The effect of planting depth,disbudding, and root pruning on root weight and aconite alkaloid content of the tuberous root of aconite

The tuberous root of aconite, Aconiti tuber, contains tonic but poisonous aconite alkaloids, such as aconitine, hipaconitine and mesaconitine. The standardization of the cultivation protocols must be established, since the quality of the crude drug, especially the content of aconite alkaloids, is influenced by cultivation conditions. Here, we report the effects of planting depth, disbudding and root pruning on the content of the aconite alkaloids as well as on the weight of the root tuber of aconite. The daughter root tubers of shallow-planted plants showed a significantly higher content of aconitine, hipaconitine and sum of aconite alkaloids per unit weight than those of deeply planted root tubers (control group), while the average weight per root tuber was lower than that of the control group. The total weight of the daughter root tubers per plant of the disbudding group was significantly higher than that of other groups, including the root-pruning group whose average weight per tuber was the highest. In conclusion, disbudding is effective in achieving both higher content of aconite alkaloids and heavier total weight of the root tuber.     

附子心脏毒性及配伍减毒增效机制研究进展

附子来源于毛茛科植物乌头Aconitum carmichaeli Debx.,最主要的毒性反应表现为心脏毒性和神经毒性,其中心脏是主要的靶器官之一。目前普遍认为附子所致心脏毒性是由双酯型二萜生物碱直接或间接作用于心脏的结果,其毒性机制与Ca²⁺超载、脂质过氧化反应、细胞凋亡以及迷走神经兴奋性增高有关。研究发现附子与其他传统中草药配伍能通过影响体内代谢过程、抗Ca²⁺超载、抗氧化应激、抗凋亡等机制发挥减毒增效作用。就近年来国内外对附子心脏毒性及配伍减毒增效相关机制的研究进展进行综述,以期为附子的深入研究和临床安全用药提供参考。     

Quantitative determination of flavonoids from the aerial part of greater knapweed (<Emphasis Type="Italic">Centaurea scabinosa</Emphasis> L.)

Quantitative determination of flavonoids from the aerial part of greater knapweed (Centaurea scabiosa L.) has been carried out by differential spectrophotometry in combination with a modified method of forming flavonoid complexes with aluminum chloride in HCl. Depending on the plant collection site, the quantitative content of flavonoids in the aerial part of greater knapweed varied within 1.3 – 2.0% (calculated as rutin). The random error of measurement did not exceed 3% at a confidence probability of 0.95. The systematic error of the proposed metohd did not exceed the error of determination. The accumulation dynamics of flavonoids in the aerial part of greater knapweed during the 2006 vegetative peroid have been tracked for plants growing in Tomsk and Kemerovo regions. The maximum content of flavonoids (1.70 ± 0.04% calculated as rutin) was observed in the stage of full flowering, which is therefore the optimum period for collecting the aerial part of the plants for the maximum yield of flavonoids. The maximum amount of flavonoids was accumulated in leaves (1.96 ± 0.04%), which is somewhat greater than the content of flavonoids in the entire aerial part of greater knapweed (1.70 ± 0.04%).     

附子对小鼠超氧化物岐化酶活性和丙二醛、NO含量的影响

目的:研究附子不同的临床使用剂量对小鼠心脏超氧化物歧化酶(SOD)活性、丙二醛(MDA)、一氧化氮(NO)含量的影响,探讨其对心脏的毒性机制.方法:制备附子及与甘草配伍的水煎液,将小鼠随机分为9组,分别以附子15,45,75,105g的临床使用剂量按等效换算系数换算成小鼠给药剂量,给小鼠灌胃20 d,测其心脏组织SOD活性及MDA、NO含量.结果:与对照组比较,单附子临床剂量45,75,105 g组小鼠心脏SOD活性明显增加,MDA含量显著降低(P＜0.05).甘草配伍后的各组与对照组比较,SOD含量有增加的趋势,但仅105 g组有明显差异(P＜0.05);除15 g组外,其余各组MDA含量均显著降低(P＜0.05);NO含量均呈下降趋势,但差异无统计学意义(P＞0.05).结论:大剂量使用附子对心脏的SOD活力、MDA和NO含量没有负面影响,相反能减轻小鼠心脏组织氧化反应.     

