Antimycobacterial terpenoids from Juniperus communis L. (Cuppressaceae)

Ethnopharmacological relevance

Juniperus communis is a plant which has been reported as a traditional cure for tuberculosis (TB) and other respiratory diseases.

Aim of the study

The aim of this study was to isolate and identify the constituents responsible for the activity of the n-hexane extract of Juniperus communis roots against Mycobacterium tuberculosis H₃₇Rv and Juniperus communis aerial parts against Mycobacterium aurum. Subsequently, it was to evaluate the activity of the pure isolated compounds against (i) drug-resistant Mycobacterium tuberculosis variants, (ii) non-replicating Mycobacterium tuberculosis and (iii) a range of non-tuberculous mycobacteria (NTM).

Materials and methods

The antimycobacterial activity of Juniperus communis extracts, fractions and constituents was determined against Mycobacterium tuberculosis H₃₇Rv, and against rifampicin-, isoniazid-, streptomycin- and moxifloxacin-resistant variants, using the microplate broth Alamar Blue assay (MABA) method. Isolated constituents were tested against non-replicating Mycobacterium tuberculosis H₃₇Rv, using the low oxygen recovery assay (LORA), and against NTM (Mycobacterium aurum, Mycobacterium phlei, Mycobacterium fortuitum and Mycobacterium smegmatis), using a broth microdilution method. Cytotoxicty studies were performed using mammalian Vero cells.

Results

The antimycobacterial activity of Juniperus communis was attributed to a sesquiterpene identified as longifolene (1) and two diterpenes, characterised as totarol (2) and trans-communic acid (3). All compounds were identified following analysis of their spectroscopic data (1D- and 2D-NMR, MS) and by comparison with the literature and commercial authentic standards when available. Revised assignments for 3 are reported. Totarol showed the best activity against Mycobacterium tuberculosis H₃₇Rv (MIC of 73.7 μM). It was also most active against the isoniazid-, streptomycin-, and moxifloxacin-resistant variants (MIC of 38.4, 83.4 and 60 μM, respectively). Longifolene and totarol were most active against the rifampicin-resistant variant (MICs of 24 and 20.2 μM, respectively). Totarol showed the best activity in the LORA assay (MIC of 81.3 μM) and against all NTM species (MICs in the range of 7–14 μM). Trans-communic acid showed good activity against Mycobacterium aurum (MIC of 13.2 μM). The low selectivity indices (SI) obtained following cytotoxicity studies indicated that the isolated terpenoids were relatively toxic towards mammalian cells. This is the first report of the isolation of (1) and (2) from Juniperus communis roots, and of (3) from the aerial parts. The antimycobacterial activity of (1) and (3), and the activity of (2) against Mycobacterium aurum, Mycobacterium fortuitum and Mycobacterium phlei, is reported for the first time. The effect of totarol on drug-resistant variants and non-replicating Mycobacterium tuberculosis has never been published.

Conclusions

The presence of antimycobacterial terpenoids in Juniperus communis aerial parts and roots justifies, to some extent, the ethnomedicinal use of this species as a traditional anti-TB remedy.     

Immobilization effect of Ruta graveolens L. on human sperm: a new hope for male contraception

AIM OF THE STUDY: Contraceptive plants which were introduced by folk in traditional remedies are investigated worldwide. In this study, the contraceptive effects of Ruta graveolens L., which has been mentioned for male contraceptive in Iranian traditional folk medicine, was experimented on human sperm. MATERIALS AND METHODS: Different doses of lyophilized aqueous extract of Ruta graveolens L. were added to an amount of fresh semen, containing 10(6) cells in a 1:1 volumic ratio. Motility and viability of cells, DNA status, mitochondrial activity and sperm revival tests were carried out. RESULTS: The sperm immobilization effects of the extract appeared immediately in a does-dependent manner and 100% of the sperms became immotile at a concentration of 100mg/ml but other parameters were intact. After washing the sperms, motility was returned in 30.8+/-3.2% of the sperms, besides coiled tails in 38.6+/-5.5% of the treated cells, in comparison to 12.5+/-2.0% of the control group (p=0.001). The part of the extract, responsible for immobilization of the sperms was stable upon boiling. CONCLUSIONS: As the cells were alive and immotile, probably some ionic currents are blocked by a thermostable component of the plant which can be promising as a new male channel blocker contraceptive.     

