeolum majus L. (HETM), as well as its possible effects on uterine contractility.

Materials and methods

Three experimental protocols were performed, (a) uterotrophic assay, (b) Hershberger assay and (c) an ex vivo test to investigate the effects of maternal administration of HETM on uterine contractility at the end of pregnancy. In all protocols three doses of the HETM were administered to Wistar rats: 3, 30 and 300 mg/kg.

Results

In vivo tests for detection of (anti)androgenic and (anti)estrogenic activities did not show any significant alterations. Similarly, no alterations were observed on uterine contractility induced by oxytocin and arachidonic acid.

Conclusions

HETM was unable to produce (anti)estrogenic or (anti)androgenic activities in the short-term in vivo screening assays performed. In addition, there was no evidence that HETM can affect uterine contractility following gestational exposure of rats.     

中国十字花科独行菜属植物的叶表皮特征研究

目的:对中国十字花科独行菜属植物进行分类鉴别研究。方法:利用光学显微镜和扫描电镜观察了中国十字花科独行菜属10种植物的叶表皮形态。结果:独行菜属植物气孔器在叶上、下表皮均有分布,气孔类型主要为不等细胞型,其次为无规则型,在少数植物种类中偶见平列型;叶表皮细胞形状为多边形或不规则形,垂周壁一般为平直或弓形、浅波、波状;独行菜属植物在叶表皮特征上具有较强的一致性,同一种植物叶上、下表皮同形或近同形,叶表面仅被单毛或无毛;扫描电镜下叶片角质层通常具有条状波纹,气孔外拱盖内缘通常为浅波状或近平滑。叶表皮细胞形态、垂周壁式样、气孔类型、气孔指数与气孔器大小以及叶片角质层特征等对该属种的区分具有重要的参考价值。结论:叶表皮特征研究可用于中国独行菜属种间分类鉴别研究,为该属药用植物资源的合理应用和开发提供了新的依据。     

Lepidium meyenii (Maca) enhances the serum levels of luteinising hormone in female rats

Ethnopharmacological relevance

Lepidium meyenii (Maca) is traditionally employed in the Andean region for its supposed fertility benefits. This study investigated the effect of Maca on the serum pituitary hormone levels during the pro-oestrus phase.

Materials and methods

Maca powder was made from the tubers of Lepidium meyenii Walp collected, dried, and reduced to powder at the plantation in Junín Plateau and was purchased from Yamano del Perú SAC. The Maca powder was identified by chemical profiling and taxonomic methods. Two groups of female Sprague-Dawley rats were provided feed with normal feed containing 5%, 25%, or 50% Maca powder ad libitum for 7 weeks. At 1800 h of the proestrus stage, the rats were euthanised, and blood samples were collected for serum isolation. The serum pituitary hormone levels were measured using enzyme-linked immunosorbent assays (ELISAs).

Results

No significant differences in feed intake or growth rate were observed among the rats. During the pro-oestrus stage, a 4.5-fold increase (P<0.01) in luteinising hormone (LH) and a 19-fold increase (P<0.01) in follicle-stimulating hormone (FSH) were observed in the sera of rats fed with 50% Maca powder compared with the control rats. No significant differences were observed in the levels of the other pituitary hormones, including growth hormone (GH), prolactin (PRL), adrenocorticotropic hormone (ACTH), and thyroid-stimulating hormone (TSH). A dose-dependent increase of LH serum levels was observed within the range of 3–30 g Maca/kg. Furthermore, the enhancement of the LH serum levels was specific to the pro-oestrus LH surge.

Conclusions

The present study demonstrates that Maca uniquely enhances the LH serum levels of pituitary hormones in female rats during the pro-oestrus LH surge and acts in a pharmacological, dose-dependent manner. These findings support the traditional use of Maca to enhance fertility and suggest a potential molecular mechanism responsible for its effects.     