Cardiotonic effect of <Emphasis Type="Italic">Apocynum venetum</Emphasis> L. extracts on isolated guinea pig atrium

The effects on guinea-pig heart muscle of extracts of Apocynum venetum L. leaf, root, stem, old stem and Venetron—a polyphenol-rich extract of leaves—were studied by recording the mechanical activity and heart rate of isolated right atria. Cymarin—a cardiac glycoside—was also determined in A. venetum extracts by LC–MS/MS analysis. All extracts examined here showed a weak cardiotonic effect, i.e., induced a contractile response of the isolated atria and increased the pulse at a concentration of 1 mg/mL, which was not inhibited by propranolol (1 μM)—a β-adrenoceptor blocker. The cymarin content in extracts of A. venetum was ranked as follows: old stem >> stem > root > leaf >> Venetron. Since the cardiotonic effects of A. venetum extracts did not reflect the cymarin content, a possible mechanism other than that of cardiac glycosides was investigated. The inhibitory effects on phosphodiesterase 3 (PDE3) were studied in a cell-free enzyme assay; all extracts of various parts of A. venetum inhibited PDE purified from human platelets. These results suggest that PDE3 inhibition may contribute to the cardiotonic effects of A. venetum extracts.     

附子及附子配伍干姜对腺嘌呤所致慢性肾衰小鼠肾功能的影响

目的：研究中药附子及附子配伍干姜对腺嘌呤所致小鼠慢性肾衰的疗效,并初步探讨其作用机制。方法：将雄性ICR小鼠随机分为正常对照组、模型组、低剂量附子组、高剂量附子组、低剂量附子＋干姜组和高剂量附子＋干姜组。正常对照组小鼠灌胃给予蒸馏水;其余各组小鼠灌胃给予腺嘌呤（第1周和第2～4周的给药剂量分别为250和130 mg.kg-1,均为每2天给药1次）,低剂量附子组、高剂量附子组、低剂量附子＋干姜组和高剂量附子＋干姜组小鼠另分别灌胃给予相应的水煎液,每天1次。实验过程中,记录各组小鼠的一般情况,并于实验结束时,对小鼠血清肌酐、尿素氮、乳酸和乳酸脱氢酶,以及肾组织谷胱甘肽、谷丙转氨酶、谷草转氨酶和丙二醛的含量进行测定,并记录附睾精子数。结果：与正常对照组相比,模型组和各给药组小鼠体重下降,摄食量减少,饮水量升高;高剂量附子组和低剂量附子＋干姜组小鼠饮水量明显低于模型组小鼠。模型组小鼠消瘦、萎靡、被毛发黄干枯不齐,部分死亡;高剂量附子＋干姜组和低剂量附子＋干姜组小鼠被毛白净有光泽,且活动性更强。高剂量附子水煎液,高剂量附子＋干姜水煎液,以及低剂量附子＋干姜水煎液对小鼠生化指标具有显著改善作用,可降低肾系数以及血清肌酐、尿素氮、乳酸和乳酸脱氢酶水平,提高精子数;可降低小鼠肾组织GSH水平,升高MDA水平;高剂量附子组和高剂量附子＋干姜组小鼠肾组织ALT水平,以及高剂量附子＋干姜组和低剂量附子＋干姜组小鼠肾组织AST水平均显著高于模型组;低剂量附子组小鼠除个别指标外,无明显的改善。结论：高剂量附子水煎液对腺嘌呤所致慢性肾功能衰竭小鼠肾功能具有一定保护作用,与干姜配伍后其疗效增加,毒性降低。     

Sequential effects of cadmium on genotoxicity and lipoperoxidation in <Emphasis Type="Italic">Vicia faba</Emphasis> roots

Kinetics of stress responses to Cd exposure (50, 100 and 200 μM) expanding from 12 to 48 h were studied in roots of hydroponically cultivated-Vicia faba seedlings. The heavy metal induced toxicity symptoms and growth arrest of Vicia roots gradually to the Cd concentration and duration of the treatment. The intracellular oxidative stress was evaluated with the H₂O₂ production. The H₂O₂ content increased gradually with the sequestered Cd and root growth inhibition. Lipid peroxidation—evidenced by malondialdehyde (MDA) content and Evans blue uptake—and genotoxicity—evidenced by mitotic index (MI) and micronuclei (MCN) values—were concomitantly investigated in root tips. By 12 h, root meristematic cells lost 15% of their mitotic activity under 50 or 100 μM Cd treatment and 50% under 200 μM Cd treatment and led cells with MCN, while the MDA content and Evans blue absorption were not affected. The loss of membrane integrity occurred subsequently by 24 h. The increase in MDA content in root cells treated with 50, 100 and 200 μM Cd was significantly higher than the control. By 48 h, the MDA content increased 134, 178 or 208% in root cells treated with 50, 100 and 200 μM Cd, respectively. The Evans blue absorption was also affected by 24 h in roots when treated with 200 μM Cd and gradually increase by 48 h with the Cd concentration of the treatment. The decrease of mitotic activity triggered by 12 h was even higher by 24 h and the MI reduced to 44, 56 or 80% compared to the control in the three different Cd concentrations tested. The different kinetics of early in vivo physiological and cytogenetic responses to Cd might be relevant to the characterization of its toxicity mechanisms in disrupting primarily the mitosis process.     