鸭跖草的化学成分研究

利用常规柱色谱及半制备高效液相色谱等手段相结合对鸭跖草化学成分进行分离纯化,从鸭跖草中分离得到15个化合物,根据其NMR和MS等光谱数据以及理化性质鉴定化合物结构,所分化合物分别鉴定为柯伊利素-7-O-β-D-葡萄糖苷(1),没食子酸甲酯(2),对香豆酸(3),原儿茶酸(4),咖啡酸(5),对羟基苯甲酸(6),2-苯乙基-β-D-葡萄糖苷(7),土大黄苷(8),(7S,8R)-dihydrodehydrodiconiferyl alcohol-9-O-β-D-glucoside(9),异牡荆素(10),芹菜素-6-C-α-L-鼠李糖苷(11),isorhamnetin-3-O-β-D-glucoside(12),槲皮素-3-O-α-L-鼠李糖苷(13),异槲皮素(14),1,2-dihydro-6,8-dimethoxy-7-1-(3,5-dimethoxy-4-hydroxyphenyl)-N¹,N²-bis-[2-(4-hydroxyphenyl)ethyl]-2,3-naphthalene dicarboxamide(15).化合物 2,5-9,11,13 等8个化合物为首次从鸭跖草属中分离得到.     

HPLC测定不同生长期鸭跖草中异荭草素的含量

目的:研究中药鸭跖草中黄酮类成分异荭草素的含量测定方法,并比较不同生长期鸭跖草中异荭草素的含量,以确定最佳采收期。方法:采用AgilentTC-C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-0.1%磷酸溶液(15∶85)为流动相,流速1mL·min-1,紫外检测器检测。结果:异荭草素的线性范围0.08～1.00μg,平均回收率101.2%,不同生长期对样品的异荭草素含量有显著影响,成熟期含量最高。结论:该方法便捷、有效,适用于检测鸭跖草中异荭草素含量,为其质量标准的制定提供依据,对确定鸭跖草的最佳采收期提供参考。     

Vasorelaxant effects and mechanisms of action of Heracleum sphondylium L. (Apiaceae) in rat thoracic aorta

Ethnopharmacological relevance

Aerial parts of Heracleum sphondylium L. (HS) are used in traditional medicine to treat hypertension. To provide pharmacological basis for this use, we investigated the vasorelaxant effects of a dichloromethane extract of HS (HSDE) and the mechanisms involved.

Materials and methods

Activity of HSDE was evaluated on rat isolated thoracic aortic rings.

Results

HSDE induced vasorelaxation in phenylephrine (PE, 10⁻⁶ mol/L) and high KCl—(6×10⁻² mol/L) pre-contracted aortic rings that was independent on the presence of endothelium. HSDE markedly decreased extracellular Ca²⁺-induced contraction in high-KCl and PE pre-challenged rings. It also inhibited the intracellular Ca²⁺ release sensitive to PE (10⁻⁶ M). The relaxant effect of HSDE were blunted by 4-amino-pyridine (4-AP, 10⁻³ mol/L), an inhibitor of voltage-dependent K⁺ channels.

Conclusion

Our results provide the first evidence that a dichloromethane extract of Heracleum sphondylium L. exhibits vasorelaxant properties through endothelium-independent mechanisms involving the inhibition of Ca²⁺ mobilization and changes in Kv channel conductances. These data argue for its use as antihypertensive therapy in traditional medicine.     

