The insecticidal activities of methanol extracts of Cordyceps militaris Link (Ascomycotina: Clavicipitaceae) cultured on fresh pupae of Bombyx mori L against 3rd-instar larvae of Plutella xylostella L were examined using direct contact application. The larvicidal activity was more pronounced in an extract of C militaris fruiting body than in an extract of the pupae separated from the culture. The biologically active constituent of the Cordyceps fruiting body was characterized as cordycepin (3'-deoxyadenosine) by spectroscopic analysis. Responses varied according to dose, exposure time and application method. In a leaf-dipping test, cordycepin at 500 mg litre-1 caused no mortality at 1 DAT (day after treatment) but 78 and 100% mortality at 2 and 4 DAT, respectively, whereas 34 and 88% mortality at 3 and 5 DAT, respectively was observed at 300 mg litre-1. Cordycepin caused body colour change from pale green to dark brown and eventually body lysis. These results suggested that the larvicidal action may be attributable to a direct effect rather than an inhibitory action on chitin synthesis. There was a significant difference in insecticidal activity of cordycepin between leaf dipping (500 mg litre-1) with 100% mortality and topical application (10 micrograms per larva) with 0% mortality, suggesting that cordycepin has stomach action. Cordycepin merits further study as a potential P xylostella control agent or as a lead compound.

Quisqualis indica (QI) has been used for treating disorders such as stomach pain, constipation, and digestion problem. This study was aimed to evaluate the therapeutic efficacy of QI extract on treating benign prostatic hyperplasia (BPH) in LNCaP human prostate cancer cell line and a testosterone-induced BPH rat model. LNCaP cells were treated with QI plus testosterone propionate (TP), and androgen receptor (AR) and prostate specific antigen (PSA) expression levels were assessed by Western blotting. To induce BPH, the rats were subjected to a daily subcutaneous injection of TP (3 mg/kg) for 4 weeks. The rats in treatment group were orally gavaged with QI (150 mg/kg) together with the TP injection. In-vitro studies showed that TPinduced increases in AR and PSA expression in LNCaP cells were reduced by QI treatment. In BPH-model rats, the prostate weight, testosterone in serum, dihydrotestosterone (DHT) concentration and 5α-reductase type 2 mRNA expression in prostate tissue were significantly reduced following the treatment with QI. TPinduced prostatic hyperplasia and the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 were significantly attenuated in QI-treated rats. In addition, QI induced apoptosis by up-regulating caspase-3 and -9 activity and decreasing the B-cell lymphoma 2 (Bcl-2)/Bcl-2-associated X protein (Bax) ratio in prostate tissues of BPH rats. Further investigation showed that TP-induced activation of AKT and glycogen synthase kinase 3β (GSK3β) was reduced by QI administration. Therefore, our findings suggest that QI attenuates the BPH state in rats through anti-proliferative and pro-apoptotic activities and might be useful in the clinical treatment of BPH.Key words benign prostatic hyperplasia; dihydrotestosterone; Quisqualis indica; testosterone Benign prostatic hyperplasia (BPH) is a common urogenital disorder that affects up to 85% of males who are over 50 years-old. 1) BPH is characterized by the increased proliferation of epithelial and stromal cells of the prostate.2) BPH generally causes lower urinary tract symptoms (LUTS), such as incomplete bladder emptying, bladder obstruction, bloody urination, and frequent urination.3)The etiology of BPH is not entirely clear. However, the development and incidence of BPH are associated with dysregulation of androgens, and with increased proliferation and decreased apoptosis of cells in the prostate gland.4-9) Testosterone and dihydrotestosterone (DHT) have key roles in the development and growth of the entire male genital tract, and they stimulate differentiation of the prostate gland. 10,11) The adrenal glands and testes synthesize testosterone, and prostatic 5α-reductase type 2 converts it to DHT. 12) DHT then binds to the androgen receptor (AR), which is transported to the nucleus, where it regulates genes important for prostate growth and differentiation. 4) BPH development and progression are associated with activation of the AKT pathway, a major growth factor-mediated signal transduction pathways. 6)Over-stimulation of the ...

The growth-inhibiting activities of materials derived from the fruiting body of Cordyceps militaris cultured on Bombyx mori pupae (CM-1) and pupae separated from the culture (CM-2), and the fruiting body of Paecilomyces japonica cultured on B. mori pupae (PJ-1) and pupae separated from the culture (PJ-2), fresh B. mori larvae (BML), fresh B. mori female pupae (BMP), and Morus alba leaves (MAL) towards eight lactic acid-producing bacteria and 11 harmful intestinal bacteria were examined using an impregnated paper disc bioassay. At 10 mg per disc, methanolic extracts from CM-1 and CM-2 strongly inhibited growth of Clostridium difficile ATCC 9689, C. paraputrificum ATCC 25780, and C. perfringens ATCC 13124 without adverse effects on the growth of eight lactic acid-producing bacteria and the other eight harmful bacteria. The methanolic extracts from PJ-1, PJ-2, BML, BMP, and MAL did not affect growth of all test bacteria. The growth-inhibiting principle of CM-1 and CM-2 towards test clostridia was characterized as cordycepin by spectroscopic analysis. The contents of cordycepin in dried CM-1 and CM-2 were 0.69% and 0.54%, respectively. These results suggest that cordycepin may be produced from the fruiting body of C. militaris cultured on B. mori pupae and then translocated to its host insect and accumulated. Structure-growth inhibition relationships of cordycepin and its eight derivatives against C. perfringens ATCC 13124 indicate that a deoxy form at either 3 or 2 position appears critical for the inhibitory activity. Natural cordycepin and its two analogues, 2 -deoxyadenosine and tubercidin, merit further study as a potential antibacterial agent against various diseases caused by harmful intestinal bacteria such as clostridia.