OBJECTIVETo study the relationships among the main agronomic characters, yield per plant,content of artemisinin of Artemisia annua, and provide the theoretical basis for breeding the A. annua varieties with high-yield and high artemisinin content.

METHODThe main agronomic characters, yield per plant, artemisinin content of the wild and cultivated A. annua of Sichuan province were investigated and determined, and the correlated relationships among them were analyzed.

RESULTIt was showed that the weight of dried stem per plant had very significantly positive correlation with the yield per plant,and the number of primary branches, the diameter of stem had significantly positive correlation with the yield per plant. The flower bud stage, first flowering stage and full-bloom stage had significantly positive correlation with the artemisinin content. The first flowering stage and full-bloom stage had significantly positive correlation with the total artemisinin content per plant. The weight of dried stem per plant,the diameter of stem and the flower bud stage had significantly correlation with the total artemisinin content per plant. A. annua with the purple-stem had significant higher artemisinin content than that with the green-stem. Through the multiple regression analysis, the classic multiple regression equation of the yield per plant was gained as Y = 0.06121-0.000 08X(1) + 0.30378X(3) - 0.00051X(4) - 0.00031X5 (F = 20.15, P < 0.0001), the classic multiple regression equation of the artemisinin content as Y = -1.45849 - 0.00099X(1) - 0.24079X(3) + 0.13362X(6) - 0.00719X(7) + 0.01454X(9) (F = 46.55, P < 0.0001), the classic multiple regression equation of the total artemisinin content per plant as Y = -2.67001 - 0.00249X(1) + 0.98873X(3) + 0.30037X(6) + 0.113X(9) F = 22.62, P < 0.001).

CONCLUSIONThe plant with purple, thick and strong stem, higher plant height, moderate primary branches number and bloom stage, small stem-branch angle should be selected for a breeding new A. annua varieties with high yield and artemisinin content.

Artemisia annua ; chemistry ; growth & development ; metabolism ; Artemisinins ; analysis ; metabolism ; Biomass ; China ; Flowers ; chemistry ; growth & development ; metabolism

OBJECTIVETo study the relative expression of the genes involved in artemisinin biosynthesis in different tissues including roots, stems, leaves and flowers of Artemisia annua, and establish the relationship between gene expression and artemisinin accumulation, eventually leading to discover the mainly effective genes involved in artemisinin biosynthesis.

METHODThe 7 functional genes involved in artemisinin biosynthesis were detected at the level of expression by using qRT-PCR, and simultaneously the content of artemisinin in the 4 investigated tissues was detected in parallel.

RESULTThe 3 genes including HMGR, DXR and FPS which were involved in the upstream pathway of artemisinin biosynthesis showed the highest expression levels in flowers, and the 4 functional genes including ADS, CYP71AV1, CPR and AAR which were involved in the artemisinin-specific biosynthetic pathway were found to be expressed in all the 4 detected tissues. The highest expression level of ADS was found in leaves, then followed by flowers, and the lowest expression level of ADS was found in roots and stems. CYP71AV1 had highest expression level in flowers and lowest in leaves. CPR showed highest expression level in flowers, and AAR had lower expression levels in the other 3 artemisinin-specific pathway genes in all the tissues. The highest content of artemisinin was found in leaves (0.343 mg x g(-1)), then followed by flowers (0.152 mg x g(-1)), roots (0.062 mg x g(-1)) and stems (0.060 mg x g(-1)).

CONCLUSIONIn the biosynthesis of artemisinin, the upstream genes including HMGR from the MVA pathway, DXR from the MEP pathway and the checkpoint gene FPS were much more active in flowers, and this suggested that flowers might be the tissues of artemisinin precursor biosynthesis, and further DXR contributed more to artemisinin biosynthesis. The positive correlation of ADS expression and artemisinin content in tissues demonstrated that ADS played a very important role in artemisinin biosynthesis, which was the ideal target for engineering the artemisinin biosynthetic pathway. In summary, the functional genes involved in artemisinin biosynthesis do not express at the same level but synergistically.

Artemisia annua ; chemistry ; genetics ; metabolism ; Artemisinins ; metabolism ; Plant Proteins ; genetics ; metabolism ; Polymerase Chain Reaction

OBJECTIVEA pot experiment with variable fertilizer treatments was carried out to study the influence of fertilization on the concentration and accumulation of polyphenols, scopoletin, chrysosplenol-D and chrysosplenetin in roots, stems and leaves and their antioxidant activities. The main aims were to fertilize scientifically in cultivation of Artemisia annua and improve the quality of the harvest organs.

METHODThese active components in leaves, stems and roots in the squaring stage were analyzed by HPLC and antioxidant activities of the extracts were evaluated by ultraviolet visible light colorimetric method.