牡荆属植物的研究进展

至今为止人们对牡荆属植物中的黃荆和蔓荆进行了较多的研究,从中发现包括黄酮类、萜类、木脂素类、甾醇类、蒽类及挥发油等在内的不同类型的多种化学成分。一些试验结果确认牡荆属植物中富含的黄酮类化合物可用于延缓衰老,防治心血管疾病等作用,显示有较好的开发应用价值。由于牡荆属植物在我国分布广泛,植物种类多样,其中很多品种已作为民间用药,如果附加科学内涵加以研究开发,该属植物将有巨大的消费市场,同时也将会成为一种涉及民生和关系区域发展的经济作物。     

蓖麻PIP5Ks基因的生物信息学及荧光定量PCR分析

目的预测磷脂酰肌醇4-磷酸5-激酶(PIP5Ks)基因家族7个基因的表达部位;测定Lm型雌性系蓖麻a Lm AB23种品系不同时期的蓖麻花序中PIP5Ks各成员相对表达量。方法利用生物信息学分析在线软件进行蛋白质理化性质分析、蛋白质疏水性分析、亚细胞定位预测、跨膜区分析。采用荧光定量PCR方法进行蓖麻PIP5Ks基因家族的生物信息学分析和采用DNAMAN程序进行序列比对。结果蓖麻PIP5Ks共有7个成员,分别为PIP5K1、PIP5K2、PIP5K4、PIP5K6、PIP5K8、PIP5K9、PIP5K11;蓖麻PIP5K对应的蛋白之间的氨基酸序列同源性达到48.06%,蓖麻PIP5Ks所对应蛋白均为亲水性蛋白,除PIP5K9和PIP5K11为不稳定蛋白质其余均为稳定蛋白质;PIP5Ks对应蛋白均不存在跨膜结构域,均为非跨膜蛋白。亚细胞定位结果显示PIP5K1、PIP5K4、PIP5K6、PIP5K9、PIP5K11蛋白具有导肽的可能性较低,并且无对应的氨基酸切割位点,即定位在其他细胞器或者可能为胞浆蛋白;PIP5K2蛋白定位在叶绿体,叶绿体转运肽数值较高;PIP5K8蛋白定位在分泌通路。利从PIP5Ks在差异表达的相对表达量变化上来看,除PIP5K4并未检测到荧光,其余PIP5Ks均有一定的差异表达,PIP5Ks的相对表达量的变化趋势均较为相近,PIP5K1、PIP5K2的相对表达量较多,其次为PIP5K8、PIP5K9的相对表达量,PIP5K6及PIP5K11只有少量的表达。结论 PIP5Ks在蓖麻中对花序轴性状可能有一定的影响,PIP5Ks在花序轴上的差异含量与花序发育具有一定的规律性。     

Anti-inflammatory and antioxidant properties of hydroalcoholic crude extract from Casearia sylvestris Sw. (Salicaceae)

Ethnopharmacological relevance

Casearia sylvestris Sw. is widely used in popular medicine to treat inflammatory conditions.

Aim of the study

To investigate the anti-inflammatory and antioxidant properties of hydroalcoholic crude extract (HCE) taken from Casearia sylvestris Sw. (Salicaceae).

Methods and results

The effect of the HCE from this plant (3–300 mg/kg) on the reduction of inflammatory response to carrageenan was investigated in pleurisy in rats (intrapleural, 2% in 0.2 mL) or paw edema in mice (intraplantar, 300 μg/20 μL, right hind paw). The plant anti-inflammatory action was assessed by its capability in inhibiting cell migration, enzymatic activity of myeloperoxidase (MPO) and production of nitrite/nitrate or edema. The in vitro antioxidant activity of this extract against lipid peroxidation and damage to proteins was assessed as possible pathways to contribute as anti-inflammatory mechanisms. Carrageenan-induced hind paw edema (739.3±11.9 μm) was reduced by HCE (30 mg/kg: 462.8±28.38 μm) to similar extents as dexametasone (365.1±16.7). In pleurisy, treatment of the animals with HCE (100 mg/kg: 0.010±0.001 mU/mg of protein) also reduced MPO activity augmented by carrageenan (0.020±0.001 mU/mg of protein) as well as leukocytes migration (carrageenan: 17.8890±2.3900 leukocytes/mL, HCE 100 mg/kg: 7.0880±9631 leukocytes/mL). Significant effects were also observed in animals treated with different doses of HCE in biochemical tests for oxidative stress analysis.