黑玛咖不同提取物的抗疲劳作用与谱效关系研究

目的研究黑玛咖不同提取物的抗疲劳作用及其超高效液相色谱(UPLC)图谱与抗疲劳作用的谱效关系,为明确黑玛咖的抗疲劳作用的物质基础提供依据。方法通过小鼠力竭游泳实验、检测肝糖原和血清乳酸水平,比较黑玛咖8种提取物的抗疲劳作用;采用UPLC-Q-TOF/MS法建立黑玛咖8种提取物的指纹图谱;以小鼠力竭游泳实验为抗疲劳作用的药效学指标,采用偏最小二乘法回归(PLSR)分析建立其谱效关系。结果黑玛咖60%、80%、95%乙醇提取物(醇提物)均明显增加小鼠力竭游泳时间,且以95%醇提物增加作用更为显著;黑玛咖80%醇提物能显著增加因过度运动所致的降低的肝糖原水平;黑玛咖95%醇提物能明显减少小鼠负重游泳后产生的血清乳酸堆积。从黑玛咖不同提取物UPLC指纹图谱中提取出23个能够表征含量差异的特征峰。采用PLSR分析,以力竭游泳时间为药效指标时,发现黑玛咖提取物中N-苄基十六酰胺、N-苄基-5-氧代-6E,8E-十八碳二烯酰胺、1,3-二苄基-2-苯基-4,5-二甲基咪唑和N-十八烷酰胺与抗疲劳作用呈正相关,且VIP值大于1。结论黑玛咖95%及80%醇提物具有显著的抗疲劳作用;明确N-苄基十六酰胺、N-苄基-5-氧代-6E,8E-十八碳二烯酰胺、1,3-二苄基-2-苯基-4,5-二甲基咪唑和N-十八烷酰胺是黑玛咖抗疲劳作用的主要有效成分。为深入研究黑玛咖抗疲劳药效物质基础及建立全面可靠的质量控制方法提供思路。     

Mosquitocidal activities of octacosane from Moschosma polystachyum Linn (lamiaceae)

The toxicity of the plant Moschosma polystachyum was evaluated against mosquito Culex quinquefasciatus. The crude leaf extract and active compound octacosane showed negligible mortality against early third instar larvae of Culex quinquefasciatus. The 24 h LC(50) value was observed at 153.2+/-1.3 mg/l and 7.2+/-1.7 mg/l for crude leaf extract and active compound octacosane, respectively. The repellent activity of active compound octacosane at 1.0 and 2.5 mg/cm(2) concentration gave 85.2+/-1.7 min and 54.6+/-2.3 min protection, respectively. The total percentage protection of octacosane was 96.2+/-0.9 at 2.5 mg/cm(2) and 86.4+/-1.3 at 1.0 mg/cm(2) concentration.     

Antinociceptive and anti-inflammatory activities of Acacia pennata wild (Mimosaceae)

The butanolic fraction of dried leaves of Acacia pennata (Mimosaceae) was tested for analgesic and anti-inflammatory activities in animal models. It showed significant protective effects against chemical stimuli (acetic acid and formalin) in the mouse. It also produced a significant increase of the threshold of sensitivity to pressure-induced pain in the rats. The extract revealed an inhibitory effect in carrageenin-induced rat paw oedema in the late phase. The results suggested that a peripheral mechanism is involved in the analgesic, associated to anti-inflammatory effect (NSAIDs-like). Among the class of compounds characterized in this fraction, flavonoids may be mainly responsible for the pharmacological activities.     

Antifungal activities of six South African Terminalia species (Combretaceae)

A serial microplate dilution method developed for bacteria was modified slightly and gave good results with several fungi. The antifungal activity of acetone, hexane, dichloromethane and methanol leaf extracts of six Terminalia species (Terminalia prunioides, Terminalia brachystemma, Terminalia sericea, Terminalia gazensis, Terminalia mollis and Terminalia sambesiaca) were tested against five fungal animal pathogens (Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Microsporum canis and Sporothrix schenkii). Methanol extracted the highest quantity, but the acetone extracts had the highest antifungal activity. Some of the extracts had antioxidant activity. Most of the antifungal extracts had MIC values of c. 0.08 mg/ml, some were with MIC values as low as 0.02 mg/ml. Microsporum canis was the most susceptible microorganism and Terminalia sericea extracts were the most active against nearly all microorganisms tested.     