RESULTThe result showed the highest concentration of polyphenols, scopoletin, chrysosplenol-D and chrysosplenetin was in leaves, followed by stems and the lowest in roots. The antioxidant activities of the leaf extracts correlated positively with the concentrations of polyphenols, scopoletin, chrysosplenol-D and chrysosplenetin. Furthermore, fertilization promoted significantly the growth of A. annua, the biomass was increased by 57.37% (chemical fertilizer), 91.63% (mixture of chemical fertilizer and manure) and 92.27% (manure), respectively, compared to the blank control (without fertilizer). Fertilization, particularly mixture fertilization of chemical fertilizer and manure, increased generally the concentration and accumulation of polyphenols, scopoletin, chrysosplenol-D and chrysosplenetin as well as DPPH x scavenging ratio.

CONCLUSIONScopoletin, chrysosplenol-D and chrysosplenetin could be synthesized and stored mainly in leaves. The leaves might thus be the chief organ of A. annua for medical treatment. Finally, the mixture fertilization of chemical fertilizer and manure should be used to increase the yield and quality of A. annua.

Antioxidants ; analysis ; metabolism ; Artemisia annua ; chemistry ; growth & development ; metabolism ; Fertilizers ; analysis ; Phenols ; analysis ; metabolism ; Plant Leaves ; chemistry ; growth & development ; metabolism ; Plant Roots ; chemistry ; growth & development ; metabolism

In this study, we investigate the bioaccessibility of heavy metals (Cu, Pb, As, Cd and Hg) in wild Artemisia annua and use target hazard quotients (THQ) proposed by US Environmental Protection Agency to assess the health risk under the heavy metal exposure. The results showed that the bioaccessibility of Cu, Pb, As, Cd and Hg in A. annua are 0.77, 0.66, 0.46, 0.68 and 0, respectively, and that the value of THQ for adults and children were 0.030 and 0.025 calculated by risk assessment model. The results indicated that the heavy metals in A. annua were not able to be completely absorbed by human body and that their contents were in a safe range. In this study, by combining the bioavailability of heavy metal and health risk assessment, we assessed the security of heavy metals of wild A. annua, which will provide reference for the standard of heavy metals for medicinal materials.
Artemisia annua ; chemistry ; metabolism ; Consumer Product Safety ; Drug Contamination ; Humans ; Metals, Heavy ; analysis ; metabolism ; Risk Assessment ; Soil Pollutants ; analysis ; metabolism

OBJECTIVETo observe the effects of intervention of moxa smoke with different concentrations on superoxide dismutase (SOD) and malondialdehyde (MDA) in serum and lung of male rats, so as to explore the safety concentration of moxa smoke.

METHODSA total of 32 Wistar male rats were randomly divided into a control group, a low-concentration group, a moderate-concentration group and a high-concentration group, 8 rats in each one. All the rats were exposed in the full-automatic toxicant exposure cabinet, and the overshadow of moxa smoke was set at 0%, 10%, 40% and 70%, respectively. Each rat was exposed for 20 min per day. After 26 weeks, the activities of SOD and content of MDA in serum, lung organ and bronchoalveolar lavage fluid were tested.

RESULTSCompared with the control group, the activities of serum SOD in the high-concentration group were reduced (P< 0. 05), but those in the low-concentration group and moderate-concentration group were not significantly different (both P>0. 05). Compared with the control group, the content of serum MDA in the low-concentration group, moderate-concentration group and high-concentration group was increased insignificantly (all P>0. 05). There were no significant differences regarding activities of SOD and content of MDA in lung organ and bronchoalveolar lavage fluid among each moxa smoke group (all P>0. 05).

CONCLUSIONThere is no obvious toxic reaction in the low-concentration group and moderate-concentration group; in the high-concentration group the antioxidant ability is damaged due to long-term exposure.

Animals ; Artemisia ; chemistry ; Lung ; enzymology ; metabolism ; Male ; Malondialdehyde ; blood ; metabolism ; Moxibustion ; Rats ; Rats, Wistar ; Smoke ; analysis ; Superoxide Dismutase ; blood ; metabolism

OBJECTIVETo explore the effects of three Chinese herbal antidotes, i.e. Herba Artemisiae annuae (A), Herba Hedyotis diffusae (H) and Rhizoma Cimicifugae (C), all were ingredients of Jiedu Quyu Ziyin Recipe, for adjusting the regulated on activation normal T cell expressed and secreated (RANTES), gene expression in serum and renal tissue of MRL/lpr mice.

METHODSFifty-four MRL/lpr mice were randomized into 9 groups, with 6 in each, and intragastrically infused with A, H, C, A+H, H+C, A+C, A+H+C (all in dosage-form of decoction), prednisone suspension and physiological saline, respectively for 12 weeks. RANTES expression in serum and renal tissue of animals were detected with ELISA and RT-PCR at the end of the study.