Conclusion

The anti-inflammatory and antioxidant effects of HCE from Casearia sylvestris Sw. suggests a potential therapeutic benefit of this plant in treatment of inflammatory conditions.     

火炭母药材HPLC指纹图谱研究

目的:建立火炭母药材的HPLC指纹图谱分析方法,为火炭母药材质量评价提供参考依据。方法:色谱柱PlatisilODS C18(4.6 mm×250 mn,5μm),流动相乙腈-0.05%磷酸溶液,梯度洗脱进行色谱分离;洗脱时间60 min,流速1.0 mL.min-1,检测波长360 nm。结果:确定17个共有色谱峰为特征峰构成火炭母药材HPLC指纹图谱,相似度评价结果表明,各产地火炭母药材相似度均在0.90以上。结论:所用方法准确可靠,所得指纹图谱共有模式可作为火炭母药材质量控制的依据。     

Immunosuppressive activity of an aqueous Viola tricolor herbal extract

Ethnopharmacological relevance

Heartsease (Viola tricolor L.), a member of the Violaceae family, has a long history as a medicinal plant and has been documented in the Pharmacopoeia of Europe. Due to its anti-inflammatory properties it is regarded as a traditional remedy against skin diseases, for example for the treatment of scabs, itching, ulcers, eczema or psoriasis, and it is also used in the treatment of inflammation of the lungs and chest such as bronchitis or asthma. Because T-cells play an important role in the pathological process of inflammatory diseases we investigated the effect of an aqueous Viola extract on lymphocyte functions and explored the ‘active’ principle of the extract using bioactivity-guided fractionation.

Material and Methods

An aqueous Viola extract was prepared by C₁₈ solid-phase extraction. Effects on proliferation of activated lymphocytes (using the cell membrane permeable fluorescein dye CFSE), apoptosis and necrosis (using annexin V and propidium iodide staining), interleukin-2 (IL-2) receptor expression (using fluorochrome-conjugated antibodies) and IL-2 cytokine secretion (using an ELISA-based bead array system) were measured by flow cytometry. Influence on lymphocyte polyfunctionality was characterized by Viola extract-induced production of IFN-γ and TNF-α, as well as its influence on lymphocyte degranulation activity. Fractionation and phytochemical analysis of the extract were performed by RP-HPLC and mass spectrometry.

Results

The aqueous Viola extract inhibited proliferation of activated lymphocytes by reducing IL-2 cytokine secretion without affecting IL-2 receptor expression. Similarly, effector functions were affected as indicated by the reduction of IFN-γ and TNF-α production; degranulation capacity of activated lymphocytes remained unaffected. Bioassay-guided fractionation and phytochemical analysis of the extract led to identification of circular plant peptides, so called cyclotides, as bioactive components.

Conclusion

An aqueous Viola extract contains bioactive cyclotides, which inhibit proliferation of activated lymphocytes in an IL-2 dependent manner. The findings provide a rationale for use of herbal Viola preparations in the therapy of disorders related to an overactive immune system. However, further studies to evaluate its clinical potency and potential risks have to be performed.     

Antiulcer activity of methanolic extract of Momordica charantia L. in rats

Aim of the study

Momordica charantia L. (Cucurbitaceae) commonly known as ‘bitter gourd’ is a multi purpose herb cultivated in different parts of the world for its edible fruits. The objective of the present study was to evaluate the effect of standardized methanolic extract of Momordica charantia L. fruits on gastric and duodenal ulcers.

Materials and methods

The effect was evaluated in acetic acid induced chronic gastric ulcer, pylorus ligation induced gastric ulcer, ethanol induced gastric ulcer, stress induced gastric ulcer, indomethacin induced gastric ulcer and cysteamine induced duodenal ulcer model. The extract was administered orally at two different doses of 100 mg/kg and 500 mg/kg.

Results

The healing of acetic acid induced gastric ulcer was increased by both doses of the extract. In pylorus-ligated rats, the extract showed significant decrease in ulcer index, total acidity, free acidity and pepsin content and an increase in gastric mucosal content. The extract also reduced the ulcer index in stress induced, ethanol induced and indomethacin induced gastric ulcers and cysteamine induced duodenal ulcer.