Influence of Prosolv and Prosolv:Mannitol 200 direct compression fillers on the physicomechanical properties of atorvastatin oral dispersible tablets

Abstract

The objective of the present study was to evaluate the influence of Prosolv® and Prosolv®: Mannitol 200 direct compression (DC) fillers on the physicomechanical characteristics of oral dispersible tablets (ODTs) of crystalline atorvastatin calcium. ODTs were formulated by DC and were analyzed for weight uniformity, hardness, friability, drug content, disintegration and dissolution. Three disintegration time (DT) test methods; European Pharmacopoeia (EP) method for conventional tablets (Method 1), a modification of this method (Method 2) and the EP method for oral lyophilisates (Method 3) were compared as part of this study. All ODTs showed low weight variation of <2.5%. Prosolv® only ODTs showed the highest tablet hardness of ～73?N, hardness decreased with increasing mannitol content. Friability of all formulations was <1% although friability of Prosolv®:Mannitol ODTs was higher than for pure Prosolv®. DT of all ODTs was <30?s. Method 2 showed the fastest DT. Method 3 was non-discriminatory giving a DT of 13–15?s for all formulations. Atorvastatin dissolution from all ODTs was >60% within 5?min despite the drug being crystalline. Prosolv® and Prosolv®:Mannitol-based ODTs are suitable for ODT formulations by DC to give ODTs with high mechanical strength, rapid disintegration and dissolution.     

乌头中主要生物碱的高效液相色谱测定

用高效液相色谱分离、测定乌头及附子中一些主要生物碱。生药的乙醚提取物在十八烷基键合相柱上,用甲醇—水—氯仿—三乙胺(70:30:2:0.1)作流动相,中乌头碱、乌头碱及次乌头碱与其它杂质能很好分离。以β-甲基萘作内标化合物,用峰高比测定各生物碱含量。曾测定了不同品种、不同产地及不同加工炮制方法的一些样品,其生物碱组成及比例相差较大。     

Evaluation of medicinal plants from Central Kalimantan for antimelanogenesis

In the course of searching for new materials to use as whitening agents, we screened 19 methanol extracts prepared from 14 medicinal plants from Central Kalimantan province, Indonesia. The screening methods used were the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging assay, a tyrosinase inhibition assay, and a melanin formation inhibition assay using B16 melanoma cells. The extracts of Willughbeia coriacea (bark part of aerial root), Phyllanthus urinaria (root), Eleutherine palmifolia (bulb), Eusideroxylon zwageri (seed), Dendrophthoe petandra (aerial root), Passiflora foetida (stem), and Vitex pinnata (root) showed DPPH radical-scavenging activity of more than 70% at 100 µg/ml. The extracts of W. coriacea (bark part of aerial root), P. urinaria (root), and D. petandra (aerial root) showed tyrosinase inhibitory activity of more than 40% using l-tyrosine as a substrate at 500 µg/ml. The extracts of W. coriacea (bark part of aerial root) and D. petandra (aerial root) showed tyrosinase inhibitory activity of more than 40% using l-DOPA as a substrate at 500 µg/ml. The extracts of W. coriacea (bark part of aerial root, 200 µg/ml), Glochidion philippcum (aerial root, 200 and 300 µg/ml), E. palmifolia (bulb, 50 µg/ml), E. zwageri (seed, 100 µg/ml), D. petandra (aerial root, 200 µg/ml), Lansium domesticum (bark, 25 µg/ml), P. foetida (stem, fruit, 300 µg/ml), and Solanum torvum (root, 300 µg/ml) strongly inhibited the melanin production of B16 melanoma cells without significant cytotoxicity. These findings indicate that some medicinal plants from Central Kalimantan are potential ingredients for skin-whitening cosmetics if their safety can be confirmed.     