Antioxidant and antihepatotoxic activities of Phellinus rimosus (Berk) Pilat

The antioxidant and antihepatotoxic activities of a wood inhabiting macrofungus, Phellinus rimosus were studied. The superoxide anion scavenging, Fe(2+)-ascorbate induced lipid peroxidation inhibiting, hydroxyl radical scavenging and nitric oxide scavenging activities of the ethyl acetate extract were determined. The results indicated that ethyl acetate extract of P. rimosus exhibited significant in vitro antioxidant activity. The ethyl acetate extract of P. rimosus also showed potent antihepatotoxic activity against carbontetrachloride-induced acute toxicity in rat liver. The amelioration of liver toxicity by the ethyl acetate extract was evident from its significant effect on the levels of serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and serum alkaline phosphatase (ALP). The results suggest that hepatoprotective effect of P. rimosus is possibly related to the free radical scavenging activity.     

Nigella sativa (black seed) oil does not affect the T-helper 1 and T-helper 2 type cytokine production from splenic mononuclear cells in allergen sensitized mice

Nigella sativa Linn. (Ranunculaceae) is known to have beneficial effects on a wide range of diseases including asthma. However, the mechanism of action in asthma and other allergic diseases is not entirely clear. The present study was planned to evaluate the effects of Nigella sativa on cytokine production of splenic mononuclear cells in ova-sensitized mice. Nineteen two-month-old BALB/c mice were given 0.3 mL of Nigella sativa oil by oro-eosophageal cannula once a day for a month. The control group consisting of 10 mice took 0.3 mL of 0.9% saline solution by the same route for the same period. In the third week of the study, all mice were sensitized by means of intraperitoneal injections of 20 μg of ovalbumin (OVA-Grade VI, Sigma). Ova injections were repeated three times with 7-day intervals. After another week, all mice were sacrificed by means of cervical dislocation. Then the splenic mononuclear cells (MNCs) of mice were cultured with OVA or Concavalin A (Con-A). From the culture supernatants, IL-4, IL-10 and IFN-γ were assessed by means of ELISA. The cytokine production of splenic MNCs of mice that were given Nigella sativa for 30 days was not significantly different than those who took saline solution instead. In conclusion, Nigella sativa oil seems not to have an immunomodulatory effect on Th1 and Th2 cell responsiveness to allergen stimulation.     

Pharmacological activities of extracts of Daniellia oliveri (Rolfe) Hutch. and Dalz. (Leguminosae)

Extracts of the stem bark of Daniellia oliveri using hexane, ethyl acetate and methanol were tested for analgesic, antipyretic and antiinflammatory activities. The hexane extract exhibited a dose related analgesic activity whilst the methanolic extract was active in the induced inflammatory condition. The ethyl acetate extract was relatively inactive and none of the extracts showed any antipyretic activity. Metabolic cage studies showed that a 70% ethanolic extract of the bark caused significant decreases in body weight, food intake, urine and stool output of rats. This extract also exhibited a competitive antagonism on histamine-induced contractions of the guinea-pig ileum and a non-competitive inhibition of acetyl choline-induced contraction of the frog rectus abdominis muscle.     

Antimalarial activities of Tithonia diversifolia (Asteraceae) and Crossopteryx febrifuga (Rubiaceae) on mice in vivo

Ethanolic extracts of the aerial part of Tithonia diversifolia and the stem bark of Crossopteryx febrifuga were investigated against early, residual (repository) and established malaria infections in vivo using Swiss albino mice at a dose range of 50-400 mg/kg per day. Chloroquine at 5 mg/kg per day was used as the positive control for the early and established infections while Pyrimethamine at 1.2 3/kg per day was used as the positive control for the residual infection test. Dose dependent chemo suppressive activities were obtained at the different levels of the infection tested. Tithonia diversifolia and Crossopteryx febrifuga gave some level of suppression of parasitaemia in the early and established infection stages. Tithonia diversifolia was active at 200 mg/kg per day in the repository test. The mean survival period of the mice treated with the extract in the established infection test was low, a possible indication of toxicity as a result of sub chronic administration of the extract. Crossopteryx febrifuga was inactive in the repository test. Beside the above limitations, the suppression of parasitaemia by the extracts at the highest dose was similar to chloroquine and pyrimathamine.