Conclusion

The methanolic extract of Momordica charantia L. fruit increases healing of gastric ulcer and also prevents development of gastric ulcers and duodenal ulcers in rats.     

鸭跖草对高脂血症小鼠血脂代谢及抗氧化能力的影响

目的:探讨鸭跖草对实验性高脂血症小鼠血脂代谢及抗氧化能力的影响.方法:昆明种雄性小鼠72只随机分为正常对照组、高脂模型组、辛伐他汀4 mg·kg·d-1组和鸭跖草高、中、低剂量组.除正常对照组灌服纯净水外,其余5组均灌服高脂乳剂0.02 mL·g-1,qd,连续14 d,鸭跖草高、中、低剂量组ig 16,8,4 g·kg-1.末次给药后,检测血清总固醇(TC)、甘油三酯(TG)、低密度脂蛋白-胆固醇(LDL-C)、高密度脂蛋白-胆固醇(HDL-C)的含量,计算动脉硬化指数(AI);测定血清、肝脏和脑组织丙二醛(MDA)含量及超氧化物歧化酶(SOD)和谷胱甘肽过氧化物酶(GSH-Px)活性.结果:与高脂模型组相比,鸭跖草3个剂量组小鼠血清TC,LDL-C水平和AI降低(P＜0.05,P＜0.01),HDL-C显著升高(P＜0.01),而TG无明显变化;鸭跖草16,8 g·kg-1剂量组小鼠血清、肝脏和脑SOD,GSH-Px活性均升高(P ＜0.05,P＜0.01),鸭跖草16,8,4 g·kg-1剂量组MDA含量均降低(P ＜0.05,P＜0.01).结论:鸭跖草能调节血脂代谢异常,可能与其抗氧化活性有关.     

Hypotensive and endothelium-independent vasorelaxant effects of methanolic extract from Curcuma longa L. in rats

Ethnopharmacological relevance

Curcuma longa L. (CL) is a yellow rhizome that is used in African traditional medicine to treat palpitation, hypertension or other related blood circulation disorders.

Aim of the study

To justify the use of CL in ethnomedicine, we investigated the vasorelaxant effect of methanolic extract of CL (CLME) and its underlying mechanisms in isolated rat mesenteric artery.

Materials and methods

The effect of CLME on the mean arterial pressure (MAP) and heart rate (HR) (pulse interval) were determined in vivo in non-anaesthetized rats. Superior mesenteric rings were isolated, suspended in organ baths containing Tyrode solution at 37 °C and gassed with 95% O₂ + 5% CO₂, under a resting tension of 0.75 g. The vasorelaxant effects of CLME were studied by means of isometric tension recording experiments.

Results

In normotensive rats, CLME (10, 20 and 30 mg/kg, i.v.) induced dose-dependent hypotension (2.0 ± 0.5%; 27.1 ± 5.0% and 26.7 ± 4.6%, respectively), and pronounced bradycardia (5.8 ± 1.2%, 19.3 ± 3.2% and 22.9 ± 4.6%, respectively). CLME (1–1000 μg/mL) induced concentration-dependent relaxation of tonic contractions evoked by phenylephrine (Phe) (10 μM) and KCl (80 mM) in rings with intact-endothelium (E_max = 82.3 ± 3.2% and 97.7 ± 0.7%) or denuded-endothelium (E_max = 91.4 ± 1.0% and 97.8 ± 1.1%). Also, in a depolarized, Ca²⁺ free medium, CLME inhibited CaCl₂ (1 μM–30 mM)-induced contractions and caused a concentration-dependent rightward shift of the response curves, indicating that CLME inhibited the contractile mechanisms involving extracellular Ca²⁺ influx. In addition, in Ca²⁺ free media containing EGTA (1 mM), CLME inhibited the transient contraction of denuded rings constricted with Phe, but not those evoked by caffeine (20 mM). In contrast, neither glibenclamide, BaCl₂, tetraethylammonium nor 4-aminopyridine affected CLME-induced relaxation.