中国防己科千金藤属药用植物资源利用研究

本文报道我国防己科18种千金藤属药用植物的资源及化学分析工作:通过薄层检查了17种生物碱在这些植物中的存在情况,测定了每种的根部所含总生物碱的含量以及用CS-910型薄层光密度计测定了其中10种生物碱的含量。结果表明,千金藤属植物是寻找异喹啉类生物碱新资源的对象,特别是有较大形块根的山乌龟亚属是今后生产肌肉松弛剂等药物有价值的原料植物;对千金藤属的化学分类提供了一定的依据。     

Physicochemical quality evaluation of natural compounds isolated from crude drugs

Aconite root has high toxicity caused by diester alkaloids, thus it was necessary to define the limiting value of diester alkaloids used in medicine formulation. To give the quality of “Processed Aconite Root” and “Powdered Processed Aconite Root” in the Japanese Pharmacopoeia (14th edn, supplement II), we established the official specification and evaluation methods of standard substances. High qualitative grade diester alkaloids, aconitine, hypaconitine, jesaconitine and mesaconitine, which were useful to evaluate the purity of processed aconite root and powdered processed aconite root, were prepared and evaluated for their stability. We studied the physicochemical specification and evaluation methods of these alkaloids. In addition, an “Aconitum diester alkaloids standard solution for purity”, which was used for the purity test, was prepared, and we also studied its physicochemical specification and evaluation methods. In addition, to evaluate the quality of processed aconite root and powdered processed aconite root, a TLC identification test was established. A monoester alkaloid of benzoylmesaconine hydrochloride was used as the reference standard in the latter test, and we also investigated its physicochemical specification and evaluation methods.     

中药附子成分研究——Ⅰ.去甲猪毛菜碱(salsolinol)的分离及其结构测定

From the lateral root of Aconitum carmichaeli Debx., Fu-Zi, which has long been used as one of the most important herbs as a heart stimulant in Chinese medicine, a cardiac and hypertensive principle Ⅱ was isolated and identified as salsolinol, 1-methyl-6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline, from its spectral data and by comparison with synthesized authentic sample.     

Toxic effects of methamidophos on paraoxonase 1 activity and on rat kidney and liver and ameliorating effects of alpha‐tocopherol

The role of alpha‐tocopherol on nephrotoxicity and hepatotoxicity induced by methamidophos (MT) was investigated in wistar rats. Animals were given via gavage, for four weeks, a low dose of MT (MT1), a high dose of MT (MT2), vitamin E (200 mg/kg of bw) or both MT2 plus vitamin E (Vit E) and control group was given distillate water. MT treatment resulted in a significant decrease in the body weight of MT2‐treated group. Moreover, MT‐treated groups had significantly lower butyrylcholinesterase (p < 0.01) and paraoxonase 1 (PON1) activities compared with the control group (p < 0.05). However, MT2‐treated group had significantly higher alkaline phosphatase activity compared with untreated rats (p < 0.05). Both MT‐treated groups had significantly higher urea (p < 0.01) and uric acid levels (p < 0.05) compared with the control group. However, significant low uric acid level (p < 0.05) was noted in MT2 plus vit E‐treated rats compared with MT2‐treated group. Histopathological changes in organ tissues were observed in both MT‐treated groups and MT2 plus vit E‐treated rats. However, the damage was reduced in MT2 plus vit E‐treated rats. Therefore, this study deduces that alpha‐tocopherol administration may ameliorate the adverse effects of subacute exposure to MT on rat liver and kidney and this antioxidant can protect PON1 from oxidative stress induced by this organophosphorus pesticide. © 2014 Wiley Periodicals, Inc. Environ Toxicol 31: 842–854, 2016.     

DPPH radical-scavenging effect on some constituents from the aerial parts of <Emphasis Type="Italic">Lippia triphylla</Emphasis>

Lippia triphylla (L'Her) O. Kuntze (Verbenaceae; common name, Lemon Verbena) is used in Peru as a spice and herb tea for the prevention of arteriosclerosis. From the aerial parts of this plant, 25 known compounds—3 phenylpropanoid glucosides, 7 flavonoids, 5 phenylethanoid glycosides, 5 lignans, 2 sesquiterpenoids, and 3 triterpenoids—were isolated, and their chemical structures were elucidated on the basis of physical and spectral data. Among them, 19 aromatic compounds were examined for their scavenging effect on the stable free radical 1,1-diphenyl-2-picrylhydrazyl—4 phenylethanoid glycosides and 5 lignans indicated a potent scavenging effect. Of note, the EC₅₀ values of two phenylethanoid glycosides reached almost thrice that of α-tocopherol.     

