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评价雄性大鼠中亚麻木酚类化合物从 Ferula huber-morathii Peşmen 根中的潜在壮阳活性。

Evaluation of the potential aphrodisiac activity of sesquiterpenoids from roots of Ferula huber-morathii Peşmen in male rats.

机构信息

Department of Pharmaceutical Botany, Faculty of Pharmacy, Ege University, Bornova, İzmir, 35030, Turkey.

Department of Pharmacology, College of Veterinary Medicine, Cairo University, Giza 12211, Egypt; Department of Pharmacology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, 11942 Al-Kharj, Saudi Arabia.

出版信息

J Ethnopharmacol. 2020 Jul 15;257:112868. doi: 10.1016/j.jep.2020.112868. Epub 2020 Apr 13.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Several species of Ferula L. genus have been used in traditional Turkish medicine as aphrodisiac to treat male sexual dysfunction. Especially, roots and oleo gum resin of F. elaeochytris Korovin, F. communis L., F. assa-foetida L. and F. gummosa Boiss. were claimed to be used for aphrodisiac activity, menstrual regulation and treatment of gastric pain in Anatolia. Ferula L. is represented by 23 taxa in Turkey, 13 of which are endemic species. F. huber-morathii Peşmen (FHM), an endemic plant, is popularly known as ''helizan, çağşır''.

AIM OF THE STUDY

This study aimed to isolate sesquiterpenoids from the roots of Ferula huber-morathii (FHM) and to confirm their aphrodisiac potential in male rats.

MATERIAL AND METHODS

In a preliminary experiment, the effects of aqueous (HO) and chloroform (CHCl) extracts of FHM were tested for their potential aphrodisiac activities in male rats. Then, sesquiterpene derivatives were isolated from the active chloroform extract of FHM roots (FHM-R) and characterized (TLC, 1D, 2D NMR, HR-MS and CD). Moreover, some of the isolates with adequate quantities were evaluated for their possible aphrodisiac effects on male rats. Single doses (10 mg/kg BW) of sildenafil citrate (SC, positive control), gummosin, mogoltavidin, deacetylkellerin, ferukrin acetate with kellerin, elaeochytrin-A and ferutinin were administered orally by gavages to male Wistar albino rats. Mount latency (ML), mount frequency (MF), intromission latency (IL), intromission frequency (IF), ejaculation latency (EL) and postejaculatory interval (PEI) were studied. In addition, copulatory efficiency (CE) and intercopulatory efficiency (ICE) were calculated.

RESULTS

The preliminary experiment revealed that the chloroform extract was the main source of the active compounds as it showed the higher aphrodisiac activity while the aqueous extract was found to be inactive. Eleven sesquiterpene derivatives, viz. gummosin, mogoltavidin, farnesiferol A, deacetylkellerin, ferukrin acetate, kellerin, teuclatriol, feruhermonin C, ferutinin, elaeochytrin A and teferidin, were isolated from the FHM-CHCl extract. Oral administration of deacetylkellerin, elaeochytrin-A and ferutinin significantly increased MF and IF. The ML and IL were significantly reduced, and ejaculation latencies were prolonged. Administration of these sesquiterpenoids also reduced the PEI. The present results revealed that ferutinin was the most effective aphrodisiac compound compared to other sesquiterpenoids. The results of 10 mg/kg of ferutinin are comparable to SC, the positive control. The results revealed that gummosin, mogoltavidin and ferukrin acetate with kellerin did not significantly alter the aphrodisiac parameters.

CONCLUSIONS

This study has established that the CHCl extract of FHM root contains sesquiterpene derivatives, especially coumarin ethers and benzoic esters. Findings of the present study demonstrate that the chloroform extract and some of the sesquiterpene derivatives significantly stimulates sexual behavior in male rats, thus suggesting that F. huber-morathii possesses an aphrodisiac activity.

摘要

民族药理学相关性

几种 Ferula L. 属的物种已在传统的土耳其医学中被用作春药,用于治疗男性性功能障碍。特别是 F. elaeochytris Korovin、F. communis L.、F. assa-foetida L. 和 F. gummosa Boiss 的根和油树脂据称具有春药活性、调节月经和治疗安纳托利亚的胃痛。土耳其有 23 种 Ferula L.,其中 13 种是特有种。F. huber-morathii Peşmen(FHM),一种特有植物,俗称“helizan, çağşır”。

研究目的

本研究旨在从 Ferula huber-morathii(FHM)的根部分离出倍半萜,并证实其在雄性大鼠中的催情潜力。

材料和方法

在初步实验中,测试了 FHM 的水(HO)和氯仿(CHCl)提取物对雄性大鼠潜在催情活性的影响。然后,从 FHM 根的活性氯仿提取物(FHM-R)中分离出倍半萜衍生物,并进行了鉴定(TLC、1D、2D NMR、HR-MS 和 CD)。此外,还评估了一些具有足够数量的分离物对雄性大鼠可能的催情作用。西地那非 citrate(SC,阳性对照)、gummosin、mogoltavidin、deacetylkellerin、ferukrin acetate with kellerin、elaechytrin-A 和 ferutinin 以 10mg/kg BW 的单剂量经灌胃给予雄性 Wistar 白化大鼠。研究了勃起潜伏期(ML)、勃起频率(MF)、插入潜伏期(IL)、插入频率(IF)、射精潜伏期(EL)和射精后间隔(PEI)。此外,还计算了交配效率(CE)和交配对效率(ICE)。

结果

初步实验表明,氯仿提取物是活性化合物的主要来源,因为它表现出更高的催情活性,而水提取物则被发现没有活性。从 FHM-CHCl 提取物中分离出 11 种倍半萜衍生物,即 gummosin、mogoltavidin、farnesiferol A、deacetylkellerin、ferukrin acetate、kellerin、teuclatriol、feruhermonin C、ferutinin、elaechytrin A 和 teferidin。口服给予 deacetylkellerin、elaechytrin-A 和 ferutinin 可显著增加 MF 和 IF。ML 和 IL 显著减少,射精潜伏期延长。这些倍半萜类化合物的给药还降低了 PEI。目前的结果表明,与其他倍半萜类化合物相比,ferutinin 是最有效的催情化合物。10mg/kg ferutinin 的结果与阳性对照 SC 相当。结果表明,gummosin、mogoltavidin 和 ferukrin acetate with kellerin 对催情参数没有显著影响。

结论

本研究表明,FHM 根的 CHCl 提取物含有倍半萜衍生物,特别是香豆素醚和苯甲酸酯。本研究的结果表明,氯仿提取物和一些倍半萜衍生物显著刺激雄性大鼠的性行为,因此表明 F. huber-morathii 具有催情活性。

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