RESULTSLevels of RANTES expression was significantly reduced in the prednisone treated group after treatment. Excepting no significant change being observed in the groups treated with A and C, the changes in the other groups were all milder than those in the group treated with A+H+C.

CONCLUSIONChinese herbal antidotes A, H and C in combination can significantly inhibit the RANTES expression in serum and renal tissue of MRL/lpr mice.

Animals ; Artemisia annua ; chemistry ; Chemokine CCL5 ; blood ; metabolism ; Cimicifuga ; chemistry ; Drugs, Chinese Herbal ; pharmacology ; Female ; Hedyotis ; chemistry ; Kidney ; metabolism ; Mice ; Mice, Inbred MRL lpr ; T-Lymphocytes ; immunology ; metabolism

Artemisia lactiflora is an important medicinal plant in China. The antitumor and antioxidant activities of the extracts of 54 endophytic fungi from the plant were screened via MTT assay and DPPH scavenging radical assay, respectively. The bioactive strains were identified based on similarity of 5.8S gene and internal transcribed spacer (ITS) sequences. The results showed that extracts from ten (18.5%) isolates exhibited antitumor activity, and which from two (3.7%) isolates exhibited antioxidant activity. The Alternaria sp. GYBH47 strain was simultaneously having antagonistic activity against HL-60 leukemia, MCF-7 breast and COLO205 colon cell lines, and Phomopsis sp. GYBH42 strain having cytotoxic and antioxidant activities. The results indicated that endophytic fungi from Artemisia lactiflora are potential resources to find valuable bioactive components.
Antineoplastic Agents ; chemistry ; pharmacology ; Artemisia ; microbiology ; Biphenyl Compounds ; metabolism ; Cell Line, Tumor ; Endophytes ; chemistry ; classification ; physiology ; Free Radical Scavengers ; chemistry ; pharmacology ; Fungi ; classification ; physiology ; Humans ; Picrates ; metabolism

The different components of crude mycelium of the predominant endophytic Colletotrichum gloeosporioides of Artemisa annua have been extracted by the methods of acid hydrolysate. We compared the effect of the isolated components on artemisin biosynthesis in hairy root cultures. Therefore, the oligosaccharide elicitor from C. gloeosporioides has been partially purified by column chromatography of Sephadex G25. The isolated oligosaccharide B II (elicitor, MW < 2500) has been revealed to promote the production of artemisinin in Artemisia annua hairy root cultures. When hairy roots of 23-day old cultures (later growth phase) were exposed to the elicitor at 0.4 mg/mL for 4 days, the maximum production of artemisinin reached to 13.51 mg/L, a 51.63% increase over the control. This is the first report on the stimulation of artemisinin production in hairy roots by the oligosaccharide elicitor from an endophytic fungus of A. annua.
Artemisia annua ; drug effects ; growth & development ; metabolism ; Artemisinins ; metabolism ; Bioreactors ; Colletotrichum ; chemistry ; Mycelium ; chemistry ; Oligosaccharides ; isolation & purification ; pharmacology ; Plant Roots ; drug effects ; growth & development ; metabolism

OBJECTIVETo study the accumulation and translocation of cadmium in the soil and Artemisia annua, and observe its effects on growth of A. annua and artemisinin content.

METHODA. annua were cultivated in pots with Cd concentration at 0.5, 1.5, 4.5 mg x kg(-1) level, respectively.

RESULT AND CONCLUSIONThe growth of A. annua was inhibited at all the Cd levels characterized by the decreases of biomass and agronomic parameters; Most of Cd was accumulated in the roots of A. annua, and the ratios of Cd concentrations in roots and aerial part were 1.8:1 and 2.3:1 at 1.5, 4.5 mg x kg(-1) Cd level, respectively. Artemisinin content increased significant at 0.5 mg x kg(-1) Cd level, but there were no significant changes comparing with control group other Cd levels.

Artemisia annua ; chemistry ; drug effects ; growth & development ; metabolism ; Artemisinins ; analysis ; metabolism ; Cadmium ; analysis ; metabolism ; toxicity ; Plant Extracts ; analysis ; metabolism ; Soil Pollutants ; analysis ; metabolism ; toxicity

The present study was designed to establish a suitable assay to explore CCR2b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure-activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2b receptor, which shed lights on the development of novel drugs as CCR2b receptor antagonists for preventing inflammation related diseases.
Artemisia ; chemistry ; Asteraceae ; chemistry ; Drug Evaluation, Preclinical ; Humans ; Kinetics ; Plant Extracts ; chemistry ; pharmacology ; Receptors, CCR2 ; antagonists & inhibitors ; genetics ; metabolism ; Structure-Activity Relationship