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Deoxyartemisinin, a compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities. 10-Deoxoartemisinin is a novel compound with a strong antimalarial effect derivatized from artemisinin. Compared to the famous antimalarial natural compound artemisinin, deoxyartemisinin lacks the peroxide bridge structure, while 10-deoxoartemisinin remains this special peroxide bridge group but loses the 10-position keto group. To clarify their pharmacological differences, the absorption, distribution, metabolism, excretion (ADME) properties of artemisinin, deoxyartemisinin, and 10-deoxoartemisinin were first predicted using QikProp software. Also, their pharmacokinetic behaviors in rats were further evaluated by a rapid, sensitive, and specific liquid chromatography–tandem mass spectrometry (LC–MS/MS) method after oral and intravenous administration of each compound, in which deoxyartemisinin and 10-deoxoartemisinin were first evaluated for their pharmacokinetics. All parameters about ADME properties calculated by software met the criteria and the ADME performance order was 10-deoxoartemisinin > deoxyartemisinin > artemisinin. The oral bioavailability of artemisinin was calculated to be 12.2 ± 0.832%, which was about 7 times higher than that of deoxyartemisinin (1.60 ± 0.317%). For 10-deoxoartemisinin, its bioavailability (26.1 ± 7.04%) was superior to artemisinin at a degree of more than twice. Considering their chemical structures, losing the peroxide bridge might decrease the absorption rate of deoxyartemisinin in the gastrointestinal tract, while retaining the peroxide bridge but losing the 10-position ketone might improve the bioavailability of 10-deoxoartemisinin.

No abstract

Neoseiulus womersleyi (Acari: Phytoseiidae) used to be the dominant species in fruit-tree orchards throughout Japan, but starting in the 1990s, N. womersleyi began to be displaced by Neoseiulus californicus in central and southwestern Japan. The present study was conducted to examine factors explaining the displacement of N. womersleyi by N. californicus. First, we confirmed under laboratory conditions that N. californicus could exclude N. womersleyi if they initially coexisted in a 1:1 ratio. During a 2-h continuous observation period, none of the heterospecific pairs had copulated and after 5 days together with heterospecific males, none of the females had laid eggs. When these females were placed with conspecific males, normal numbers of offspring were produced. Moreover, conspecific matings were not substantially disturbed in the presence of heterospecific males or females. Total fecundity was significantly lower in N. womersleyi than in N. californicus, but their r m values did not differ from each other. On the other hand, the frequency of intraguild predation by N. californicus on N. womersleyi was significantly higher than vice versa. From these results, we concluded that not reproductive interference nor differential female fecundity but asymmetrical intraguild predation seemed to explain the competitive exclusion of N. womersleyi by N. californicus.

No abstract