Conclusions

These results demonstrate the hypotensive and bradycardic effects of CLME, as well as its potent vasodilation of rat mesenteric arteries. These effects, may in part, be due to the inhibition of extracellular Ca²⁺ influx and/or inhibition of intracellular Ca²⁺ mobilization from Phe-sensitive stores.     

Mechanisms of vasorelaxation induced by Ziziphora clinopodioides Lam. (Lamiaceae) extract in rat thoracic aorta

Aim of the study

Ziziphora clinopodioides Lam. (ZC) is widely used in Uyghur folk medicine for the treatment of hypertension diseases in Xinjiang, an autonomous region of China. To provide pharmacological basis for this traditional use, we explored the vasodilating effects of ZC and investigated the underlying mechanisms.

Materials and methods

Activity of hexane (ZCHE), dichloromethane (ZCDE) and aqueous (ZCAE) extracts of ZC were evaluated on isolated rat aortic rings pre-contracted with phenylephrine (PE) or high KCl. The mechanisms were evaluated on ZCDE, the most potent extract.

Results

ZCDE-induced relaxation in endothelium-intact aortic rings pre-contracted with phenylephrine (PE, 10⁻⁶ M) or high KCl (6 × 10⁻² M), with respective EC₅₀ values of 0.27 ± 0.03 and 0.34 ± 0.04 g/l. Mechanic removal of the endothelium did not significantly modify ZCDE-induced relaxation. In endothelium-denuded aorta pre-contracted with PE (10⁻⁶ M), the vasorelaxant effect of ZCDE was significantly decreased by 4-amino-pyridine (10⁻³ M), but not by glibenclamide (10⁻⁴ M), iberiotoxin (3 × 10⁻⁸ M) and thapsigargin (10⁻⁷ M). In Ca²⁺ free solution, ZCDE significantly inhibited extracellular Ca²⁺-induced contraction in high KCl and PE pre-contracted rings. Additionally ZDCE inhibited the intracellular Ca²⁺ release sensitive to PE (10⁻⁶ M).

Conclusions

The results demonstrate that ZDCE exhibits endothelium-independent vasodilating properties that are mediated by inhibition of extracellular Ca²⁺ influx through voltage- and receptor-operated Ca²⁺ channels (VDDCs and ROCCs), by inhibition of Ca²⁺ release from intracellular stores, and also by the opening of voltage-dependent K⁺ channels.     

Trapa natans L. root extract suppresses hyperglycemic and hepatotoxic effects in STZ-induced diabetic rat model

Ethnopharmacological relevance

Trapa natans L. has a folkloric reputation as nutrient, appetizer and astringent. Its utility as antidiabetic, anticancer, diuretic, aphrodisiac, antidiarrhoeal and in many other maladies is well reported in the literature. Therefore, the present study has been carried out to study the antihyperglycemic effect of root extract of Trapa natans L. and its various fractions. Furthermore, hepatotoxic effects and lipid peroxidation risks have also been evaluated.

Methods

The ethanol extract and its successive fractions obtained from roots of Trapa natans have been administered in sucrose loaded and STZ- induced diabetic Wistar rats at doses of 50, 100 and 200 mg/kg b.w. Glibenclamide was used as positive control. The evaluation of protective effects of extract as well as fractions against hepatotoxicity and lipid peroxidation at 600 mg/kg b.w. has also been carried out.

Results

The methanol fraction emerged as the most potent antihyperglycemic fraction. It has also been found that the ethanolic extract as well as its fractions did not cause any lipid peroxidation and hepatotoxicity risks.

Conclusion

It can be concluded that the intense investigations of the methanol fraction obtained from Trapa natans root extract can be done to provide an alternative natural therapy for hyperglycemia.     

The medicinal uses of Callicarpa L. in traditional Chinese medicine: An ethnopharmacological,phytochemical and pharmacological review

Ethnopharmacological relevance

Callicarpa L. (Verbenaceae) has been used for centuries in Traditional Chinese Medicine (TCM) for the prevention and treatment of a wide number of health disorders such as inflammation, rheumatism, hematuria, fracture, hematemesis, menoxenia, gastrointestinal bleeding, scrofula, etc.