Total Phenolic Content,Antioxidant, and Antibacterial Activity of Rumex crispus Grown Wild in Turkey

Abstract

In the current study, we evaluated total phenolic content, antioxidant activity (by using β -carotene bleaching assay), and antibacterial activity of aqueous and methanol extracts of the aerial part of the Rumex crispus L. (Polygonaceae) naturally grown in the Eastern Anatolia region of Turkey. The aerial part of the plant had high total phenolic content (56.31 μ g/mg DW). The antioxidant activity of aqueous and methanol extracts of the aerial part of R. crispus L., BHA, and BHT were found to be 92.35%, 95.49%, 98.16%, and 96.66%, respectively. Although the antioxidant activity of the aqueous and methanol extracts of R. crispus was lower than that of the BHA and BHT, the difference between these was not statistically significant, p < 0.05. The methanol extract possessed strong antibacterial activity against Agrobacterium tumefaciens, Bacillus cereus, Bacillus subtilis, Pseudomonas corrugate, Pseudomonas syringae pv. tomato, Salmonella typhimurium, Serratia liquefaciens, Vibrio cholerae, Yersinia frederiksenii, and Yersinia pseudotuberculosis. Therefore, the aerial part of R. crispus can be used as an effective and safe source of antioxidants and antibacterial agent.     

反相高效液相色谱法测定参附注射液及市售黑附片中乌头碱的含量

目的　测定参附注射液及市售黑附片中乌头碱的含量。方法　用RP HPLC ,流动相为乙腈 醋酸铵缓冲液 (pH10 5 ) ,紫外检测波长 2 3 0nm ,流速 0 8ml·min-1。结果　对照品的线性范围 1 3 9～ 2 2 2 4 μg(r =0 9997) ;市售黑附片中的乌头碱比参附注射液中的高 3倍。结论　方法简便、快速、准确、重现性好 ,可以作为样品的检验方法     

附子的化学成分研究

利用各种色谱方法对毛茛科(Ranunculaceae)植物川乌(Aconitum carmichaeli Debx.) 的子根附子的化学成分进行了研究,从中分离得到了8个二萜生物碱类化合物,根据化合物的理化性质和波谱数据确定了化合物的结构,它们分别为海替生(1)、8-乙氧基-14-苯甲酰基中乌头原碱(2)、10-羟基乌头碱(3)、次乌头碱(4)、中乌头碱(5)、北草乌碱(6)、尼奥灵(7)、附子灵(8),其中化合物1～3为首次从该植物中分离得到.     

Toxicological potential of mycotoxin MT81 and its benzoylated derivative on testicular spermatogenesis and steroidogenesis in mature male Wistar albino rats

Mycotoxin MT81 was isolated, purified, and identified from a fungal strain of Penicillium nigricans. It is a CNS depressant, hyperglycemic agent and produces massive bone marrow depression, hepatotoxicity, and nephrotoxicity. Its benzolylated analog (benzoylated-MT81) was synthesized in our laboratory having a LD₅₀ value of 87.1?mg/kg body weight in mice. This study was designed to assess the toxicological effects of mycotoxin MT81 and its analog on testicular spermatogenesis and steroidogenesis in mature albino rats. The sperm count and percentage of motile sperm were decreased markedly in MT81- and benzoylated-MT81-treated rats. The body weight and the weight of testis were reduced, whereas weight of adrenal gland was increased in a dose-dependent manner in the toxin-treated rats. MT81 and its derivative caused accumulation of ascorbic acid and total cholesterol in the testis and reduction in the activities of Δ⁵-3β-hydroxysteroid dehydrogenase (Δ⁵-3β-HSD) and glucose-6-phosphate dehydrogenase (G-6-P-D), whereas the ascorbic acid and cholesterol content of adrenal gland were decreased and enzyme activities were elevated. This experiment suggests that MT81 and benzoylated-MT81 both produce inhibition of testicular spermatogenesis and steroidogenesis but increase adrenal steroidogenesis and ultimately sterility of male rats.