Aims of the review

To assess the scientific evidence for therapeutic Callicarpa in TCM and to identify future research needs.

Methods

The available information on the ethnopharmacological uses in Chinese medicine, phytochemistry, pharmacology and clinical practice of Callicarpa species was collected via a library and electronic search (PubMed, ScienceDirect, Google Scholar and CNKI).

Results

A variety of ethnomedical use of Callicarpa has been recorded in many ancient Chinese books. Phytochemical investigation of this genus has resulted in identification of more than 200 chemical constituents, among which diterpenes, triterpenoids and flavonoids are the predominant groups. The isolates and crude extract have exhibited a wide spectrum of in vitro and in vivo pharmacological effects involving anti-inflammatory, hemostatic, neuroprotective, anti-amnesic, antitubercular, antioxidant, antimicrobial and analgesic activities. Preparations containing Callicarpa species exerted good efficacy on clinical applications of gynecological inflammation, internal and external hemorrhage as well as acne vulgaris and chronic pharyngitis, etc. From the toxicity perspective, only three Callicarpa species have been assessed.

Conclusions

Pharmacological results have validated the use of Callicarpa species in the traditional medicine. As literature demonstrated, terpenoids and flavonoids are perhaps responsible for most of the activities shown by the plants of this genus. However, the detailed active compounds and the underlying mechanisms remain a work in progress. In addition, more attention should be paid to C. nudiflora as well as the domain of rheumatism.     

Antidepressant-like effects of the extract from Cimicifuga foetida L.

Ethnopharmacological relevance: Cimicifuga foetida L., a traditional Chinese medicine, has been developed for the treatment of perimenopausal symptoms including depression in China (Brand name: XIMINGTING^®, XMT). The primary active constituents are believed to be the triterpene glycosides. Nevertheless, there are no studies about the antidepressant-like effects of XMT in rodents.     

Hexane extract of Poncirus trifoliata (L.) Raf. stimulates the motility of rat distal colon

Aim of the study

Poncirus trifoliata (L.) Raf. (Rutaceae, PT) has been commonly used for treating gastrointestinal (GI) disorders in Korean traditional medicine, but its pharmacological roles in the regulation of colonic motility have not been clarified. This study investigated the regulatory effects of PT on the colonic motility.

Materials and methods

Immature fruits of PT were sequentially partitioned with MeOH, n-hexane, CHCl₃, EtOAc, n-BuOH and H₂O, and the effects of PT extracts on the contractility of colonic strips and colonic luminal transit in rats were measured in vitro and in vivo, respectively.

Results

Among six different extracts, only hexane extract of PT (PTHE) dose-dependently increased the low frequency contraction of longitudinal muscle in distal colonic strips, and the ED₅₀ value was revealed to be 0.71 μg/ml. The contractile patterns induced by PTHE were remarkably different from those caused by acetylcholine (ACh) and serotonin (5-HT). The stimulatory effects of PTHE on the whole distal colonic strips were more prominent than on the mucosa/submucosa-denuded segments. The M₂ receptor-preferring, methoctramine (0.5 μM), and M₃ receptor-preferring antagonist, 4-DAMP (0.5 μM) significantly blocked the PTHE (1 μg/ml)-induced contraction of distal colon longitudinal muscles, whereas the 5-HT receptor antagonists (1.0 μM, alone or in combination) selective for 5-HT₃ (ondansetron), 5-HT₄ (GR113808) and 5-HT_{1, 2, 5–7} (methysergide) receptors did not change the PTHE (1 μg/ml)-induced contractility of distal colon longitudinal muscles. SNAP (0.1 mM), a NO donor, enhanced the stimulatory effects of PTHE on the longitudinal muscle of distal colon, but l-NAME (0.1 mM), a NO synthesis inhibitor, had no effects. PTHE (10–100 mg/kg) caused a dose-dependent increase of colonic luminal transit.

Conclusions

Collectively, these findings suggest that PTHE specifically acts on the longitudinal muscle of distal colon in rats, and these stimulatory effects are likely mediated, at least, by activation of acetylcholinergic M₂ and M₃ receptors.